Our Group
We are a team of PhD students, master students, postdocs and technicians with expertise in chemistry, biochemistry, biology and pharmaceutical sciences working together towards our common goals on diverse projects in the field of radiopharmaceutical sciences as outlined below.
Background
Radiopharmaceutical sciences is an interdisciplinary field of applied research that combines expertise in physics, (radio)chemistry, (radio)biology, (radio)pharmacy and (nuclear) medicine with the aim to develop and investigate radiopharmaceuticals in view of their clinical application.
The development of radiopharmaceuticals for tumor targeting includes the design, synthesis and radiolabeling of tumor-specific ligands, their preclinical in vitro and in vivo evaluation and – in an ideal case – their clinical translation and application in nuclear medicine/oncology.
Nuclear imaging makes use of radiopharmaceuticals that – based on the employed radionuclide – emit gamma-radiation or positrons for Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET), respectively. The detection of the emitted radiation provides information about (patho)physiological processes on a molecular level and enables diagnosis and staging of a (cancer) diseases.
Targeted radionuclide therapy or endoradiotherapy makes use of radiopharmaceuticals that – based on the employed radionuclide – emit alpha particles, beta minus particles and/or Auger electrons. The specific accumulation of therapeutic radiopharmaceuticals in malignant lesions enables direct irradiation of cancer cells and is, thus, a strategy of particular value for the treatment of metastatic disease.
Nuclear imaging is most often employed for the staging and restaging of cancer diseases before and after therapy. It enables the detection of metastatic disease and demonstrates whether the applied therapy is effective in reducing the tumor burden. The concept of “radiotheragnostics” using target-specific radiopharmaceuticals pursues an additional goal in that the diagnostic image provides information about the expression of a specific therapeutic target which is useful for subsequent application of radionuclide therapy. This concept has been implemented in clinical routine for patients with cancer types that express for example the somatostatin receptor or prostate-specific membrane antigen for which targeted radionuclide therapies exist. In future, radioimaging agents may also serve for the selection of patients with diseases who could profit from other treatment options such as tumor target-specific (immuno)therapies.
Research Interests
The research of our group is dedicated to the design and evaluation of small-molecular-weight tumor targeting radioligands for theragnostic application, among those are radioconjugates for folate receptor (FR)-targeting as well as for targeting the prostate-specific membrane antigen (PSMA).
Our goal is to optimize the pharmacokinetic profile of the radioligands by various chemical modifications such as the derivatization with albumin-binding entities.
A major interest lies in the application and (radio)biological investigation of different radiation types using non-standard (exotic) radionuclides, which are promising for the development of the theragnostic concept.
In view of a therapeutic application, we are interested in the combination of targeted radionuclide therapy with other cancer treatments (e.g. chemotherapy, immunotherapy).
Research Projects
The development of radiopharmaceuticals with favorable pharmacokinetics requires the synthesis of compound libraries to gain knowledge about structure-activity relationships, which can subsequently be used for structural optimization. For this reason, our research group established synthetic methods for the fast and easy preparation of a broad range of structurally modified tumor-targeting folate conjugates.
The folate radioconjugates accumulated specifically in folate receptor (FR)-positive tumor tissue, however, a significant amount of activity was retained in the kidneys. A major breakthrough was achieved by the derivatization of folate radioconjugates with an albumin-binding entity. The enhanced blood circulation of these novel class of folate radioconjugates resulted in an increased uptake of activity in the tumor, but reduced retention in the kidneys.
This promising approach was translated also to PSMA-targeted radioligands. It resulted in the development of new PSMA radioligands that show great potential for therapeutic application. Current projects focus on the optimization of the pharmacokinetic properties of these and other tumor targeting agents using different types of albumin binder and linker entities, respectively.
Non-standard (exotic) radionuclides are developed and produced by the Radionuclide Development group (headed by Dr. Nicholas van der Meulen).
The group is particularly interested in radionuclides of the same element (radioisotopes) which allow the preparation of chemically identical radiopharmaceuticals for imaging and therapy, respectively. Scandium comprises three medically interesting radioisotopes: 43Sc and 44Sc are useful for positron emission tomography (PET) and 47Sc is a radioisotope for therapeutic application and single photon emission computed tomography (SPECT). Over the last decade we have been investigating scandium radioisotopes in several preclinical studies.
A large number of pioneering studies have been performed with terbium sister radioisotopes. Terbium is unique as it comprises four radioisotopes for all four modalities in nuclear medicine, including SPECT (155Tb), PET (152Tb), alpha (149Tb) and beta radionuclide therapy (161Tb). Over the last decade, we have performed studies with all four radioisotopes in preclinical settings.
Currently, several preclinical projects are on-going with terbium sister radioisotopes in the group and in collaboration with external partners.
161Tb is the most advanced in terms of production and preclinical investigations. Tumor-cell based in vitro studies, in which the effect of 161Tb-PSMA-617 was compared to that of 177Lu-PSMA-617, demonstrated the advantage of using 161Tb over 177Lu due to the co-emission of a substantial number of conversion and Auger electrons.
Recently, new projects have been initiated with regard to more in-depth studies using other exotic radionuclides such as 175Yb and 165Er.
Over the last years, we have been investigating the radiosensitizing effects of chemotherapeutic agents (e.g. the antifolate pemetrexed).
Our group investigated the effect of radiation to enhance the tumor response to immunotherapy. In a recently performed preclinical study, our group demonstrated the effect of 177Lu-DOTA-folate as an immune stimulus to enhance anti-CTLA-4 immunotherapy in a syngeneic breast tumor mouse model.
18F-AzaFol, a PET agent for imaging folate receptor-positive tumors, was investigated in a multicenter clinical trial at three hospitals in Switzerland (NCT03242993).
Several projects are on-going with regard to first-in-man applications of novel PSMA-targeting radioligands and for the investigation of non-standard radionuclides.
The application of 152Tb-PSMA-617 for imaging of prostate-specific membrane antigen (PSMA)-positive prostate cancer, was demonstrated in a patient with metastatic castration-resistant prostate cancer (mCRPC) at Zentralklinik, Bad Berka, Germany.
Prizes and Awards
Marie Curie Award 2021 (EANM, Barcelona, Spain - virtual event)
In October 2021, Viviane Tschan* received the Marie Curie Award at the Annual Meeting of the European Association of Nuclear Medicine (EANM).
*PhD student in the group from 2018-2022
Marie Curie Award 2018 (EANM, Düsseldorf, Germany)
In October 2018, PD Dr. Cristina Müller received the Marie Curie Award at the Annual Meeting of the European Association of Nuclear Medicine (EANM).
Ruzicka Prize 2014 (ETH Zurich, Switzerland)
In November 2014, PD Dr. Cristina Müller received the Ruzicka Prize of the ETH Zurich.
The Ruzicka Prize, named after the ETH professor and Nobel laureate Leopold Ruzicka, is considered one of the most important awards for the promotion of young scientists in the field of chemistry in Switzerland.
Presentation Prize 2021 (Doktorandentag, Institute of Pharmaceutical Sciences, ETH Zurich, Switzerland)
In February 2021, Luisa Deberle* won the Award for Best Oral Presentation
Presentation title: "Novel Synthetic Strategies for the Development of Diverse Folate Radioconjugates"
*PhD student in the group from 2018-2022
Presentation Prize 2019 (SGNM, St. Gallen, Switzerland)
In June 2019, PD Dr. Cristina Müller was awarded with the Presentation Prize 2019 of the Swiss Society of Nuclear Medicine (SGNM)
Presentation title: "161Tb-based Prostate Cancer Therapy: Investigation of the 177Lu-PLUS Effect"
August-Abegg-Fonds Prize 2018 (Doktorandentag, Institute of Pharmaceutical Sciences, ETH Zurich)
Christoph Umbricht* was awarded for the best oral presentation
Presentation title: "Preclinical development of novel PSMA-targeting radioligands - modulation of albumin-binding properties to improve prostate cancer therapy"
*PhD student in the group from 2015-2019
Poster Prize 2021 (77th Annual Meeting of the Swiss Society of Urology, Interlaken, Switzerland)
In September 2021, Viviane Tschan* was awarded a Poster Prize in the "Basic Science" Category
Presentation title: "Improved Radionuclide Therapy of Prostate Cancer - Preclinical Comparison of the Albumin-binding [177Lu]Lu-Ibu-DAB-PSMA to [177Lu]Lu-PSMA"
*PhD student in the group from 2018-2022
Best Virtual Poster Award 2021 (Swiss Chemical Society and DSM Nutritional Products)
In September 2021, Luisa Deberle* was awarded the Best Virtual Poster in the "Medicinal Chemistry" Category
Poster title: "Novel Synthetic Strategies Enable the Efficient Development of Folate Conjugates for Radiotheragnostic Application"
*PhD student in the group from 2018-2022
Alavi-Mandell Award 2022
In June 2022, Patrycja Guzik* received the Alavi-Mandell Award as a First Author of the following publication :
"Identification of a PET Radiotracer for Imaging of the Folate Receptor-α: A Potential Tool to Select Patients for Targeted Tumor Therapy"
Authors: Patrycja Guzik, Hsin-Yu Fang, Luisa M. Deberle, Martina Benešová, Susan Cohrs, Silvan D. Boss, Simon M. Ametamey, Roger Schibli, Cristina Müller*
*PhD student in the group from 2017-2021
Best Paper 2020 in Eur J Nucl Med Mol Imaging
In October 2021, the following article was selected for the EANM Springer Prize (one out of three)
"Terbium-161 for PSMA-targeted radionuclide therapy of prostate cancer"
Authors: Cristina Müller*, Christoph A. Umbricht, Nadezda Gracheva, Viviane J. Tschan, Giovanni Pellegrini, Peter Bernhardt, Jan Rijn Zeevaart, Ulli Köster, Roger Schibli, Nicholas P. van der Meulen
Award for the best publication in EJNMMI Research in 2018
44Sc-PSMA-617 for radiotheragnostics in tandem with 177Lu-PSMA-617—preclinical investigations in comparison with 68Ga-PSMA-11 and 68Ga-PSMA-617
Authors: Christoph A. Umbricht, Martina Benešová, Raffaella M. Schmid, Andreas Türler, Roger Schibli, Nicholas P. van der Meulen and Cristina Müller*
Scientific Contributions
Publications
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Corpetti M, Müller C, Beltran H, de Bono J, Theurillat JP
Prostate-specific membrane antigen–targeted therapies for prostate cancer: towards improving therapeutic outcomes
European Urology. 2024; 85(3): 193-204. https://doi.org/10.1016/j.eururo.2023.11.018
DORA PSI -
Favaretto C, Grundler PV, Talip Z, Köster U, Johnston K, Busslinger SD, et al.
Terbium-149 production: a focus on yield and quality improvement towards preclinical application
Scientific Reports. 2024; 14(1): 3284 (12 pp.). https://doi.org/10.1038/s41598-024-53610-2
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Fricke J, Westerbergh F, McDougall L, Favaretto C, Christ E, Nicolas GP, et al.
First-in-human administration of terbium-161-labelled somatostatin receptor subtype 2 antagonist ([161Tb]Tb-DOTA-LM3) in a patient with a metastatic neuroendocrine tumour of the ileum
European Journal of Nuclear Medicine and Molecular Imaging. 2024; 51: 2517-2519. https://doi.org/10.1007/s00259-024-06641-w
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Gomes CV, Mendes BM, Paixão L, Gnesin S, Müller C, van der Meulen NP, et al.
Comparison of the dosimetry of scandium-43 and scandium-44 patient organ doses in relation to commonly used gallium-68 for imaging neuroendocrine tumours
EJNMMI Physics. 2024; 11(1): 61 (14 pp.). https://doi.org/10.1186/s40658-024-00669-5
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Sarogni P, Brindani N, Zamborlin A, Gonnelli A, Menicagli M, Mapanao AK, et al.
Tumor growth-arrest effect of tetrahydroquinazoline-derivative human topoisomerase II-alpha inhibitor in HPV-negative head and neck squamous cell carcinoma
Scientific Reports. 2024; 14(1): 9150 (10 pp.). https://doi.org/10.1038/s41598-024-59592-5
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Song Y, Zou J, Castellanos EA, Matsuura N, Ronald JA, Shuhendler A, et al.
Theranostics - a sure cure for cancer after 100 years?
Theranostics. 2024; 14(6): 2464-2488. https://doi.org/10.7150/thno.96675
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Vaccarin C, Mapanao AK, Deberle LM, Becker AE, Borgna F, Marzaro G, et al.
Design and preclinical evaluation of a novel prostate-specific membrane antigen radioligand modified with a transthyretin binder
Cancers. 2024; 16(7): 1262 (13 pp.). https://doi.org/10.3390/cancers16071262
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Vaccarin C, Veit G, Hegedus T, Torres O, Chilin A, Lukacs GL, et al.
Synthesis and biological evaluation of pyrazole-pyrimidones as a new class of correctors of the cystic fibrosis transmembrane conductance regulator (CFTR)
Journal of Medicinal Chemistry. 2024; 67: 13891-13908. https://doi.org/10.1021/acs.jmedchem.4c00685
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Wallimann RH, Hensinger H, Müller C, Schibli R, Kneuer R, Schindler P
Liquid chromatography ICP-MS to assess the stability of 175Lu- and natGa-based tumor-targeting agents towards the development of 177Lu- and 68Ga-labeled radiopharmaceuticals
Pharmaceutics. 2024; 16(3): 299 (13 pp.). https://doi.org/10.3390/pharmaceutics16030299
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Beyer D, Vaccarin C, Deupi X, Mapanao AK, Cohrs S, Sozzi-Guo F, et al.
A tool for nuclear imaging of the SARS-CoV-2 entry receptor: molecular model and preclinical development of ACE2-selective radiopeptides
EJNMMI Research. 2023; 13(1): 32 (14 pp.). https://doi.org/10.1186/s13550-023-00979-2
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Busslinger SD, Becker AE, Vaccarin C, Deberle LM, Renz M-L, Groehn V, et al.
Investigations using albumin binders to modify the tissue distribution profile of radiopharmaceuticals exemplified with folate radioconjugates
Cancers. 2023; 15(17): 4259 (19 pp.). https://doi.org/10.3390/cancers15174259
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Ermini ML, Summa M, Zamborlin A, Frusca V, Mapanao AK, Mugnaioli E, et al.
Copper nano-architecture topical cream for the accelerated recovery of burnt skin
Nanoscale Advances. 2023; 5(4): 1212-1219. https://doi.org/10.1039/d2na00786j
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Favaretto C, Grundler PV, Talip Z, Landolt S, Sepini L, Köster U, et al.
161Tb-DOTATOC production using a fully automated disposable cassette system: a first step toward the introduction of 161Tb into the clinic
Journal of Nuclear Medicine. 2023; 64(7): 1138-1144. https://doi.org/10.2967/jnumed.122.265268
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Müller C, van der Meulen NP, Schibli R
Opportunities and potential challenges of using terbium-161 for targeted radionuclide therapy in clinics
European Journal of Nuclear Medicine and Molecular Imaging. 2023; 50: 3181-3184. https://doi.org/10.1007/s00259-023-06316-y
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Sarogni P, Zamborlin A, Mapanao AK, Logghe T, Brancato L, van Zwol E, et al.
Hyperthermia reduces irradiation-induced tumor repopulation in an in vivo pancreatic carcinoma model
Advanced biology. 2023; 7(10): 2200229 (9 pp.). https://doi.org/10.1002/adbi.202200229
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Tschan VJ, Busslinger SD, Bernhardt P, Grundler PV, Zeevaart JR, Köster U, et al.
Albumin-binding and conventional PSMA ligands in combination with 161Tb: biodistribution, dosimetry, and preclinical therapy
Journal of Nuclear Medicine. 2023; 64(10): 1625-1631. https://doi.org/10.2967/jnumed.123.265524
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Wallimann RH, Schindler P, Hensinger H, Tschan VJ, Busslinger SD, Kneuer R, et al.
Inductively coupled plasma mass spectrometry - a valid method for the characterization of metal conjugates in view of the development of radiopharmaceuticals
Molecular Pharmaceutics. 2023; 20(4): 2150-2158. https://doi.org/10.1021/acs.molpharmaceut.2c01092
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Benešová M, Guzik P, Deberle LM, Busslinger SD, Landolt T, Schibli R, et al.
Design and evaluation of novel albumin-binding folate radioconjugates: systematic approach of varying the linker entities
Molecular Pharmaceutics. 2022; 19: 963-973. https://doi.org/10.1021/acs.molpharmaceut.1c00932
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Borgna F, Haller S, Monné Rodriguez JM, Ginj M, Grundler PV, Zeevaart JR, et al.
Combination of terbium-161 with somatostatin receptor antagonists - a potential paradigm shift for the treatment of neuroendocrine neoplasms
European Journal of Nuclear Medicine and Molecular Imaging. 2022; 49: 1113-1126. https://doi.org/10.1007/s00259-021-05564-0
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Borgna F, Deberle LM, Busslinger SD, Tschan VJ, Walde LM, Becker AE, et al.
Preclinical investigations to explore the difference between the diastereomers [177Lu]Lu-SibuDAB and [177Lu]Lu-RibuDAB toward prostate cancer therapy
Molecular Pharmaceutics. 2022; 19(7): 2105-2114. https://doi.org/10.1021/acs.molpharmaceut.1c00994
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Busslinger SD, Tschan VJ, Richard OK, Talip Z, Schibli R, Müller C
[225Ac]Ac-SibuDAB for targeted alpha therapy of prostate cancer: preclinical evaluation and comparison with [225Ac]Ac-PSMA-617
Cancers. 2022; 14(22): 5651 (16 pp.). https://doi.org/10.3390/cancers14225651
DORA PSI -
Che PP, Mapanao AK, Gregori A, Ermini ML, Zamborlin A, Capula M, et al.
Biodegradable ultrasmall-in-nano architectures loaded with cisplatin prodrug in combination with ionizing radiation induces DNA damage and apoptosis in pancreatic ductal adenocarcinoma
Cancers. 2022; 14(12): 3034 (17 pp.). https://doi.org/10.3390/cancers14123034
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Di Liddo R, Verona M, Vaccarin C, Acquasaliente L, Schrenk S, Piccione M, et al.
Preliminary discovery of small molecule inhibitors of Epidermal Growth Factor Receptor (EGFR) that bind to the extracellular domain
Cancers. 2022; 14(15): 3647 (22 pp.). https://doi.org/10.3390/cancers14153647
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Franceschinis E, Roverso M, Gabbia D, De Martin S, Brusegan M, Vaccarin C, et al.
Self-emulsifying formulations to increase the oral bioavailability of 4,6,4′-trimethylangelicin as a possible treatment for cystic fibrosis
Pharmaceutics. 2022; 14(9): 1806. https://doi.org/10.3390/pharmaceutics14091806
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Hemmingsson J, Svensson J, van der Meulen NP, Müller C, Bernhardt P
Active bone marrow S-values for the low-energy electron emitter terbium-161 compared to S-values for lutetium-177 and yttrium-90
EJNMMI Physics. 2022; 9(1): 65 (13 pp.). https://doi.org/10.1186/s40658-022-00495-7
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Miller IS, Khan S, Shiels LP, Das S, O' Farrell AC, Connor K, et al.
Implementing subtype-specific pre-clinical models of breast cancer to study pre-treatment aspirin effects
Cancer Medicine. 2022; 11(20): 3820-3836. https://doi.org/10.1002/cam4.4756
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Tschan VJ, Borgna F, Schibli R, Müller C
Impact of the mouse model and molar amount of injected ligand on the tissue distribution profile of PSMA radioligands
European Journal of Nuclear Medicine and Molecular Imaging. 2022; 49: 470-480. https://doi.org/10.1007/s00259-021-05446-5
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Tschan VJ, Borgna F, Busslinger SD, Stirn M, Monné Rodriguez JM, Bernhardt P, et al.
Preclinical investigations using [177Lu]Lu-Ibu-DAB-PSMA toward its clinical translation for radioligand therapy of prostate cancer
European Journal of Nuclear Medicine and Molecular Imaging. 2022; 49: 3639-3650. https://doi.org/10.1007/s00259-022-05837-2
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Tupini C, Chilin A, Rossi A, De Fino I, Bragonzi A, D’Aversa E, et al.
New TMA (4,6,4′-trimethyl angelicin) analogues as anti-inflammatory agents in the treatment of cystic fibrosis lung disease
International Journal of Molecular Sciences. 2022; 23(22): 14483 (20 pp.). https://doi.org/10.3390/ijms232214483
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Vaccarin C, Gabbia D, Franceschinis E, De Martin S, Roverso M, Bogialli S, et al.
Improved trimethylangelicin analogs for cystic fibrosis: design, synthesis and preliminary screening
International Journal of Molecular Sciences. 2022; 23(19): 11528 (14 pp.). https://doi.org/10.3390/ijms231911528
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Baum RP, Singh A, Kulkarni HR, Bernhardt P, Rydén T, Schuchardt C, et al.
First-in-human application of terbium-161: a feasibility study using 161Tb-DOTATOC
Journal of Nuclear Medicine. 2021; 62(10): 1391-1397. https://doi.org/10.2967/jnumed.120.258376
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Bernhardt P, Svensson J, Hemmingsson J, van der Meulen NP, Zeevaart JR, Konijnenberg MW, et al.
Dosimetric analysis of the short-ranged particle emitter 161Tb for radionuclide therapy of metastatic prostate cancer
Cancers. 2021; 13(9): 2011 (13 pp.). https://doi.org/10.3390/cancers13092011
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Borgna F, Barritt P, Grundler PV, Talip Z, Cohrs S, Zeevaart JR, et al.
Simultaneous visualization of 161Tb-and 177Lu-labeled somatostatin analogues using dual-isotope SPECT imaging
Pharmaceutics. 2021; 13(4): 536 (13 pp.). https://doi.org/10.3390/pharmaceutics13040536
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Deberle LM, Benešová M, Becker AE, Ratz M, Guzik P, Schibli R, et al.
Novel synthetic strategies enable the efficient development of folate conjugates for cancer radiotheranostics
Bioconjugate Chemistry. 2021; 32(8): 1617-1628. https://doi.org/10.1021/acs.bioconjchem.1c00198
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Favaretto C, Talip Z, Borgna F, Grundler PV, Dellepiane G, Sommerhalder A, et al.
Cyclotron production and radiochemical purification of terbium-155 for SPECT imaging
EJNMMI Radiopharmacy and Chemistry. 2021; 6: 37 (17 pp.). https://doi.org/10.1186/s41181-021-00153-w
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Guzik P, Fang H-Y, Deberle LM, Benešová M, Cohrs S, Boss SD, et al.
Identification of a PET radiotracer for imaging of the folate receptor-α: a potential tool to select patients for targeted tumor therapy
Journal of Nuclear Medicine. 2021; 62(10): 1475-1481. https://doi.org/10.2967/jnumed.120.255760
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Guzik P, Benešová M, Ratz M, Monné Rodríguez JM, Deberle LM, Schibli R, et al.
Preclinical evaluation of 5-methyltetrahydrofolate-based radioconjugates - new perspectives for folate receptor-targeted radionuclide therapy
European Journal of Nuclear Medicine and Molecular Imaging. 2021; 48: 972-983. https://doi.org/10.1007/s00259-020-04980-y
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Guzik P, Siwowska K, Fang H-Y, Cohrs S, Bernhardt P, Schibli R, et al.
Promising potential of [177Lu]Lu-DOTA-folate to enhance tumor response to immunotherapy - a preclinical study using a syngeneic breast cancer model
European Journal of Nuclear Medicine and Molecular Imaging. 2021; 48: 984-994. https://doi.org/10.1007/s00259-020-05054-9
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Haixia X, Oliveira da Silva de Barros A, do Vale Chaves e Mello F, Sozzi-Guo F, Müller C, Gemini-Piperni S, et al.
Graphene: insights on biological, radiochemical and ecotoxicological aspects
Journal of Biomedical Nanotechnology. 2021; 17(1): 131-148. https://doi.org/10.1166/jbn.2021.3006
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Kramer V, Fernández R, Lehnert W, Jiménez-Franco LD, Soza-Ried C, Eppard E, et al.
Biodistribution and dosimetry of a single dose of albumin-binding ligand [177Lu]Lu-PSMA-ALB-56 in patients with mCRPC
European Journal of Nuclear Medicine and Molecular Imaging. 2021; 48: 893-903. https://doi.org/10.1007/s00259-020-05022-3
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Lima TVM, Gnesin S, Strobel K, del Sol Pérez M, Roos JE, Müller C, et al.
Fifty shades of scandium: comparative study of PET capabilities using Sc-43 and Sc-44 with respect to conventional clinical radionuclides
Diagnostics. 2021; 11(10): 1826 (11 pp.). https://doi.org/10.3390/diagnostics11101826
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Müller C, Schibli R, Bernhardt P, Köster U, van der Meulen NP
Terbium radionuclides for theranostics
In: Caplan MJ, ed. Reference module in biomedical sciences. sine loco: Elsevier; 2021:(12 pp.). https://doi.org/10.1016/B978-0-12-822960-6.00076-4
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Talip Z, Borgna F, Müller C, Ulrich J, Duchemin C, Ramos JP, et al.
Production of mass-separated erbium-169 towards the first preclinical in vitro investigations
Frontiers in Medicine. 2021; 8: 643175 (11 pp.). https://doi.org/10.3389/fmed.2021.643175
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Borgna F, Deberle LM, Cohrs S, Schibli R, Müller C
Combined application of albumin-binding [177Lu]Lu-PSMA-ALB-56 and fast-cleared PSMA inhibitors: optimization of the pharmacokinetics
Molecular Pharmaceutics. 2020; 17(6): 2044-2053. https://doi.org/10.1021/acs.molpharmaceut.0c00199
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Deberle LM, Tschan VJ, Borgna F, Sozzi-Guo F, Bernhardt P, Schibli R, et al.
Albumin-binding PSMA radioligands: impact of minimal structural changes on the tissue distribution profile
Molecules. 2020; 25(11): 2542 (16 pp.). https://doi.org/10.3390/molecules25112542
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Deberle LM, Benešová M, Umbricht CA, Borgna F, Büchler M, Zhernosekov K, et al.
Development of a new class of PSMA radioligands comprising ibuprofen as an albumin-binding entity
Theranostics. 2020; 10(4): 1678-1693. https://doi.org/10.7150/thno.40482
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Durán MT, Juget F, Nedjadi Y, Bochud F, Grundler PV, Gracheva N, et al.
Determination of 161Tb half-life by three measurement methods
Applied Radiation and Isotopes. 2020; 159: 109085 (9 pp.). https://doi.org/10.1016/j.apradiso.2020.109085
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Gnesin S, Müller J, Burger IA, Meisel A, Siano M, Früh M, et al.
Radiation dosimetry of 18F-AzaFol: a first in-human use of a folate receptor PET tracer
EJNMMI Research. 2020; 10(1): 32 (12 pp.). https://doi.org/10.1186/s13550-020-00624-2
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Lima TVM, Gnesin S, Nitzsche E, Ortega PG, Müller C, van der Meulen NP
First phantom-based quantitative assessment of scandium-44 using a commercial PET device
Frontiers in Physics. 2020; 8: 241 (10 pp.). https://doi.org/10.3389/fphy.2020.00241
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Marin I, Rydèn T, Van Essen M, Svensson J, Gracheva N, Köster U, et al.
Establishment of a clinical SPECT/CT protocol for imaging of 161Tb
EJNMMI Physics. 2020; 7(1): 45 (16 pp.). https://doi.org/10.1186/s40658-020-00314-x
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Müller C, Schibli R, Maurer B
Can nuclear imaging of activated macrophages with folic acid-based radiotracers serve as a prognostic means to identify COVID-19 patients at risk?
Pharmaceuticals. 2020; 13(9): 238 (8 pp.). https://doi.org/10.3390/ph13090238
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Müller C, Béhé M, Geistlich S, van der Meulen NP, Schibli R
Targeted radiotherapeutics from 'bench-to-bedside'
Chimia. 2020; 74(12): 939-945. https://doi.org/10.2533/CHIMIA.2020.939
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Nedjadi Y, Juget F, Desorgher L, Durán MT, Bochud F, Müller C, et al.
Activity standardisation of 161Tb
Applied Radiation and Isotopes. 2020; 166: 109411 (13 pp.). https://doi.org/10.1016/j.apradiso.2020.109411
DORA PSI -
Nizou G, Favaretto C, Borgna F, Grundler PV, Saffon-Merceron N, Platas-Iglesias C, et al.
Expanding the scope of pyclen-picolinate lanthanide chelates to potential theranostic applications
Inorganic Chemistry. 2020; 59(16): 11736-11748. https://doi.org/10.1021/acs.inorgchem.0c01664
DORA PSI -
Pietzsch H-J, Mamat C, Müller C, Schibli R
Single photon emission computed tomography tracer
In: Schober O, Kiessling F, Debus J, eds. Molecular imaging in oncology. Recent results in cancer research. Cham: Springer Nature; 2020:227-282. https://doi.org/10.1007/978-3-030-42618-7_7
DORA PSI -
van der Meulen NP, Hasler R, Talip Z, Grundler PV, Favaretto C, Umbricht CA, et al.
Developments toward the implementation of 44Sc production at a medical cyclotron
Molecules. 2020; 25(20): 4706 (16 pp.). https://doi.org/10.3390/molecules25204706
DORA PSI -
Boss SD, Müller C, Siwowska K, Schmid RM, Groehn V, Schibli R, et al.
Diastereomerically pure 6R- and 6S-3'-aza-2'-18F-fluoro-5-methyltetrahydrofolates show unprecedentedly high uptake in folate receptor-positive KB tumors
Journal of Nuclear Medicine. 2019; 60(1): 135-141. https://doi.org/10.2967/jnumed.118.213314
DORA PSI -
Cicone F, Gnesin S, Denoël T, Stora T, van der Meulen NP, Müller C, et al.
Internal radiation dosimetry of a 152Tb-labeled antibody in tumor-bearing mice
EJNMMI Research. 2019; 9: 53 (10 pp.). https://doi.org/10.1186/s13550-019-0524-7
DORA PSI -
Gracheva N, Müller C, Talip Z, Heinitz S, Köster U, Zeevaart JR, et al.
Production and characterization of no-carrier-added 161Tb as an alternative to the clinically-applied 177Lu for radionuclide therapy
EJNMMI Radiopharmacy and Chemistry. 2019; 4: 12 (16 pp.). https://doi.org/10.1186/s41181-019-0063-6
DORA PSI -
Kranzbühler B, Salemi S, Umbricht CA, Deberle LM, Müller C, Burger IA, et al.
Concentration‐dependent effects of dutasteride on prostate‐specific membrane antigen (PSMA) expression and uptake of 177Lu‐PSMA‐617 in LNCaP cells
Prostate. 2019; 79(12): 1477-1483. https://doi.org/10.1002/pros.23868
DORA PSI -
Müller C, De Prado Leal M, Dominietto MD, Umbricht CA, Safai S, Perrin RL, et al.
Combination of proton therapy and radionuclide therapy in mice: preclinical pilot sudy at the Paul Scherrer Institute
Pharmaceutics. 2019; 11(9): 450 (13 pp.). https://doi.org/10.3390/pharmaceutics11090450
DORA PSI -
Müller C, Singh A, Umbricht CA, Kulkarni HR, Johnston K, Benešová M, et al.
Preclinical investigations and first-in-human application of 152Tb-PSMA-617 for PET/CT imaging of prostate cancer
EJNMMI Research. 2019; 9(1): 68 (10 pp.). https://doi.org/10.1186/s13550-019-0538-1
DORA PSI -
Müller C, Umbricht CA, Gracheva N, Tschan VJ, Pellegrini G, Bernhardt P, et al.
Terbium-161 for PSMA-targeted radionuclide therapy of prostate cancer
European Journal of Nuclear Medicine and Molecular Imaging. 2019; 46(9): 1919-1930. https://doi.org/10.1007/s00259-019-04345-0
DORA PSI -
Radford LL, Fernandez S, Beacham R, Sayed RE, Farkas R, Benešová M, et al.
New 55Co-labeled albumin-binding folate derivatives as potential PET agents for folate receptor imaging
Pharmaceuticals. 2019; 12(4): 166 (12 pp.). https://doi.org/10.3390/ph12040166
DORA PSI -
Rupp NJ, Umbricht CA, Pizzuto DA, Lenggenhager D, Töpfer A, Müller J, et al.
First clinico-pathological evidence of a non PSMA-related uptake mechanism for 68Ga-PSMA-11 in salivary glands
Journal of Nuclear Medicine. 2019; 60(9): 1270-1276. https://doi.org/10.2967/jnumed.118.222307
DORA PSI -
Schniering J, Benešová M, Brunner M, Haller S, Cohrs S, Frauenfelder T, et al.
18F-AzaFol for detection of folate receptor-β positive macrophages in experimental interstitial lung disease - a proof-of-concept study
Frontiers in Immunology. 2019; 10: 2724 (15 pp.). https://doi.org/10.3389/fimmu.2019.02724
DORA PSI -
Siwowska K, Guzik P, Domnanich KA, Monné Rodríguez JM, Bernhardt P, Ponsard B, et al.
Therapeutic potential of 47Sc in comparison to 177Lu and 90Y: preclinical investigations
Pharmaceutics. 2019; 11(8): 424 (13 pp.). https://doi.org/10.3390/pharmaceutics11080424
DORA PSI -
Umbricht CA, Köster U, Bernhardt P, Gracheva N, Johnston K, Schibli R, et al.
Alpha-PET for prostate cancer: preclinical investigation using 149Tb-PSMA-617
Scientific Reports. 2019; 9: 17800 (10 pp.). https://doi.org/10.1038/s41598-019-54150-w
DORA PSI -
Zhang J, Singh A, Kulkarni HR, Schuchardt C, Müller D, Wester H-J, et al.
From bench to bedside—the Bad Berka experience with first-in-human studies
Seminars in Nuclear Medicine. 2019; 49(5): 422-437. https://doi.org/10.1053/j.semnuclmed.2019.06.002
DORA PSI -
van der Meulen NP, Hasler R, Blanc A, Farkas R, Benešová M, Talip Z, et al.
Implementation of a new separation method to produce qualitatively improved 64Cu
Journal of Labelled Compounds and Radiopharmaceuticals. 2019; 62(8): 460-470. https://doi.org/10.1002/jlcr.3730
DORA PSI -
Benešová M, Umbricht CA, Schibli R, Müller C
Albumin-binding PSMA ligands: optimization of the tissue distribution profile
Molecular Pharmaceutics. 2018; 15(3): 934-946. https://doi.org/10.1021/acs.molpharmaceut.7b00877
DORA PSI -
Boss SD, Müller C, Siwowska K, Büchel JI, Schmid RM, Groehn V, et al.
Reduced 18F-folate conjugates as a new class of PET tracers for folate receptor imaging
Bioconjugate Chemistry. 2018; 29(4): 1119-1130. https://doi.org/10.1021/acs.bioconjchem.7b00775
DORA PSI -
Kranzbühler B, Salemi S, Umbricht CA, Müller C, Burger IA, Sulser T, et al.
Pharmacological upregulation of prostate-specific membrane antigen (PSMA) expression in prostate cancer cells
Prostate. 2018; 78(10): 758-765. https://doi.org/10.1002/pros.23522
DORA PSI -
Lindenblatt D, Terraneo N, Pellegrini G, Cohrs S, Spycher PR, Vukovic D, et al.
Combination of lutetium-177 labelled anti-L1CAM antibody chCE7 with the clinically relevant protein kinase inhibitor MK1775: a novel combination against human ovarian carcinoma
BMC Cancer. 2018; 18: 922 (14 pp.). https://doi.org/10.1186/s12885-018-4836-1
DORA PSI -
Müller C, Guzik P, Siwowska K, Cohrs S, Schmid RM, Schibli R
Combining albumin-binding properties and interaction with pemetrexed to improve the tissue distribution of radiofolates
Molecules. 2018; 23(6): 1465 (12 pp.). https://doi.org/10.3390/molecules23061465
DORA PSI -
Müller C, Domnanich KA, Umbricht CA, van der Meulen NP
Scandium and terbium radionuclides for radiotheranostics: current state of development towards clinical application
British Journal of Radiology. 2018; 91(1091): 20180074 (13 pp.). https://doi.org/10.1259/bjr.20180074
DORA PSI -
Schniering J, Borgna F, Siwowska K, Benešová M, Cohrs S, Hasler R, et al.
In vivo labeling of plasma proteins for imaging of enhanced vascular permeability in the lungs
Molecular Pharmaceutics. 2018; 15(11): 4995-5004. https://doi.org/10.1021/acs.molpharmaceut.8b00606
DORA PSI -
Schniering J, Benešová M, Brunner M, Haller S, Cohrs S, Frauenfelder T, et al.
Visualisation of interstitial lung disease by molecular imaging of integrin αvβ3 and somatostatin receptor 2
Annals of the Rheumatic Diseases. 2018; 78(2): 218-227. https://doi.org/10.1136/annrheumdis-2018-214322
DORA PSI -
Umbricht CA, Benešová M, Hasler R, Schibli R, van der Meulen NP, Müller C
Design and preclinical evaluation of an albumin-binding PSMA ligand for 64Cu-based PET imaging
Molecular Pharmaceutics. 2018; 15(12): 5556-5564. https://doi.org/10.1021/acs.molpharmaceut.8b00712
DORA PSI -
Umbricht CA, Benešová M, Schibli R, Müller C
Preclinical development of novel PSMA-targeting radioligands: modulation of albumin-binding properties to improve prostate cancer therapy
Molecular Pharmaceutics. 2018; 15(6): 2297-2306. https://doi.org/10.1021/acs.molpharmaceut.8b00152
DORA PSI -
de Visser HM, Korthagen NM, Müller C, Ramakers RM, Krijger GC, Lafeber FPJG, et al.
Imaging of folate receptor expressing macrophages in the rat groove model of osteoarthritis: using a new DOTA-folate conjugate
Cartilage. 2018; 9(2): 183-191. https://doi.org/10.1177/1947603517738073
DORA PSI -
Baum RP, Singh A, Benešová M, Vermeulen C, Gnesin S, Köster U, et al.
Clinical evaluation of the radiolanthanide terbium-152: first-in-human PET/CT with 152Tb-DOTATOC
Dalton Transactions. 2017; 46(42): 14638-14646. https://doi.org/10.1039/c7dt01936j
DORA PSI -
Domnanich KA, Müller C, Benešová M, Dressler R, Haller S, Köster U, et al.
47Sc as useful β–-emitter for the radiotheragnostic paradigm: a comparative study of feasible production routes
EJNMMI Radiopharmacy and Chemistry. 2017; 2: 5 (17 pp.). https://doi.org/10.1186/s41181-017-0024-x
DORA PSI -
Domnanich KA, Eichler R, Müller C, Jordi S, Yakusheva V, Braccini S, et al.
Production and separation of 43Sc for radiopharmaceutical purposes
EJNMMI Radiopharmacy and Chemistry. 2017; 2: 14 (17 pp.). https://doi.org/10.1186/s41181-017-0033-9
DORA PSI -
Honarvar H, Müller C, Cohrs S, Haller S, Westerlund K, Eriksson Karlström A, et al.
Evaluation of the first 44Sc-labeled Affibody molecule for imaging of HER2-expressing tumors
Nuclear Medicine and Biology. 2017; 45: 15-21. https://doi.org/10.1016/j.nucmedbio.2016.10.004
DORA PSI -
Kopka K, Benešová M, Bařinka C, Haberkorn U, Babich J
Glu-ureido-based inhibitors of prostate-specific membrane antigen: lessons learned during the development of a novel class of low-molecular-weight theranostic radiotracers
Journal of Nuclear Medicine. 2017; 58(Suppl. 2): 17S-26S. https://doi.org/10.2967/jnumed.116.186775
DORA PSI -
Müller C, Farkas R, Borgna F, Schmid RM, Benešová M, Schibli R
Synthesis, radiolabeling, and characterization of plasma protein-binding ligands: potential tools for modulation of the pharmacokinetic properties of (radio)pharmaceuticals
Bioconjugate Chemistry. 2017; 28(9): 2372-2383. https://doi.org/10.1021/acs.bioconjchem.7b00378
DORA PSI -
Müller C, van der Meulen NP, Benešová M, Schibli R
Therapeutic radiometals beyond 177Lu and 90Y: production and application of promising α-particle, β–-particle, and Auger electron emitters
Journal of Nuclear Medicine. 2017; 58(Suppl. 2): 91S-96S. https://doi.org/10.2967/jnumed.116.186825
DORA PSI -
Pellegrini G, Siwowska K, Haller S, Antoine D, Schibli R, Kipar A, et al.
A short-term biological indicator for long-term kidney damage after radionuclide therapy in mice
Pharmaceuticals. 2017; 10(2): 57 (13 pp.). https://doi.org/10.3390/ph10020057
DORA PSI -
Singh A, van der Meulen NP, Müller C, Klette I, Kulkarni HR, Türler A, et al.
First-in-human PET/CT imaging of metastatic neuroendocrine neoplasms with cyclotron-produced 44Sc-DOTATOC: a proof-of-concept study
Cancer Biotherapy and Radiopharmaceuticals. 2017; 32(4): 124-132. https://doi.org/10.1089/cbr.2016.2173
DORA PSI -
Siwowska K, Schmid RM, Cohrs S, Schibli R, Müller C
Folate receptor-positive gynecological cancer cells: in vitro and in vivo characterization
Pharmaceuticals. 2017; 10(3): 72 (17 pp.). https://doi.org/10.3390/ph10030072
DORA PSI -
Siwowska K, Haller S, Bortoli F, Benešová M, Groehn V, Bernhardt P, et al.
Preclinical comparison of albumin-binding radiofolates: impact of linker entities on the in vitro and in vivo properties
Molecular Pharmaceutics. 2017; 14(2): 523-532. https://doi.org/10.1021/acs.molpharmaceut.6b01010
DORA PSI -
Umbricht CA, Benešová M, Schmid RM, Türler A, Schibli R, van der Meulen NP, et al.
44Sc-PSMA-617 for radiotheragnostics in tandem with 177Lu-PSMA-617—preclinical investigations in comparison with 68Ga-PSMA-11 and 68Ga-PSMA-617
EJNMMI Research. 2017; 7(1): 9 (10 pp.). https://doi.org/10.1186/s13550-017-0257-4
DORA PSI -
Walser M, Umbricht CA, Fröhli E, Nanni P, Hajnal A
β-integrin de-phosphorylation by the Density-Enhanced Phosphatase DEP-1 attenuates EGFR signaling in C. elegans
PLoS Genetics. 2017; 13(1): e1006592 (22 pp.). https://doi.org/10.1371/journal.pgen.1006592
DORA PSI -
Boss SD, Betzel T, Müller C, Fischer CR, Haller S, Reber J, et al.
Comparative studies of three pairs of α- and γ-conjugated folic acid derivatives labeled with fluorine-18
Bioconjugate Chemistry. 2016; 27(1): 74-86. https://doi.org/10.1021/acs.bioconjchem.5b00644
DORA PSI -
Bunka M, Müller C, Vermeulen C, Haller S, Türler A, Schibli R, et al.
Imaging quality of 44Sc in comparison with five other PET radionuclides using Derenzo phantoms and preclinical PET
Applied Radiation and Isotopes. 2016; 110: 129-133. https://doi.org/10.1016/j.apradiso.2016.01.006
DORA PSI -
Domnanich K, Müller C, Farkas R, Schmid RM, Ponsard B, Schibli R, et al.
44Sc for labeling of DOTA- and NODAGA-functionalized peptides: preclinical in vitro and in vivo investigations
EJNMMI Radiopharmacy and Chemistry. 2016; 1: 8 (19 pp.). https://doi.org/10.1186/s41181-016-0013-5
DORA PSI -
Farkas R, Siwowska K, Ametamey SM, Schibli R, van der Meulen NP, Müller C
64Cu- and 68Ga-based PET imaging of folate receptor-positive tumors: development and evaluation of an albumin-binding NODAGA−folate
Molecular Pharmaceutics. 2016; 13(6): 1979-1987. https://doi.org/10.1021/acs.molpharmaceut.6b00143
DORA PSI -
Haller S, Pellegrini G, Vermeulen C, van der Meulen NP, Köster U, Bernhardt P, et al.
Contribution of Auger/conversion electrons to renal side effects after radionuclide therapy: preclinical comparison of 161Tb-folate and 177Lu-folate
EJNMMI Research. 2016; 6(1): 13 (11 pp.). https://doi.org/10.1186/s13550-016-0171-1
DORA PSI -
Krall N, Pretto F, Mattarella M, Müller C, Neri D
A 99mTc-labeled ligand of carbonic anhydrase IX selectively targets renal cell carcinoma in vivo
Journal of Nuclear Medicine. 2016; 57(6): 943-949. https://doi.org/10.2967/jnumed.115.170514
DORA PSI -
Müller C, Vermeulen C, Köster U, Johnston K, Türler A, Schibli R, et al.
Alpha-PET with terbium-149: evidence and perspectives for radiotheragnostics
EJNMMI Radiopharmacy and Chemistry. 2016; 1(1): 5 (5 pp.). https://doi.org/10.1186/s41181-016-0008-2
DORA PSI -
Müller C, Vermeulen C, Johnston K, Köster U, Schmid R, Türler A, et al.
Preclinical in vivo application of 152Tb-DOTANOC: a radiolanthanide for PET imaging
EJNMMI Research. 2016; 6: 35 (10 pp.). https://doi.org/10.1186/s13550-016-0189-4
DORA PSI -
Baldoni D, Waibel R, Bläuenstein P, Galli F, Iodice V, Signore A, et al.
Evaluation of a novel Tc-99m labelled vitamin B12 derivative for targeting Escherichia coli and Staphylococcus aureus In Vitro and in an experimental foreign-body infection model
Molecular Imaging and Biology. 2015; 17(6): 829-837. https://doi.org/10.1007/s11307-015-0832-x
DORA PSI -
Haller S, Reber J, Brandt S, Bernhardt P, Groehn V, Schibli R, et al.
Folate receptor-targeted radionuclide therapy: preclinical investigation of anti-tumor effects and potential radionephropathy
Nuclear Medicine and Biology. 2015; 42(10): 770-779. https://doi.org/10.1016/j.nucmedbio.2015.06.006
DORA PSI -
Haller S, Ametamey SM, Schibli R, Müller C
Investigation of the chick embryo as a potential alternative to the mouse for evaluation of radiopharmaceuticals
Nuclear Medicine and Biology. 2015; 42(3): 226-233. https://doi.org/10.1016/j.nucmedbio.2014.10.010
DORA PSI -
Siebelt M, Korthagen N, Wei W, Groen H, Bastiaansen-Jenniskens Y, Müller C, et al.
Triamcinolone acetonide activates an anti-inflammatory and folate receptor-positive macrophage that prevents osteophytosis in vivo
Arthritis Research and Therapy. 2015; 17(1): 352 (13 pp.). https://doi.org/10.1186/s13075-015-0865-1
DORA PSI -
Siwowska K, Müller C
Preclinical development of small-molecular-weight folate-based radioconjugates: a pharmacological perspective
Quarterly Journal of Nuclear Medicine and Molecular Imaging. 2015; 59(3): 269-286.
DORA PSI -
van der Meulen NP, Bunka M, Domnanich K, Müller C, Haller S, Vermeulen C, et al.
Cyclotron production of 44Sc: from bench to bedside
Nuclear Medicine and Biology. 2015; 42(9): 745-751. https://doi.org/10.1016/j.nucmedbio.2015.05.005
DORA PSI -
Müller C, Reber J, Haller S, Dorrer H, Bernhardt P, Zhernosekov K, et al.
Direct in vitro and in vivo comparison of 161Tb and 177Lu using a tumour-targeting folate conjugate
European Journal of Nuclear Medicine and Molecular Imaging. 2014; 41(3): 476-485. https://doi.org/10.1007/s00259-013-2563-z
DORA PSI -
Müller C, Reber J, Haller S, Dorrer H, Köster U, Johnston K, et al.
Folate receptor targeted alpha-therapy using terbium-149
Pharmaceuticals. 2014; 7(3): 353-365. https://doi.org/10.3390/ph7030353
DORA PSI -
Müller C, Fischer E, Behe M, Köster U, Dorrer H, Reber J, et al.
Future prospects for SPECT imaging using the radiolanthanide terbium-155 — production and preclinical evaluation in tumor-bearing mice
Nuclear Medicine and Biology. 2014; 41(S): e58-e65. https://doi.org/10.1016/j.nucmedbio.2013.11.002
DORA PSI -
Müller A, Beck K, Rancic Z, Müller C, Fischer CR, Betzel T, et al.
Imaging aherosclerotic plaque inflammation via folate receptor targeting using a novel 18F-folate radiotracer
Molecular Imaging and Biology. 2014; 13(2): (11 pp.). https://doi.org/10.2310/7290.2013.00074
DORA PSI -
Müller C, Bunka M, Haller S, Köster U, Groehn V, Bernhardt P, et al.
Promising prospects for 44Sc-/47Sc-based theragnostics: application of 47Sc for radionuclide tumor therapy in mice
Journal of Nuclear Medicine. 2014; 55(10): 1658-1664. https://doi.org/10.2967/jnumed.114.141614
DORA PSI -
Ocak M, Gillman AG, Bresee J, Zhang L, Vlad AM, Müller C, et al.
Folate receptor-targeted multimodality imaging of ovarian cancer in a novel syngeneic mouse model
Molecular Pharmaceutics. 2014; 12(2): 542-553. https://doi.org/10.1021/mp500628g
DORA PSI -
Sah BR, Schibli R, Waibel R, Von Boehmer L, Bläuenstein P, Nexo E, et al.
Tumor imaging in patients with advanced tumors using a new 99mTc-radiolabeled vitamin B12 derivative
Journal of Nuclear Medicine. 2014; 55(1): 43-49. https://doi.org/10.2967/jnumed.113.122499
DORA PSI -
Siebelt M, van der Windt AE, Groen HC, Sandker M, Waarsing JH, Müller C, et al.
FK506 protects against articular cartilage collagenous extra-cellular matrix degradation
Osteoarthritis and Cartilage. 2014; 22(4): 591-600. https://doi.org/10.1016/j.joca.2014.02.003
DORA PSI -
Siebelt M, Groen HC, Koelewijn SJ, de Blois E, Sandker M, Waarsing JH, et al.
Increased physical activity severely induces osteoarthritic changes in knee joints with papain induced sulfate-glycosaminoglycan depleted cartilage
Arthritis Research and Therapy. 2014; 16(1): R32 (12 pp.). https://doi.org/10.1186/ar4461
DORA PSI -
Siebelt M, Waarsing JH, Groen HC, Müller C, Koelewijn SJ, de Blois E, et al.
Inhibited osteoclastic bone resorption through alendronate treatment in rats reduces severe osteoarthritis progression
Bone. 2014; 66: 163-170. https://doi.org/10.1016/j.bone.2014.06.009
DORA PSI -
Weiss A, Berndsen RH, Dubois M, Müller C, Schibli R, Griffioen AW, et al.
In vivo anti-tumor activity of the organometallic ruthenium(ii)-arene complex [Ru(η6-p-cymene)Cl2(pta)] (RAPTA-C) in human ovarian and colorectal carcinomas
Chemical Science. 2014; 5(12): 4742-4748. https://doi.org/10.1039/c4sc01255k
DORA PSI -
Betzel T, Müller C, Groehn V, Müller A, Reber J, Fischer CR, et al.
Radiosynthesis and preclinical evaluation of 3′-aza-2′-[18F]fluorofolic acid: a novel PET radiotracer for folate receptor targeting
Bioconjugate Chemistry. 2013; 24(2): 205-214. https://doi.org/10.1021/bc300483a
DORA PSI -
Fischer CR, Groehn V, Reber J, Schibli R, Ametamey SM, Müller C
Improved PET imaging of tumors in mice using a novel 18F-folate conjugate with an albumin-binding entity
Molecular Imaging and Biology. 2013; 15(6): 649-654. https://doi.org/10.1007/s11307-013-0651-x
DORA PSI -
Grünberg J, Jeger S, Sarko D, Dennler P, Zimmermann K, Mier W, et al.
DOTA-functionalized polylysine: a high number of DOTA chelates positively influences the biodistribution of enzymatic conjugated anti-tumor antibody chCE7agl
PLoS One. 2013; 8(4): e60350 (10 pp.). https://doi.org/10.1371/journal.pone.0060350
DORA PSI -
Müller C, Struthers H, Winiger C, Zhernosekov K, Schibli R
DOTA conjugate with an albumin-binding entity enables the first folic acid-targeted 177Lu-radionuclide tumor therapy in mice
Journal of Nuclear Medicine. 2013; 54(1): 124-131. https://doi.org/10.2967/jnumed.112.107235
DORA PSI -
Müller C
Folate-based radiotracers for PET imaging - update and perspectives
Molecules. 2013; 18(5): 5005-5031. https://doi.org/10.3390/molecules18055005
DORA PSI -
Müller C, Reber J, Schlup C, Leamon CP, Schibli R
In vitro and in vivo evaluation of an innocuous drug cocktail to improve the quality of folic acid targeted nuclear imaging in preclinical research
Molecular Pharmaceutics. 2013; 10(3): 967-974. https://doi.org/10.1021/mp300428p
DORA PSI -
Müller C, Bunka M, Reber J, Fischer C, Zhernosekov K, Türler A, et al.
Promises of cyclotron-produced 44Sc as a diagnostic match for trivalent β--emitters: in vitro and in vivo study of a 44Sc-DOTA-folate conjugate
Journal of Nuclear Medicine. 2013; 54(12): 2168-2174. https://doi.org/10.2967/jnumed.113.123810
DORA PSI -
Müller C, Schibli R
Prospects in folate receptor-targeted radionuclide therapy
Frontiers in Oncology. 2013; 3: 249 (10 pp.). https://doi.org/10.3389/fonc.2013.00249
DORA PSI -
Reber J, Haller S, Leamon CP, Müller C
177Lu-EC0800 combined with the antifolate pemetrexed: preclinical pilot study of folate receptor targeted radionuclide tumor therapy
Molecular Cancer Therapeutics. 2013; 12(11): 2436-2445. https://doi.org/10.1158/1535-7163.MCT-13-0422-T
DORA PSI -
Siebelt M, Jahr H, Groen HC, Sandker M, Waarsing JH, Kops N, et al.
Hsp90 inhibition protects against biomechanically induced osteoarthritis in rats
Arthritis and Rheumatism. 2013; 65(8): 2102-2112. https://doi.org/10.1002/art.38000
DORA PSI -
Weber CJ, Müller S, Safley SA, Gordon KB, Amancha P, Villinger F, et al.
Expression of functional folate receptors by human parathyroid cells
Surgery. 2013; 154(6): 1385-1393. https://doi.org/10.1016/j.surg.2013.06.045
DORA PSI -
Winkel LCJ, Groen HC, van Thiel BS, Müller C, van der Steen AFW, Wentzel JJ, et al.
Folate receptor-targeted single-photon emission computed tomography/computed tomography to detect activated macrophages in atherosclerosis: can it distinguish vulnerable from stable atherosclerotic plaques?
Molecular Imaging. 2013; 13(1): 1-5. https://doi.org/10.2310/7290.2013.00061
DORA PSI -
Däpp S, Müller C, Garayoa EG, Bläuenstein P, Maes V, Brans L, et al.
PEGylation, increasing specific activity and multiple dosing as strategies to improve the risk-benefit profile of targeted radionuclide therapy with 177Lu-DOTA-bombesin analogues
EJNMMI Research. 2012; 2(1): 24 (12 pp.). https://doi.org/10.1186/2191-219X-2-24
DORA PSI -
Fischer E, Grünberg J, Cohrs S, Hohn A, Waldner-Knogler K, Jeger S, et al.
L1-CAM-targeted antibody therapy and 177Lu-radioimmunotherapy of disseminated ovarian cancer
International Journal of Cancer. 2012; 130(11): 2715-2721. https://doi.org/10.1002/ijc.26321
DORA PSI -
Fischer CR, Müller C, Reber J, Müller A, Krämer SD, Ametamey SM, et al.
[18F]fluoro-deoxy-glucose folate: a novel PET radiotracer with improved in vivo properties for folate receptor targeting
Bioconjugate Chemistry. 2012; 23(4): 805-813. https://doi.org/10.1021/bc200660z
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Furger E, Fedosov SN, Launholt Lildballe D, Waibel R, Schibli R, Nexo E, et al.
Comparison of recombinant human haptocorrin expressed in human embryonic kidney cells and native haptocorrin
PLoS One. 2012; 7(5): e37421 (9 pp.). https://doi.org/10.1371/journal.pone.0037421
DORA PSI -
Krämer SD, Mu L, Müller A, Keller C, Kuznetsova OF, Schweinsberg C, et al.
5-(2-18F-fluoroethoxy)-L-tryptophan as a substrate of system L transport for tumor imaging by PET
Journal of Nuclear Medicine. 2012; 53(3): 434-442. https://doi.org/10.2967/jnumed.111.096289
DORA PSI -
Müller C, Zhernosekov K, Köster U, Johnston K, Dorrer H, Hohn A, et al.
A unique matched quadruplet of terbium radioisotopes for PET and SPECT and for α- and β−-radionuclide therapy: an in vivo proof-of-concept study with a new receptor-targeted folate derivative
Journal of Nuclear Medicine. 2012; 53(12): 1951-1959. https://doi.org/10.2967/jnumed.112.107540
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Müller C
Folate based radiopharmaceuticals for imaging and therapy of cancer and inflammation
Current Pharmaceutical Design. 2012; 18(8): 1058-1083. https://doi.org/10.2174/138161212799315777
DORA PSI -
Reber J, Struthers H, Betzel T, Hohn A, Schibli R, Müller C
Radioiodinated folic acid conjugates: evaluation of a valuable concept to improve tumor-to-background contrast
Molecular Pharmaceutics. 2012; 9(5): 1213-1221. https://doi.org/10.1021/mp200511t
DORA PSI -
Dias CR, Jeger S, Osso JAJ, Müller C, De Pasquale C, Hohn A, et al.
Radiolabeling of rituximab with 188Re and 99mTc using the tricarbonyl technology
Nuclear Medicine and Biology. 2011; 38(1): 19-28. https://doi.org/10.1016/j.nucmedbio.2010.05.010
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Däpp S, Garayoa EG, Maes V, Brans L, Tourwé DA, Müller C, et al.
PEGylation of 99mTc-labeled bombesin analogues improves their pharmacokinetic properties
Nuclear Medicine and Biology. 2011; 38(7): 997-1009. https://doi.org/10.1016/j.nucmedbio.2011.02.014
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Groehn V, Moser R, Ross TL, Betzel T, Müller C, Schibli R, et al.
Synthesis of precursors for 18F-labeling of folic acid for PET application
Synthesis. 2011; 2011(22): 3639-3648. https://doi.org/10.1055/s-0030-1260247
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Müller C, Schibli R
Folic acid conjugates for nuclear imaging of folate receptor-positive cancer
Journal of Nuclear Medicine. 2011; 52(1): 1-4. https://doi.org/10.2967/jnumed.110.076018
DORA PSI -
Müller C, Vlahov IR, Santhapuram HKR, Leamon CP, Schibli R
Tumor targeting using 67Ga-DOTA-Bz-folate — investigations of methods to improve the tissue distribution of radiofolates
Nuclear Medicine and Biology. 2011; 38(5): 715-723. https://doi.org/10.1016/j.nucmedbio.2010.12.013
DORA PSI -
Piscaer TM, Müller C, Mindt TL, Lubberts E, Verhaar JAN, Krenning EP, et al.
Imaging of activated macrophages in experimental osteoarthritis using folate-targeted animal single-photon-emission computed tomography/computed tomography
Arthritis and Rheumatism. 2011; 63(7): 1898-1907. https://doi.org/10.1002/art.30363
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Müller C, Reddy JA, Leamon CP, Schibli R
Effects of the antifolates pemetrexed and CB3717 on the tissue distribution of 99mTc-EC20 in xenografted and syngeneic tumor-bearing mice
Molecular Pharmaceutics. 2010; 7(2): 597-604. https://doi.org/10.1021/mp900296k
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Ross TL, Honer M, Müller C, Groehn V, Schibli R, Ametamey SM
A new 18F-labeled folic acid derivative with improved properties for the PET imaging of folate receptor-positive tumors
Journal of Nuclear Medicine. 2010; 51(11): 1756-1762. https://doi.org/10.2967/jnumed.110.079756
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Zahnd C, Kawe M, Stumpp MT, De Pasquale C, Tamaskovic R, Nagy-Davidescu G, et al.
Efficient tumor targeting with high-affinity designed ankyrin repeat proteins: effects of affinity and molecular size
Cancer Research. 2010; 70(4): 1595-1605. https://doi.org/10.1158/0008-5472.CAN-09-2724
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Harris DA, Pellikka R, Gasser O, Blaeuenstein P, Waibel R, Schubiger PA, et al.
In-line radiolabeling: a novel continuous-flow system for commercial-scale protein labeling
Journal of Nuclear Medicine. 2009; 50(7): 1178-1186. https://doi.org/10.2967/jnumed.108.056812
DORA PSI -
Mindt TL, Müller C, Stuker F, Salazar J-F, Hohn A, Mueggler T, et al.
A “click chemistry” approach to the efficient synthesis of multiple imaging probes derived from a single precursor
Bioconjugate Chemistry. 2009; 20(10): 1940-1949. https://doi.org/10.1021/bc900276b
DORA PSI -
Müller C, Mindt TL, de Jong M, Schibli R
Evaluation of a novel radiofolate in tumour-bearing mice: promising prospects for folate-based radionuclide therapy
European Journal of Nuclear Medicine and Molecular Imaging. 2009; 36(6): 938-946. https://doi.org/10.1007/s00259-008-1058-9
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Sparr C, Michel U, Marti RE, Müller C, Schibli R, Moser R, et al.
Synthesis of a novel γ-folic acid-Nτ-histidine conjugate suitable for labeling with 99mTc and 188Re
Synthesis. 2009;(05): 787-792. https://doi.org/10.1055/s-0028-1083345
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Struthers H, Hagenbach A, Abram U, Schibli R
Organometallic [Re(CO)3]+ and [Re(CO)2(NO)]2+ labeled substrates for human thvmidine kinase 1
Inorganic Chemistry. 2009; 48(12): 5154-5163. https://doi.org/10.1021/ic9000126
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Desbouis D, Struthers H, Spiwok V, Küster T, Schibli R
Synthesis, in vitro, and in silico evaluation of organometallic technetium and rhenium thymidine complexes with retained substrate activity toward human thymidine kinase type 1
Journal of Medicinal Chemistry. 2008; 51(21): 6689-6698. https://doi.org/10.1021/jm800530p
DORA PSI -
Hohn A, Zimmermann K, Schaub E, Hirzel W, Schubiger PA, Schibli R
Production and separation of "non-standard" PET nuclides at a large cyclotron facility: the experiences at the Paul Scherrer Institute in Switzerland
Quarterly Journal of Nuclear Medicine and Molecular Imaging. 2008; 52(2): 145-150.
DORA PSI -
Mindt TL, Müller C, Melis M, de Jong M, Schibli R
"Click-to-chelate": in vitro and in vivo comparison of a 99mTc(CO)3-labeled N(τ)-histidine folate derivative with its isostructural, clicked 1,2,3-triazole analogue
Bioconjugate Chemistry. 2008; 19(8): 1689-1695. https://doi.org/10.1021/bc800183r
DORA PSI -
Struthers H, Spingler B, Mindt TL, Schibli R
"Click-to-chelate": design and incorporation of triazole-containing metal-chelating systems into biomolecules of diagnostic and therapeutic interest
Chemistry: A European Journal. 2008; 14(20): 6173-6183. https://doi.org/10.1002/chem.200702024
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Waibel R, Treichler H, Schaefer NG, van Staveren DR, Mundwiler S, Kunze S, et al.
New derivatives of vitamin B12 show preferential targeting of tumors
Cancer Research. 2008; 68(8): 2904-2911. https://doi.org/10.1158/0008-5472.CAN-07-6771
DORA PSI -
Desbouis D, Schubiger PA, Schibli R
Synthesis of tricarbonyl rhenium and technetium complexes of a 5′-carboxamide 5-ethyl-2′-deoxyuridine for selective inhibition of herpes simplex virus thymidine kinase 1
Journal of Organometallic Chemistry. 2007; 692(6): 1340-1347. https://doi.org/10.1016/j.jorganchem.2006.10.011
DORA PSI -
Mindt T, Struthers H, Garcia-Garayoa E, Desbouis D, Schibli R
Strategies for the development of novel tumor targeting technetium and rhenium radiopharmaceuticals
Chimia. 2007; 61(11): 725-731. https://doi.org/10.2533/chimia.2007.725
DORA PSI -
Müller C, Schubiger PA, Schibli R
Isostructural folate conjugates radiolabeled with the matched pair 99mTc/188Re: a potential strategy for diagnosis and therapy of folate receptor-positive tumors
Nuclear Medicine and Biology. 2007; 34(6): 595-601. https://doi.org/10.1016/j.nucmedbio.2007.05.011
DORA PSI -
Stichelberger M, Desbouis D, Spiwok V, Scapozza L, Schubiger PA, Schibli R
Synthesis, in vitro and in silico assessment of organometallic rhenium(I) and technetium(I) thymidine complexes
Journal of Organometallic Chemistry. 2007; 692(6): 1255-1264. https://doi.org/10.1016/j.jorganchem.2006.08.101
DORA PSI -
Zehnder-Fjällman AHM, Marty C, Halin C, Hohn A, Schibli R, Ballmer-Hofer K, et al.
Evaluation of anti-VEGFR-3 specific scFv antibodies as potential therapeutic and diagnostic tools for tumor lymph-angiogenesis
Oncology Reports. 2007; 18(4): 933-941. https://doi.org/10.3892/or.18.4.933
DORA PSI -
Bettio A, Honer M, Müller C, Brühlmeier M, Müller U, Schibli R, et al.
Synthesis and preclinical evaluation of a folic acid derivative labeled with 18F for PET imaging of folate receptor-positive tumors
Journal of Nuclear Medicine. 2006; 47(7): 1153-1160. http://jnm.snmjournals.org/content/47/7/1153.long.
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García-Garayoa E, Maes V, Bläuenstein P, Blanc A, Hohn A, Tourwé D, et al.
Double-stabilized neurotensin analogues as potential radiopharmaceuticals for NTR-positive tumors
Nuclear Medicine and Biology. 2006; 33(4): 495-503. https://doi.org/10.1016/j.nucmedbio.2006.01.007
DORA PSI -
Mindt TL, Struthers H, Brans L, Anguelov T, Schweinsberg C, Maes V, et al.
"Click to chelate": synthesis and installation of metal chelates into biomolecules in a single step
Journal of the American Chemical Society. 2006; 128(47): 15096-15097. https://doi.org/10.1021/ja066779f
DORA PSI -
Müller C, Brühlmeier M, Schubiger PA, Schibli R
Effects of antifolate drugs on the cellular uptake of radiofolates in vitro and in vivo
Journal of Nuclear Medicine. 2006; 47(12): 2057-2064. http://jnm.snmjournals.org/content/47/12/2057.long.
DORA PSI -
Müller C, Schubiger PA, Schibli R
In vitro and in vivo targeting of different folate receptor-positive cancer cell lines with a novel 99mTc-radiofolate tracer
European Journal of Nuclear Medicine and Molecular Imaging. 2006; 33(10): 1162-1170. https://doi.org/10.1007/s00259-006-0118-2
DORA PSI -
Müller C, Hohn A, Schubiger PA, Schibli R
Preclinical evaluation of novel organometallic 99mTc-folate and 99mTc-pteroate radiotracers for folate receptor-positive tumour targeting
European Journal of Nuclear Medicine and Molecular Imaging. 2006; 33(9): 1007-1016. https://doi.org/10.1007/s00259-006-0111-9
DORA PSI -
Müller C, Schubiger PA, Schibli R
Synthesis and in vitro/in vivo evaluation of novel 99mTc(CO)3-folates
Bioconjugate Chemistry. 2006; 17(3): 797-806. https://doi.org/10.1021/bc050323q
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