A5018308209- Radiopharmaceutical Chemistry and Applications
- Medical Imaging Techniques and Applications
- Sarcoma Diagnosis and Treatment
- Peptidase Inhibition and Analysis
- Medical Imaging and Pathology Studies
- Bone Tumor Diagnosis and Treatments
- Orthopedic Infections and Treatments
- Proteoglycans and glycosaminoglycans research
- Chemical Synthesis and Analysis
- Melanoma and MAPK Pathways
- interferon and immune responses
- Osteoarthritis Treatment and Mechanisms
- Total Knee Arthroplasty Outcomes
- Click Chemistry and Applications
- Cell Adhesion Molecules Research
- Knee injuries and reconstruction techniques
- Lung Cancer Treatments and Mutations
- Radiomics and Machine Learning in Medical Imaging
- Inflammatory mediators and NSAID effects
- Nanoplatforms for cancer theranostics
- Immunotherapy and Immune Responses
- Monoclonal and Polyclonal Antibodies Research
- Musculoskeletal synovial abnormalities and treatments
- Cancer Immunotherapy and Biomarkers
- Computational Drug Discovery Methods
Inserm
2014-2024
Clermont Université
2008-2024
Imagerie Moléculaire et Stratégies Théranostiques
2017-2024
Université Clermont Auvergne
2012-2023
Centre Jean Perrin
2005-2018
Cyclopharma (France)
2010
Tumor hypoxia is a characteristic of cancer cell growth and invasion, promoting angiogenesis, which facilitates metastasis. Oxygen delivery remains impaired because tumor vessels are anarchic leaky, contributing to dissemination. Counteracting by normalizing in order improve drug radio therapy efficacy avoid stem-like selection highly challenging issue. We show here that inositol trispyrophosphate (ITPP) treatment stably increases oxygen tension blood flow melanoma breast syngeneic models....
Our project deals with a multimodal approach using single fluorinated and iodinated melanin-targeting structure offering both imaging (positron emission tomography (PET)/fluorine-18) treatment (targeted radionuclide therapy/iodine-131) of melanoma. Six 6-iodoquinoxaline-2-carboxamide derivatives various side chains bearing fluorine were synthesized radiofluorinated, their in vivo biodistribution was studied by PET B16Bl6 primary melanoma-bearing mice. Among this series, [(18)F]8 emerged as...
The GATE Monte Carlo simulation platform based on the Geant4 toolkit is under constant improvement for dosimetric calculations. In this study, we explore its use dosimetry of preclinical targeted radiotherapy melanoma using a new specific melanin-targeting radiotracer labeled with iodine 131. Calculated absorbed fractions and S values spheres murine models (digital CT-scan-based mouse phantoms) are compared between EGSnrc codes considering monoenergetic electrons detailed energy spectrum...
This study reports a series of 14 new iodinated and fluorinated compounds offering both early imaging (123I, 124I, 18F) systemic treatment (131I) melanoma potentialities. The biodistribution each 125I-labeled tracer was evaluated in model B16F0-bearing mice, using vivo serial γ scintigraphic imaging. Among this series, [125I]56 emerged as the most promising compound terms specific tumoral uptake kinetic profile. To validate our multimodality concept, radiosynthesis [18F]56 then optimized...
PURPOSE: This work reports, in melanoma models, the theranostic potential of ICF15002 as a single fluorinated and iodinated melanin-targeting compound. METHODS: Studies were conducted murine syngeneic B16BL6 model A375 SK-MEL-3 human xenografts. was radiolabeled with fluorine-18 for positron emission tomography (PET) imaging biodistribution, iodine-125 metabolism study, iodine-131 targeted radionuclide therapy (TRT). TRT efficacy assessed by tumor volume measurement, mechanistics dosimetry...
Phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates (PAIB-SOs) are a new family of antimitotic prodrugs bioactivated in breast cancer cells expressing CYP1A1. In this study, we report that the 14C-labeled prototypical PAIB-SO [14C]CEU-818 and its counterpart [14C]CEU-602 distributed whole mouse body they show short half-life mice. To circumvent limitation, evaluated effect homologation alkyl side chain imidazolidin-2-one moiety PAIB-SOs. Our studies evidence PAIB-SOs bearing an...
Radioiodobenzamides are the best-known agents under study for diagnosis of cutaneous melanoma and its metastases. We report synthesis a new BAT derivative radiopharmaceutical in which radioiodine is replaced by 99m-technetium. The cyclic intermediary methyl 4-[3-(4,4,7,7-tetramethyl-5,6-dithia-2,9-diazacyclodecyl)-2-oxapropyl]benzoate (5) occurred two different conformations identified spectroscopic analysis. final ligand was radiolabeled using nitridotechnetium core ligand-exchange...
[123I]-N-(2-Diethylaminoethyl)-4-iodobenzamide (123I-BZA) has been the best scintigraphic agent described so far for malignant melanoma and ocular diagnosis. We replaced 123I by more convenient radioisotope 99mTc synthesized four bis(aminoethanethiol) derivatives. describe synthesis of a new oxo-technetium complex (TcO-Cf), prepared in very high yield (radiochemical > 95%), that exhibits an affinity pigmented tumor cells. This was evaluated vivo mice bearing C57B16 murine melanoma. After...
Benzamide-based radioligands targeting melanin were first developed for imaging melanoma and then therapeutic purpose with targeted radionuclide therapy (TRT). [131I]ICF01012 presents a highly favorable pharmacokinetics profile in vivo therapy. Tumour growth reduction increase survival have been established preclinical models of melanoma. According the these results, we initiate first-in-human study aimed to determine recommended dose administer treatment patients pigmented metastatic...
The proteasome is a multicatalytic protease that plays critical role in the cell. control of proteasomes could, thus, provide weapon for treatment cancer. Therefore, we have synthesized six new peptide aldehyde inhibitors linked to N-(2-diethylaminoethyl)benzamide (BZA-CO) structure, order target cytotoxic activity malignant melanoma cells. Biological studies demonstrated influence length and composition amino acid chain on cytotoxicity our compounds. Among them, compound 19 presents highest...
This study aimed to report the first single-photon emission computed tomographic (SPECT) imaging of articular cartilage in mice using 99m Tc-NTP 15-5 radiotracer. Mice intravenously injected with were submitted (1) dynamic planar imaging, (2) static (3) 1 mm pinhole SPECT acquisition, and (4) dissection. Tomographic reconstruction data was performed a three-dimensional ordered subset expectation maximization algorithm, slices reconstructed three axes. rapidly accumulated joint, peak...
This study determined, using the intraarticular complete Freund adjuvant arthritis mice model, whether radiotracer <sup>99m</sup>Tc-<i>N</i>-(triethylammonium)-3-propyl-[15]ane-N5 (<sup>99m</sup>Tc-NTP 15-5) targeting proteoglycans has a pathophysiologic validity for in vivo imaging of rheumatoid (RA) and its response to chronic nonsteroidal antiinflammatory drugs. <b>Methods:</b> We investigated time course cartilage remodeling by <sup>99m</sup>Tc-NTP 15-5 scintigraphy, bone damages...
To date, surgery remains the only option for treatment of chondrosarcoma, which is radio- and chemoresistant due in part to its large extracellular matrix (ECM) poor vascularity. In case unresectable locally advanced or metastatic diseases with a prognosis, improving management chondrosarcoma still challenge. Our team developed an attractive approach improvement therapeutic index chemotherapy by targeting proteoglycan (PG)-rich tissues using quaternary ammonium (QA) function conjugated...