A5053358840- Medical Imaging Techniques and Applications
- Radiopharmaceutical Chemistry and Applications
- interferon and immune responses
- Monoclonal and Polyclonal Antibodies Research
- Peptidase Inhibition and Analysis
- Nanoplatforms for cancer theranostics
- Proteoglycans and glycosaminoglycans research
- Receptor Mechanisms and Signaling
- HER2/EGFR in Cancer Research
- Phosphodiesterase function and regulation
- Glioma Diagnosis and Treatment
- Cell Adhesion Molecules Research
- Glycosylation and Glycoproteins Research
- Pharmacological Receptor Mechanisms and Effects
- Bone Tumor Diagnosis and Treatments
- Fluorine in Organic Chemistry
- Sarcoma Diagnosis and Treatment
- Cancer therapeutics and mechanisms
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Catalytic Reactions
- Click Chemistry and Applications
- Prostate Cancer Treatment and Research
- MicroRNA in disease regulation
Imagerie Moléculaire et Stratégies Théranostiques
2006-2024
Université Clermont Auvergne
2015-2024
Inserm
2015-2024
Centre Jean Perrin
2008-2015
Molécules d'Intérêt Biologique
2006-2013
Helmholtz-Zentrum Dresden-Rossendorf
2011-2012
Cyclopharma (France)
2010
Centre National de la Recherche Scientifique
2010
Abstract Triazoles from “click chemistry” are convenient ligands for the formation of platinum complexes bearing combined triazole–amine or triazole–carboxylate moieties. Striking differences in chelation modes observed between two series. One exhibits selective cytotoxicity against breast cancer cells lines. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
Tetraspanin 8 (TSPAN8) overexpression is correlated with poor prognosis in human colorectal cancer (CRC). A murine mAb Ts29.2 specific for TSPAN8 provided significant efficiency immunotherapy CRC pre-clinical models. We therefore evaluate the feasability of targeting radiolabeled Ts29.2. Staining tissue micro-arrays revealed that espression was restricted to a few healthy tissues. DOTA-Ts29.2 111In or 177Lu radiochemical purities >95%, activity ranging from 300 600 MBq/mg, and...
Over the last decade, upconversion nanoparticles (UCNP) have been widely investigated in nanomedicine due to their high potential as imaging agents near-infrared (NIR) optical window of biological tissues. Here, we successfully develop active targeted UCNP probes for dual NIR-NIR fluorescence and radioactive-guided surgery prostate-specific membrane antigen (PSMA)(+) prostate cancers. We designed a one-pot thermolysis synthesis method obtain oleic acid-coated spherical NaYF4:Yb,Tm@NaYF4...
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...
Abstract Glioma are clinically challenging tumors due to their location and invasiveness nature, which often hinder complete surgical resection. The evaluation of the isocitrate dehydrogenase mutation status has become crucial for effective patient stratification. Through a transdisciplinary approach, we have developed an 18 F-labeled ligand non-invasive assessment IDH1R132H variant by using positron emission tomography (PET) imaging. In this study, successfully prepared diastereomerically...
Abstract Triazole chelators, synthesized by click chemistry, are convenient ligands for palladium(II) and platinum(II). Conformational changes induced the complexation of these Pd II Pt complexes with guanosine similar to those cisplatin. In addition, behave like cisplatin regard relaxation supercoiled plasmid DNA.
Abstract In this study, we synthesized and evaluated a new spirocyclic piperidine derivative 3 , containing 4‐fluorobutyl side chain, as PET radioligand for neuroimaging of σ 1 receptors. vitro, compound displayed high affinity receptors ( K i =1.2 n M ) well selectivity. [ 18 F] radiosynthesis was performed from the corresponding tosylate precursor, with radiochemical yield (45–51 %), purity (>98 specific activity (>201 GBq μmol −1 ). Metabolic stability in brain CD‐1 mice verified,...
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...
As evidenced by the number of publications and patents published in last years, radiosynthesis 6‐[ 18 F]fluoro‐3,4‐dihydroxy‐ L ‐phenylalanine ([ F]FDOPA) using nucleophilic [ F]F‐ process remains currently a challenge for radiochemists scientific community even if promising methods radiofluorination electron‐rich aromatic structures were recently developed from arylboronate, arylstannane or iodonium salt precursors. In such context, based on use an triflate precursor, we optimized fast...
Phosphodiesterases (PDEs) are enzymes that play a major role in cell signalling by hydrolysing the secondary messengers cyclic adenosine monophosphate (cAMP) and/or guanosine (cGMP) throughout body and brain. Altered nucleotide-mediated has been associated with wide array of disorders, including neurodegenerative disorders. Recently, PDE5 shown to be involved disorders such as Alzheimer's disease, but its precise not elucidated yet. To visualize quantify expression this enzyme brain, we...
Phosphodiesterase 10A (PDE10A) is a key enzyme of intracellular signal transduction which involved in the regulation neurotransmission. The molecular imaging PDE10A by PET expected to allow better understanding physiological and pathological processes related expression function brain. aim this study was develop new 18F-labeled ligand based on 6,7-dimethoxy-4-pyrrolidinylquinazoline evaluate its properties biodistribution studies. Nucleophilic substitution 7-tosyloxy-analogue led...
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...
Abstract Background ( S )-[ 18 F]FETrp is a promising PET radiotracer for imaging IDO1 activity, one of the main enzymes involved in tryptophan metabolism that plays key role several diseases including cancers. To date, radiosynthesis this analogue remains highly challenging due to partial racemization occurring during nucleophilic radiofluorination step. This work aims develop short, epimerization-free and efficient automated procedure from corresponding enantiopure tosylate precursor....
3-[ 18 F]Fluoropropanesulfonyl chloride, a recently proposed prosthetic agent for fluorine-18 labelling, was prepared in two-step radiosynthesis via F]fluoropropyl thiocyanate as an intermediate. Two benzenesulfonate-based radiolabelling precursors were by various routes. Comparing the reactivities of 3-thiocyanatopropyl nosylate and corresponding tosylate towards [ F]fluoride former proved to be superior accounting labelling yields up 85%. Conditions reliable transformation sulfonyl...