PERIGAUD Christian
Fonction : user SAP
Thème de Recherche: Nucléosides & Effecteurs Phosphorylés (responsable de)
christian.perigaud
umontpellier.fr
0448792054
Bureau: N1H13, Etg: 1 - Site : Pôle Chimie Balard Recherche
Domaines de Recherche: - Sciences du Vivant/Cancer
- Chimie/Chimie analytique
- Chimie/Chimie thérapeutique
- Sciences du Vivant/Biochimie, Biologie Moléculaire/Biochimie
- Chimie/Chimie organique
- Sciences du Vivant/Biologie cellulaire
- Sciences du Vivant/Bio-Informatique, Biologie Systémique
- Informatique/Bio-informatique
- Chimie/ou physique
- Sciences du Vivant/Médecine humaine et pathologie/Dermatologie
- Sciences du Vivant/Immunologie/Immunité innée
- Sciences du Vivant/Sciences pharmaceutiques
- Sciences du Vivant/Biochimie, Biologie Moléculaire/Biophysique
- Sciences du Vivant/Autre
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Dernieres productions scientifiques :
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Beta-hydroxyphosphonate ribonucleoside analogues derived from 4-substituted-1,2,3-triazoles as IMP/GMP mimics: synthesis and biological evaluation
Auteur(s): Nguyen V. T., Hospital A., Lionne C., Jordheim L.P., Dumontet C., Perigaud C., Chaloin L., Peyrottes S.
(Article) Publié:
Beilstein Journal Of Organic Chemistry, vol. 12 p.1476--1486 (2016)
Ref HAL: hal-01812668_v1
PMID 27559400
DOI: 10.3762/bjoc.12.144
Résumé: A series of seventeen beta-hydroxyphosphonate ribonucleoside analogues containing 4-substituted-1,2,3-triazoles was synthesized and fully characterized. Such compounds were designed as potential inhibitors of the cytosolic 5'-nucleotidase II (cN-II), an enzyme involved in the regulation of purine nucleotide pools. NMR and molecular modelling studies showed that a few derivatives adopted similar structural features to IMP or GMP. Five derivatives were identified as modest inhibitors with 53 to 64% of cN-II inhibition at 1 mM
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Identification of noncompetitive inhibitors of cytosolic 5′-nucleotidase II using a fragment-based approach
Auteur(s): Marton Zsuzsanna, Guillon R., Krimm Isabelle, Rahimova Rahila, Egron D., Jordheim Lars P., Aghajari Nushin, Dumontet Charles, Perigaud C., Lionne Corinne, Peyrottes S., Chaloin Laurent
(Article) Publié:
European Journal Of Medicinal Chemistry, vol. 58 p.9680-9696 (2015)
Ref HAL: hal-01251800_v1
PMID 26599519
DOI: 10.1021/acs.jmedchem.5b01616
Résumé: We used a combined approach based on fragment-based drug design (FBDD) and in silico methods to design potential inhibitors of the cytosolic 5'-nucleotidase II (cN-II), which has been recognized as an important therapeutic target in hematological cancers. Two subgroups of small compounds (including adenine and biaryl moieties) were identified as cN-II binders and a fragment growing strategy guided by molecular docking was considered. Five compounds induced a strong inhibition of the 5'-nucleotidase activity in vitro, and the most potent ones were characterized as noncompetitive inhibitors. Biological evaluation in cancer cell lines showed synergic effect with selected anticancer drugs. Structural studies using X-ray crystallography lead to the identification of new binding sites for two derivatives and of a new crystal form showing important domain swapping. Altogether, the strategy developed herein allowed identifying new original noncompetitive inhibitors against cN-II that act in a synergistic manner with well-known antitumoral agents.
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201Tl+-labelled Prussian blue nanoparticles as contrast agents for SPECT scintigraphy.
Auteur(s): Perrier Marine, Busson Muriel, Massasso Giovanni, long jérome, Boudousq Vincent, Pouget Jean-Pierre, Peyrottes S., Perigaud C., Porredon-Guarch Constança, de Lapuente Joaquin, Borras Miquel, Larionova Joulia, Guari Yannick
(Article) Publié:
Nanoscale, vol. 6 p.13425-13429 (2014)
Ref HAL: hal-01084124_v1
DOI: 10.1039/c4nr03044c
Résumé: Prussian blue (PB) and its analogues on the nanometric scale are exciting nano-objects that combine the advantages of molecular-based materials and nanochemistry. Herein, we demonstrate that ultra-small PB nanoparticles of 2–3 nm can be easily labelled with radioactive 201Tl+ to obtain new nanoprobes as radiotracers for 201-thallium-based imaging.
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Synthesis of {[5-(adenin-9-yl)-2-furyl]methoxy}methyl phosphonic acid and evaluations against human adenylate kinases.
Auteur(s): Perigaud C.
(Article) Publié:
Bioorganic & Medicinal Chemistry Letters / Bioorganic And Medicinal Chemistry Letters, vol. 24 p.4227-4230 (2014)
Ref HAL: hal-01061638_v1
DOI: 10.1016/j.bmcl.2014.07.036
Résumé: AMP mimics constitute an important class of therapeutic derivatives to treat diseases where the pool of ATP is involved. A new phosphonate derivative of 9-(5-hydroxymethylfuran-2-yl)adenine was synthesized in a multi-step sequence from commercially available adenosine. Its ability to behave as a substrate of human adenylate kinases 1 and 2 was assessed. The phosphonate was shown to be a moderate but selective substrate of the mitochondrial human AK2, better than well-known antiviral acyclic phosphonates 9-(2-phosphonomethoxyethyl)adenine (PMEA, Adefovir) and (R)-9-(2-phosphonomethoxypropyl)adenine (PMPA, Tenofovir). Putative binding mode within adenylate kinase NMP site revealed by molecular docking in comparison to AMP native substrate allowed to illustrate this selective behavior.
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Exploring prodrug approaches for albitiazolium and its analogues.
Auteur(s): Peyrottes S., Caldarelli S., Wein Sharon, Perigaud C., Vial Henri
(Article) Publié:
Current Topics In Medicinal Chemistry, vol. 14 p.1653-1667 (2014)
Ref HAL: hal-01078458_v1
PMID 25116583
DOI: 10.2174/1568026614666140808121746
Résumé: Choline analogues such as bis-thiazolium salts are thought to inhibit choline transport into Plasmodiuminfected erythrocytes, thus preventing parasite PC biosynthesis, and also to interact with plasmodial haemoglobin degradation in the food vacuole. This new and multiple mode of action is a major asset of these new class of antimalarials, as they could help delay resistance development. We synthesized and designed various sets of analogues, notably prodrugs, since the oral bioavailability of bis-thiazolium salts is relatively low. The chemistry underlying this synthesis relies on inexpensive and readily available starting materials and is straightforward. This is essential since the ultimate objective is to obtain affordable and orally available drugs for uncomplicated malaria treatment.
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