Laboratoire

Chimie et biocatalyse

Responsable

Sylvie Pochet

CNRS UMR3523

Département de Biologie structurale et chimie

• Biochemistry
• Bioorganic Chemistry
• Chemical biology
• DNA biosynthesis, modification, repair and degradation
• Medicinal Chemistry
• Molecular interactions
• Organic Chemistry
• Auto-immune disease
• Bacterial diseases
• Fungal diseases
• Immunodeficiency
• Anticancer treatments
• Chemical probes
• Pharmacology, pharmacogenomics, drug discovery and design, drug therapy
• Prevention and treatment of infection by pathogens
• Chemical library screening

VOIR TOUSFermer

Présentation

 

 

Groupes

Group

Yves Janin

Groupe : Yves Janin

Group

Hélène Munier-Lehmann

Groupe: Biochimie et criblage

Membres

Sylvie Pochet

Responsable de Structure

Responsable

Frédéric Bonhomme

Ingénieur(e) de Recherche

Laurence Dugue

Technicien(ne)

Marie-Ange Garnier

Personnel Administratif

Olivier Helynck

Technicien(ne)

Valérie Huteau

Technicien(ne)

Yves Janin

Chef(fe) de Groupe

Hélène Munier-Lehmann

Chef(fe) de Groupe

Sophie Vichier-Guerre

Chercheur(euse) Permanent(e)

Eloi Coutant

Etudiant(e) en thèse

Loic Sanchez

Etudiant(e)

Glwadys Gagnot

Etudiant(e) M2

Steve Chiumento

Etudiant(e) M2

Patrick Walter

Etudiant(e) en thèse

Anciens Membres

Pierre Alexandr Kaminski

Julie Paoletti

Claire Amiable

Elise Salanouve

Anne Noel

Nicolas Wlodarczyk

Sandrine Guillou

Soizic Prado

Alex Cartier

Luke Alvey

Olivier Nesme

Nathalie Trawinski

Thuy-Ha Dao

Céline Taglang

Laura Lanoe

Valérie Toum

Gigliola Zanghì

Thomas Alexandre

Isabelle Salard-Arnaud

Alexandru Lupan

Edouard Seclaman

Laurene Vaupre

Victor Penaud

Khaled BENKALI

Brice Murciano

Dhenesh Puvanendran

William Pauly-Batard

Vincent Hervin

Judith Souphron

Insaf ESSADIK

Aurélie Bourderioux

Projets

AEGIS (Accelerated Early staGe drug dIScovery)

AEGIS is a Marie Skłodowska -Curie Innovative Training Network (ITN) for early stage researchers (ESR) funded by the European Commission under the H2020 Programme the EU framework programme for research and innovation. The principal […]

Inhibitors of Pseudomonas aeruginosa IMPDH

IMPDH from Pseudomonas aeruginosa (see Inosine-5′-monophosphate dehydrogenase project) was found to be allosterically regulated by MgATP (Labesse et al., 2013). The discovery of this mode of regulation of the catalytic activity, never described before […]

Inhibitors of TMPK from Mycobacterium tuberculosis

TMPK from Mycobacterium tuberculosis belongs to the NMPK family, which was chosen as potential targets for the development of new antimicrobials (see “Nucleoside monophosphate kinases” project).Based on the 3D-structure of TMPK from M. tuberculosis […]

Design and optimization of new bioluminescent systems better-suited to in cellulo and in vivo conditions

The use of light from the abyss in biology In the last decades, bioluminescent systems based on the expression of a luciferase and the addition of a luciferin to monitor the emission of light have […]

Finding new antimycobacterials, the dibenzofurans story

A selective antimycobacterial effectThis project started from the modest but rather selective antimycobacterial effect of “dibenzofuran” derivatives such as compounds 1 and 2. Their minimum inhibitory concentration necessary to prevent 99 % (MIC 99) […]

Inhibitors of the 2’-deoxyribonucleotide N-hydrolase DNPH1, an enzyme involved in cellular growth and angiogenesis

Nucleoside analogues as potential antitumor agents.  This project aims to characterize and validate the nucleotide N-hydrolase DNPH1 as a new target in oncology. Inhibition of Rcl alone or in combination with other chemotherapeutic drugs should […]

Alkoxypyrazoles, inhibitors of dihydroorotate dehydrogenase (DHODH)

A thousand fold improvement of an antiviral activity The starting point of this project was the modest activity displayed by compounds 1 and 2, on the phenotypic Measles-based antiviral assay designed by Pierre-Olivier Vidalain (1) […]

ATPase inhibitors, the cases of human heat shock protein 90 and bacterial type IIA topoisomerases

Organic synthesis, still the limiting factor of Medicinal Chemistry? This ongoing project is based on our reviews (1-3) on the inhibitors of the ATPase functions of human heat shock protein 90 (HSP90) or bacterial type […]

Inhibitors of bacterial NAD kinases

NAD mimics as potential antibacterial agentsThe NAD(P) biosynthesis pathways have attracted recent interest as a source of enzyme targets for the development of antimicrobial agents. Our own research focused on the structure-based development of […]

Alkoxypyrazoles, new chemical entities

Removing “chemical blind spots”, the case of the hydroxpyrazolesThe synthesis of 5-hydroxypyrazoles has been trivial for about 140 years. Indeed, the synthetic path found by Knorr in 1883 was extensively used over the years […]

Inosine-5′-monophosphate dehydrogenase

 Inosine-5′-monophosphate dehydrogenase (IMPDH) is ubiquitously essential for the biosynthesis of guanosine nucleotides and catalyzes the NAD-dependent oxidation of IMP to XMP. IMPDH is a major target in the design of both antitumor and immunosuppresive […]

Nucleoside monophosphate kinases (NMPKs)

NMPKs are ubiquitous enzymes, which catalyze the reversible transfer of phosphoryl group from ATP to an NMP, and are essential for cell division, growth and metabolism. In bacteria there are five NMPKs, each one […]

Brevets

NOVEL ANTIBACTERIAL COMPOUNDS

The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim 1. The compounds are useful in the prevention and/or treatment […]

Publications

• 2016
  Expedient and generic synthesis of imidazole nucleosides by enzymatic transglycosylation - S. Vichier-Guerre, L. Dugué, F. Bonhomme and S. Pochet - Organic & Biomolecular Chemistry
• 2016
  Synthesis and evaluation of original bioisosteres of bacterial type IIA topoisomerases inhibitors - Stéphanie Petrella, Alexandra Aubry, Geneviève Janvier, Eloi Paul Coutant, Alex Cartier, Thuy-Ha Dao, Frédéric Bonhomme, Laurence Motreff, Cédric Pissis, Chantal Bizet, Dominique Clermont, Evelyne Begaud, Pascal Retailleau, Hélène Munier-Lehmann, Estelle Capton, Claudine Mayer, Yves Janin - Canadian Journal of Chemistry
• 2016
  Respiratory syncytial virus infection in macaques is not suppressed by intranasal sprays of pyrimidine biosynthesis inhibitors - Grandin C, Hourani ML, Janin YL, Dauzonne D, Munier-Lehmann H, Paturet A, Taborik F, Vabret A, Contamin H, Tangy F, Vidalain PO - Antiviral research
• 2015
  The Toxicity of a Novel Antifungal Compound Is Modulated by Endoplasmic Reticulum-Associated Protein Degradation Components - Raj S, Krishnan K, Askew DS, Helynck O, Suzanne P, Lesnard A, Rault S, Zeidler U, d'Enfert C, Latgé JP, Munier-Lehmann H, Saveanu C - Antimicrobial agents and chemotherapy
• 2015
  Synthetic Routes to Coelenterazine and Other Imidazo[1,2-a]pyrazin-3-one Luciferins: Essential Tools for Bioluminescence-Based Investigations - Coutant EP, Janin YL - Chemistry: A European Journal
• 2015
  Crystallographic studies of two variants of Pseudomonas aeruginosa IMPDH with impaired allosteric regulation - Labesse G, Alexandre T, Gelin M, Haouz A, Munier-Lehmann H - Acta crystallographica. Section D, Biological crystallography
• 2015
  Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH) - Lucas-Hourani M, Munier-Lehmann H, El Mazouni F, Malmquist NA, Harpon J, Coutant EP, Guillou S, Helynck O, Noel A, Scherf A, Phillips MA, Tangy F, Vidalain PO, Janin YL - Journal of medicinal chemistry
• 2015
  Unprecedented formation of 8(R),5′-O-cycloribonucleosides through a triflation reaction of purine ribonucleosides - Claire Amiable and Sylvie Pochet - Tetrahedron
• 2015
  Two classes of bacterial IMPDHs according to their quaternary structures and catalytic properties - Alexandre T, Raynal B, Rayna B, Munier-Lehmann H - PloS one
• 2015
  A study of Negishi cross-coupling reactions with benzylzinc halides to prepare original 3-ethoxypyrazoles - Coutant, E. P.; Janin, Y. L. - Synthesis
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  Voir la liste complète de publications

Contact

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Address
25-28 Rue du Docteur Roux
75015, Paris
France