Jean-Francois Guichou
ABCIS: Atelier de Bio & Chimie Informatique Structurale
04 67 41 77 12
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Liste des publications
2024
2023
Development of HC-258, a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration
Fnaiche A, Chan HC, Paquin A, Gonzalez Suarez N, Vu V, Li F, Allali-Hassani A, Cao MA, Szewczyk MM, Bolotokova A, Allemand F, Gelin M, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Guichou JF, Annabi B, Gagnon A, ACS Med Chem Lett, 2023
Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings
Fnaiche A, Melin L, Suarez NG, Paquin A, Vu V, Li F, Allali-Hassani A, Bolotokova A, Allemand F, Gelin M, Cotelle P, Woo S, LaPlante SR, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Guichou JF, Annabi B, Gagnon A, Bioorg Med Chem Lett, 2023
The novel cyclophilin inhibitor C105SR reduces hepatic ischaemia-reperfusion injury via mitoprotection
Kheyar A, Ahnou N, Ahmed-Belkacem A, Hulin A, Pressiat C, Ghaleh B, Guichou JF, Morin D, Pawlotsky JM, Teixeira-Clerc F, JHEP Rep, 2023
Linkers in fragment-based drug design: an overview of the literature
Grenier D, Audebert S, Preto J, Guichou JF, Krimm I, Expert Opin Drug Discov, 2023
Cyclophilin A Isomerisation of Septin 2 Mediates Abscission during Cytokinesis
Gorry RL, Brennan K, Lavin PTM, Mazurski T, Mary C, Matallanas D, Guichou JF, Mc Gee MM, Int J Mol Sci, 2023
Small-Molecule Cyclophilin Inhibitors Potently Reduce Platelet Procoagulant Activity
Van Bael J, Vandenbulcke A, Ahmed-Belkacem A, Guichou JF, Pawlotsky JM, Samyn J, Barendrecht AD, Maas C, De Meyer SF, Vanhoorelbeke K, Tersteeg C, Int J Mol Sci, 2023
A Tripartite Complex HIV-1 Tat-Cyclophilin A-Capsid Protein Enables Tat Encapsidation That Is Required for HIV-1 Infectivity
Schatz M, Marty L, Ounadjela C, Tong PBV, Cardace I, Mettling C, Milhiet PE, Costa L, Godefroy C, Pugniere M, Guichou JF, Mesnard JM, Blaise M, Beaumelle B, J Virol, 2023
2022
Toward the Design of Ligands Selective for the C-Terminal Domain of TEADs
Liberelle M, Toulotte F, Renault N, Gelin M, Allemand F, Melnyk P, Guichou JF, Cotelle P, J Med Chem, 2022
A Histone Deacetylase (HDAC) Inhibitor with Pleiotropic In Vitro Anti-Toxoplasmaand Anti-PlasmodiumActivities Controls Acute and Chronic ToxoplasmaInfection in Mice
Jublot D, Cavailles P, Kamche S, Francisco D, Fontinha D, Prudencio M, Guichou JF, Labesse G, Sereno D, Loeuillet C, Int J Mol Sci, 2022
2021
Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors
Sturbaut M, Bailly F, Coevoet M, Sileo P, Pugniere M, Liberelle M, Magnez R, Thuru X, Chartier-Harlin MC, Melnyk P, Gelin M, Allemand F, Guichou JF, Cotelle P, Eur J Med Chem, 2021
Design, Synthesis and Evaluation of a Series of 1,5-Diaryl-1,2,3-triazole-4-carbohydrazones as Inhibitors of the YAP-TAZ/TEAD Complex
Gibault F, Sturbaut M, Coevoet M, Pugniere M, Burtscher A, Allemand F, Melnyk P, Hong W, Rubin BP, Pobbati AV, Guichou JF, Cotelle P, Bailly F, ChemMedChem, 2021
2020
A phenyl pyrrolidine derivative reveals a dual inhibition mechanism of myocardial mitochondrial permeability transition pore, which is limited by its myocardial distribution
Panel M, Ahmed-Belkacem A, Ruiz I, Guichou JF, Pawlotsky JM, Ghaleh B, Morin D, J Pharmacol Exp Ther, 2020
Circulating tumor DNA genomics reveals potential mechanisms of resistance to BRAF-targeted therapies in BRAF-mutant metastatic non-small cell lung cancer patients
Ortiz-Cuaran S, Mezquita L, Swalduz A, Aldea M, Mazieres J, Leonce C, Jovelet C, Pradines A, Avrillon V, Chumbi Flores WR, Lacroix L, Loriot Y, Westeel V, Ngo-Camus M, Tissot C, Raynaud C, Gervais R, Brain E, Monnet I, Giroux Leprieur E, Caramella C, Mahier-Aut Oukhatar C, Hoog-Labouret N, de Kievit F, Howarth K, Morris C, Green E, Friboulet L, Chabaud S, Guichou JF, Perol M, Besse B, Blay JY, Saintigny P, Planchard D, Clin Cancer Res, 2020
Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action
Patinote C, Deleuze-Masquefa C, Kaddour KH, Vincent LA, Larive R, Zghaib Z, Guichou JF, Assaf MD, Cuq P, Bonnet PA, Eur J Med Chem, 2020
Fragment Linking Strategies for Structure-Based Drug Design
Bancet A, Raingeval C, Lomberget T, Le Borgne M, Guichou JF, Krimm I, J Med Chem, 2020
2019
Small-molecule inhibitors of cyclophilins block opening of the mitochondrial permeability transition pore and protect mice from hepatic ischemia-reperfusion injury
Panel M, Ruiz I, Brillet R, Lafdil F, Teixeira-Clerc F, Nguyen CT, Calderaro J, Gelin M, Allemand F, Guichou JF, Ghaleh B, Ahmed-Belkacem A, Morin D, Pawlotsky JM, Gastroenterology, 2019
The Ellagitannin Metabolite Urolithin C is a Glucose-Dependent Regulator of Insulin Secretion through L-type Calcium Channel Activation
Bayle M, Neasta J, Dall'Asta M, Gautheron G, Virsolvy A, Quignard JF, Youl E, Magous R, Guichou JF, Crozier A, Del Rio D, Cros G, Oiry C, Br J Pharmacol, 2019
Novel and selective TLR7 antagonists among the imidazo[1,2-a]pyrazines, imidazo[1,5-a]quinoxalines and pyrazolo[1,5-a]quinoxalines series
Bou Karroum N, Moarbess G, Guichou JF, Bonnet PA, Patinote C, Bouharoun-Tayoun H, Chamat S, Cuq P, Diab-Assaf M, Kassab I, Masquefa C, J Med Chem, 2019
A Tiny Change Makes a Big Difference in the Anti-Parasitic Activities of an HDAC Inhibitor
Loeuillet C, Touquet B, Guichou JF, Labesse G, Sereno D, Int J Mol Sci, 2019
Structural basis for chemically-induced homodimerization of a single domain antibody
Lesne J, Chang HJ, De Visch A, Paloni M, Barthe P, Guichou JF, Mayonove P, Barducci A, Labesse G, Bonnet J, Cohen-Gonsaud M, Sci Rep, 2019
2018
Structural determinants of the catalytic mechanism of Plasmodium CCT, a key enzyme of malaria lipid biosynthesis
Guca E, Nagy GN, Hajdu F, Marton L, Izrael R, Hoh F, Yang Y, Vial H, Vertessy BG, Guichou JF, Cerdan R, Sci Rep, 2018
Characterization of the anti-hepatitis C virus activity of new non-peptidic small-molecule cyclophilin inhibitors with a potential for broad anti-
Nevers Q, Ruiz I, Ahnou N, Donati F, Brillet R, Softic L, Chazal M, Jouvenet N, Fourati S, Baudesson C, Bruscella P, Gelin M, Guichou JF, Pawlotsky JM, Ahmed-Belkacem A, Antimicrob Agents Chemother, 2018
Toward the Discovery of a Novel Class of YAPaTEAD Interaction Inhibitors by Virtual Screening Approach Targeting YAPaTEAD ProteinaProtein Interface
Gibault F, Coevoet M, Sturbaut M, Farce A, Renault N, Allemand F, Guichou JF, Drucbert AS, Foulon C, Magnez R, Thuru X, Corvaisier M, Huet G, Chavatte P, Melnyk P, Bailly F, Cotelle P, Cancers (Basel), 2018
Synthesis of aminophenylhydroxamate and aminobenzylhydroxamate derivatives and in vitro screening for antiparasitic and histone deacetylase inhibitory activity
Loeuillet C, Touquet B, Oury B, Eddaikra N, Pons JL, Guichou JF, Labesse G, Sereno D, Int J Parasitol Drugs Drug Resist, 2018
2016
Fragment-based discovery of a new family of non-peptidic small-molecule cyclophilin inhibitors with potent antiviral activities
Ahmed-Belkacem A, Colliandre L, Ahnou N, Nevers Q, Gelin M, Bessin Y, Brillet R, Cala O, Douguet D, Bourguet W, Krimm I, Pawlotsky JM, Guichou JF, Nat Commun, 2016
Nuclear Envelope Protein SUN2 Promotes Cyclophilin-A-Dependent Steps of HIV Replication
Lahaye X, Satoh T, Gentili M, Cerboni S, Silvin A, Conrad C, Ahmed-Belkacem A, Rodriguez EC, Guichou JF, Bosquet N, Piel M, Le Grand R, King MC, Pawlotsky JM, Manel N, Cell Rep, 2016
New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships
Zghaib Z, Guichou JF, Vappiani J, Bec N, Hadj-Kaddour K, Vincent LA, Paniagua-Gayraud S, Larroque C, Moarbess G, Cuq P, Kassab I, Deleuze-Masquefa C, Diab-Assaf M, Bonnet PA, Bioorg Med Chem, 2016
New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors
Moarbess G, Guichou JF, Paniagua-Gayraud S, Chouchou A, Marcadet O, Leroy F, Ruedas R, Cuq P, Deleuze-Masquefa C, Bonnet PA, Eur J Med Chem, 2016
Aminoglycoside binding and catalysis specificity of aminoglycoside 2a-phosphotransferase IVa: A thermodynamic, structural and kinetic study
Kaplan E, Guichou JF, Chaloin L, Kunzelmann S, Leban N, Serpersu EH, Lionne C, Biochim Biophys Acta, 2016
2015
Combining `dry' co-crystallization and in situ diffraction to facilitate ligand screening by X-ray crystallography
Gelin M, Delfosse V, Allemand F, Hoh F, Sallaz-Damaz Y, Pirocchi M, Bourguet W, Ferrer JL, Labesse G, Guichou JF, Acta Crystallogr D Biol Crystallogr, 2015
Two crystal structures of the FK506-binding domain of Plasmodium falciparum FKBP35 in complex with rapamycin at high resolution
Bianchin A, Allemand F, Bell A, Chubb AJ, Guichou JF, Acta Crystallogr D Biol Crystallogr, 2015
2014
Comparing Binding Modes of Analogous Fragments Using NMR in Fragment-Based Drug Design: Application to PRDX5
Aguirre C, Brink TT, Guichou JF, Cala O, Krimm I, PLoS ONE, 2014
Protein-ligand structure guided by backbone and side-chain proton chemical shift perturbations
Aguirre C, Ten Brink T, Cala O, Guichou JF, Krimm I, J Biomol NMR, 2014
Inhibition of RNA binding to hepatitis C virus RNA-dependent RNA polymerase: a new mechanism for antiviral intervention
Ahmed-Belkacem A, Guichou JF, Brillet R, Ahnou N, Hernandez E, Pallier C, Pawlotsky JM, Nucleic Acids Res, 2014
Homodimerization of RBPMS2 through a new RRM-interaction motif is necessary to control smooth muscle plasticity
Sagnol S, Yang Y, Bessin Y, Allemand F, Hapkova I, Notarnicola C, Guichou JF, Faure S, Labesse G, de Santa Barbara P, Nucleic Acids Res, 2014
2013
2012
Fragment and conquer: from structure to complexes to function.
Guichou JF, Labesse G, Structure, 2012
e-Drug3D: 3D structure collections dedicated to drug repurposing and fragment-based drug design.
Pihan E, Colliandre L, Guichou JF, Douguet D, Bioinformatics, 2012
2011
The Leishmania nicotinamidase is essential for NAD+ production and parasite proliferation
Gazanion E, Garcia D, Silvestre R, Gerard C, Guichou JF, Labesse G, Seveno M, Cordeiro-Da-Silva A, Ouaissi A, Sereno D, Vergnes B, Mol Microbiol, 2011
In-plate protein crystallization, in situ ligand soaking and X-ray diffraction
le Maire A, Gelin M, Pochet S, Hoh F, Pirocchi M, Guichou JF, Ferrer JL, Labesse G, Acta Crystallogr D Biol Crystallogr, 2011
2008
N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists
Benod C, Subra G, Nahoum V, Mallavialle A, Guichou JF, Milhau J, Robles S, Bourguet W, Pascussi JM, Balaguer P, Chavanieu A, Bioorg Med Chem, 2008
Nuclear receptor ligand-binding domains: reduction of helix H12 dynamics to favour crystallization
Nahoum V, Lipski A, Quillard F, Guichou JF, Boublik Y, Perez E, Germain P, de Lera AR, Bourguet W, Acta Crystallogr Sect F Struct Biol Cryst Commun, 2008
Structural basis for the interaction between focal adhesion kinase and CD4
Garron ML, Arthos J, Guichou JF, McNally J, Cicala C, Arold ST, J Mol Biol, 2008
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement
Frey V, Viaud J, Subra G, Cauquil N, Guichou JF, Casara P, Grassy G, Chavanieu A, Eur J Med Chem, 2008
2007
2006
Structure-based design, synthesis, and biological evaluation of novel inhibitors of human cyclophilin A
Guichou JF, Viaud J, Mettling C, Subra G, Lin YL, Chavanieu A, J Med Chem, 2006
Structural basis for the Akt (PKB) kinase inhibition by the peptide Akt-in: an NMR study.
Ropars V, Guichou J-F, Auguin D, Barthe P, Noguchi M, Roumestand C, C. R. Chimie, 2006
2005
Strength and character of peptide/anion interactions
Chavanieu A, Guichou JF, Prado-Gotor R, Perez-Tejeda P, Jimenez R, Lopez-Cornejo P, Sanchez F, J Phys Chem B, 2005
Chemical cross-linking photosensitized by ruthenium chelate as a new tool for signaling studies
Duroux-Richard I, Guichou JF, Subra G, Mouillac B, Vassault P, Marie J, Chavanieu A, Bonnafous JC, Eur. Biophys. J., 2005
Crosslinking photosensitized by a ruthenium chelate as a tool for labeling and topographical studies of G-protein-coupled receptors
Duroux-Richard I, Vassault P, Subra G, Guichou JF, Richard E, Mouillac B, Barberis C, Marie J, Bonnafous JC, Chem Biol, 2005
Characterization of the interaction between retinoic acid receptor/retinoid X receptor (RAR/RXR) heterodimers and transcriptional coactivators through structural and fluorescence anisotropy studies
Pogenberg V, Guichou JF, Vivat-Hannah V, Kammerer S, Perez E, Germain P, de Lera AR, Gronemeyer H, Royer CA, Bourguet W, J Biol Chem, 2005
2004
TLR-independent control of innate immunity in Caenorhabditis elegans by the TIR domain adaptor protein TIR-1, an ortholog of human SARM
Couillault C, Pujol N, Reboul J, Sabatier L, Guichou JF, Kohara Y, Ewbank JJ, Nat Immunol, 2004
Purification and crystallization of the heterodimeric complex of RARbeta and RXRalpha ligand-binding domains in the active conformation
Pogenberg V, Guichou JF, Bourguet W, Acta Crystallogr D Biol Crystallogr, 2004
Crystal Structure of the Coiled-coil Dimerization Motif of Geminin: Structural and Functional Insights on DNA Replication Regulation
Thepaut M, Maiorano D, Guichou JF, Auge MT, Dumas C, Mechali M, Padilla A, J Mol Biol, 2004