Détail - canceropole-wordpress

Frantz MC, Pellissier LP, Pflimlin E, Loison S, Gandía J, Marsol C, Durroux T, Mouillac B, Becker JAJ, Le Merrer J, Valencia C, Villa P, Bonnet D, Hibert M

J. Med. Chem.. 2018 Sep 24;:

Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia.

Regenass P, Abboud D, Daubeuf F, Lehalle C, Gizzi P, Riché S, Hachet-Haas M, Rohmer F, Gasparik V, Boeglin D, Haiech J, Knehans T, Rognan D, Heissler D, Marsol C, Villa P, Galzi JL, Hibert M, Frossard N, Bonnet D

J. Med. Chem.. 2018 Aug 14;:

WNK1 kinase and its partners Akt, SGK1 and NBC-family Na/HCO3 cotransporters are potential therapeutic targets for glioblastoma stem-like cells linked to Bisacodyl signaling.

Chen W, Zebaze LN, Dong J, Chézeau L, Inquimbert P, Hugel S, Niu S, Bihel F, Boutant E, Réal E, Villa P, Junier MP, Chneiweiss H, Hibert M, Haiech J, Kilhoffer MC, Zeniou M

Oncotarget. 2018 Jun 5;9(43):27197-27219

From the Promiscuous Asenapine to Potent Fluorescent Ligands Acting at a Series of Aminergic G-Protein-Coupled Receptors.

Hounsou C, Baehr C, Gasparik V, Alili D, Belhocine A, Rodriguez T, Dupuis E, Roux T, Mann A, Heissler D, Pin JP, Durroux T, Bonnet D, Hibert M

J. Med. Chem.. 2018 Jan 11;61(1):174-188

[(11)C]PF-3274167 as a PET radiotracer of oxytocin receptors: Radiosynthesis and evaluation in rat brain.

Vidal B, Karpenko IA, Liger F, Fieux S, Bouillot C, Billard T, Hibert M, Zimmer L

Nucl. Med. Biol.. 2017 Aug;55:1-6

A Time-Resolved FRET Cell-Based Binding Assay for the Apelin Receptor.

Valencia C, Dujet C, Margathe JF, Iturrioz X, Roux T, Trinquet E, Villa P, Hibert M, Dupuis E, Llorens-Cortes C, Bonnet D

ChemMedChem. 2017 Apr;:

Comparative Study of the Synthesis and Structural and Physicochemical Properties of Diketopiperazines vs Aza-diketopiperazines.

Regenass P, Bosc D, Riché S, Gizzi P, Hibert M, Karmazin L, Ganesan A, Bonnet D

J. Org. Chem.. 2017 Mar;82(6):3239-3244

Development of original metabolically stable apelin-17 analogs with diuretic and cardiovascular effects.

Gerbier R, Alvear-Perez R, Margathe JF, Flahault A, Couvineau P, Gao J, De Mota N, Dabire H, Li B, Ceraudo E, Hus-Citharel A, Esteoulle L, Bisoo C, Hibert M, Berdeaux A, Iturrioz X, Bonnet D, Llorens-Cortes C

FASEB J.. 2017 Feb;31(2):687-700

A step-economical multicomponent synthesis of 3D-shaped aza-diketopiperazines and their drug-like chemical space analysis.

Regenass P, Riché S, Péron F, Rognan D, Hibert M, Girard N, Bonnet D

Org. Biomol. Chem.. 2016 Sep;14(37):8859-8863

Convenient Access to Fluorescent Probes by Chemoselective Acylation of Hydrazinopeptides: Application to the Synthesis of the First Far-Red Ligand for Apelin Receptor Imaging.

Margathe JF, Iturrioz X, Regenass P, Karpenko IA, Humbert N, de Rocquigny H, Hibert M, Llorens-Cortes C, Bonnet D

Chemistry. 2016 Jan;22(4):1399-405

Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.

Karpenko IA, Margathe JF, Rodriguez T, Pflimlin E, Dupuis E, Hibert M, Durroux T, Bonnet D

J Med Chem. 2015 Mar 12;58(5):2547-52

Squaraine as a bright, stable and environment-sensitive far-red label for receptor-specific cellular imaging.

Karpenko IA, Klymchenko AS, Gioria S, Kreder R, Shulov I, Villa P, Mely Y, Hibert M, Bonnet D

Chem Commun (Camb). 2015 Feb 18;51(14):2960-3

Tampering with cell division by using small-molecule inhibitors of CDK-CKS protein interactions.

Hamdi A, Lesnard A, Suzanne P, Robert T, Miteva MA, Pellerano M, Didier B, Ficko-Blean E, Lobstein A, Hibert M, Rault S, Morris MC, Colas P

Chembiochem. 2015 Feb 9;16(3):432-9

A strategy to discover decoy chemokine ligands with an anti-inflammatory activity.

Abboud D, Daubeuf F, Do QT, Utard V, Villa P, Haiech J, Bonnet D, Hibert M, Bernard P, Galzi JL, Frossard N

Sci Rep. 2015 Oct 7;5:14746

Chemical Library Screening and Structure-Function Relationship Studies Identify Bisacodyl as a Potent and Selective Cytotoxic Agent Towards Quiescent Human Glioblastoma Tumor Stem-Like Cells.

Zeniou M, Feve M, Mameri S, Dong J, Salome C, Chen W, El-Habr EA, Bousson F, Sy M, Obszynski J, Boh A, Villa P, Assad Kahn S, Didier B, Bagnard D, Junier MP, Chneiweiss H, Haiech J, Hibert M, Kilhoffer MC

PLoS One. 2015 Aug 13;10(8):e0134793

Fluorogenic Squaraine Dimers with Polarity-Sensitive Folding As Bright Far-Red Probes for Background-Free Bioimaging.

Karpenko IA, Collot M, Richert L, Valencia C, Villa P, Mely Y, Hibert M, Bonnet D, Klymchenko AS

J Am Chem Soc. 2014 Dec 29.

Time-Resolved FRET Binding Assay to Investigate Hetero-Oligomer Binding Properties: Proof of Concept with Dopamine D/D Heterodimer.

Hounsou C, Margathe JF, Oueslati N, Belhocine A, Dupuis E, Thomas C, Mann A, Ilien B, Rognan D, Trinquet E, Hibert M, Pin JP, Bonnet D, Durroux T

ACS Chem Biol. 2014 Nov 11.

Design of a general-purpose European compound screening library for EU-OPENSCREEN.

Horvath D, Lisurek M, Rupp B, Kuhne R, Specker E, von Kries J, Rognan D, Andersson CD, Almqvist F, Elofsson M, Enqvist PA, Gustavsson AL, Remez N, Mestres J, Marcou G, Varnek A, Hibert M, Quintana J, Frank R

ChemMedChem. 2014 Oct;9(10):2309-26

Diastereoselective synthesis of novel aza-diketopiperazines via a domino cyclohydrocarbonylation/addition process.

Regenass P, Margathe JF, Mann A, Suffert J, Hibert M, Girard N, Bonnet D

Chem Commun (Camb). 2014 Sep 4;50(68):9657-60

Structure-activity relationship studies toward the discovery of selective apelin receptor agonists.

Margathe JF, Iturrioz X, Alvear-Perez R, Marsol C, Riche S, Chabane H, Tounsi N, Kuhry M, Heissler D, Hibert M, Llorens-Cortes C, Bonnet D

J Med Chem. 2014 Apr 10;57(7):2908-19

Quantitative structure-property relationship modeling: a valuable support in high-throughput screening quality control.

Ruggiu F, Gizzi P, Galzi JL, Hibert M, Haiech J, Baskin I, Horvath D, Marcou G, Varnek A

Anal Chem. 2014 Mar 4;86(5):2510-20

Red fluorescent turn-on ligands for imaging and quantifying G protein-coupled receptors in living cells.

Karpenko IA, Kreder R, Valencia C, Villa P, Mendre C, Mouillac B, Mely Y, Hibert M, Bonnet D, Klymchenko AS

Chembiochem. 2014 Feb 10;15(3):359-63

Selective fluorescent nonpeptidic antagonists for vasopressin V(2) GPCR: application to ligand screening and oligomerization assays.

Loison S, Cottet M, Orcel H, Adihou H, Rahmeh R, Lamarque L, Trinquet E, Kellenberger E, Hibert M, Durroux T, Mouillac B, Bonnet D

J Med Chem. 2012 Oct 25;55(20):8588-602

Adsorption of [Mn-19] Aggregates with S=83/2 onto HOPG Surfaces.

Ako AM, Alam MS, Mameri S, Lan YH, Hibert M, Stocker M, Muller P, Anson CE, Powell AK

. 2012 Sep;26:4131-40.

Combinatorial aid for underprivileged scaffolds: solution and solid-phase strategies for a rapid and efficient access to novel aza-diketopiperazines (Aza-DKP).

Bonnet D, Margathe JF, Radford S, Pflimlin E, Riche S, Doman P, Hibert M, Ganesan A

ACS Comb Sci. 2012 May 14;14(5):323-34

Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.

Daval SB, Valant C, Bonnet D, Kellenberger E, Hibert M, Galzi JL, Ilien B

J Med Chem. 2012 Mar 8;55(5):2125-43

Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo.

Gasparik V, Daubeuf F, Hachet-Haas M, Rohmer F, Gizzi P, Haiech J, Galzi JL, Hibert M, Bonnet D, Frossard N

. 2012 Jan;3(1):10-4.

Identification of Nonpeptide Oxytocin Receptor Ligands by Receptor-Ligand Fingerprint Similarity Search.

Weill N, Valencia C, Gioria S, Villa P, Hibert M, Rognan D

. 2011 Jun;30(6-7):521-6.

The neutralizing ligands to the onslaught of chemokines.

Hachet-Haas M, Bonnet D, Daubeuf F, Hibert M, Haiech J, Frossard N, Galzi JL

. 2011 Mar;319:52-5.

Identification by high-throughput screening of inhibitors of Schistosomamansoni NAD(+) catabolizing enzyme.

Kuhn I, Kellenberger E, Said-Hassane F, Villa P, Rognan D, Lobstein A, Haiech J, Hibert M, Schuber F, Muller-Steffner H

Bioorg Med Chem. 2010 Nov 15;18(22):7900-10

The apelin receptor: from ligand discovery to physiological role.

De Mota N, Iturrioz X, Alvear R, Reaux A, Chartrel N, Bonnet D, Dabire H, Gerbier R, Berdeaux A, Moos F, Maigret B, Galzi JL, Hibert M, Vaudry H, Llorens-Cortes C

Regul Pept. 2010 Sep 9;164(1):26

Identification and pharmacological properties of E339-3D6, the first nonpeptidic apelin receptor agonist.

Iturrioz X, Alvear-Perez R, De Mota N, Franchet C, Guillier F, Leroux V, Dabire H, Le Jouan M, Chabane H, Gerbier R, Bonnet D, Berdeaux A, Maigret B, Galzi JL, Hibert M, Llorens-Cortes C

FASEB J. 2010 May;24(5):1506-17

Neutralizing endogenous chemokines with small molecules. Principles and potential therapeutic applications.

Galzi JL, Hachet-Haas M, Bonnet D, Daubeuf F, Lecat S, Hibert M, Haiech J, Frossard N

Pharmacol Ther. 2010 Apr;126(1):39-55

Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.

Frantz MC, Rodrigo J, Boudier L, Durroux T, Mouillac B, Hibert M

J Med Chem. 2010 Feb 25;53(4):1546-62.

Homodimerization of the death-associated protein kinase catalytic domain: development of a new small molecule fluorescent reporter.

Zimmermann M, Atmanene C, Xu Q, Fouillen L, Van Dorsselaer A, Bonnet D, Marsol C, Hibert M, Sanglier-Cianferani S, Pigault C, McNamara LK, Watterson DM, Haiech J, Kilhoffer MC

PLoS One. 2010 Nov 30;5(11):e14120.

Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration.

Valant C, Maillet E, Bourguignon JJ, Bucher B, Utard V, Galzi JL, Hibert M

J Med Chem. 2009 Oct 8;52(19):5999-6011.

Biased agonist pharmacochaperones of the AVP V2 receptor may treat congenital nephrogenic diabetes insipidus.

Jean-Alphonse F, Perkovska S, Frantz MC, Durroux T, Mejean C, Morin D, Loison S, Bonnet D, Hibert M, Mouillac B, Mendre C

J Am Soc Nephrol. 2009 Oct;20(10):2190-203

Identification of allosteric inhibitors blocking the hepatitis C virus polymerase NS5B in the RNA synthesis initiation step.

Betzi S, Eydoux C, Bussetta C, Blemont M, Leyssen P, Debarnot C, Ben-Rahou M, Haiech J, Hibert M, Gueritte F, Grierson DS, Romette JL, Guillemot JC, Neyts J, Alvarez K, Morelli X, Dutartre H, Canard B

Antiviral Res. 2009 Oct;84(1):48-59

Identification by high throughput screening of small compounds inhibiting the nucleic acid destabilization activity of the HIV-1 nucleocapsid protein.

Shvadchak V, Sanglier S, Rocle S, Villa P, Haiech J, Hibert M, Van Dorsselaer A, Mely Y, de Rocquigny H

Biochimie. 2009 Jul;91(7):916-23

Limitations in a frataxin knockdown cell model for Friedreich ataxia in a high-throughput drug screen.

Calmels N, Seznec H, Villa P, Reutenauer L, Hibert M, Haiech J, Rustin P, Koenig M, Puccio H

BMC Neurol. 2009 Aug 24;9:46.

Small neutralizing molecules to inhibit actions of the chemokine CXCL12.

Hachet-Haas M, Balabanian K, Rohmer F, Pons F, Franchet C, Lecat S, Chow KY, Dagher R, Gizzi P, Didier B, Lagane B, Kellenberger E, Bonnet D, Baleux F, Haiech J, Parmentier M, Frossard N, Arenzana-Seisdedos F, Hibert M, Galzi JL

J Biol Chem. 2008 Aug 22;283(34):23189-99