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Items: 10


Establishing Drug Discovery and Identification of Hit Series for the Anti-apoptotic Proteins, Bcl-2 and Mcl-1.

Murray JB, Davidson J, Chen I, Davis B, Dokurno P, Graham CJ, Harris R, Jordan A, Matassova N, Pedder C, Ray S, Roughley SD, Smith J, Walmsley C, Wang Y, Whitehead N, Williamson DS, Casara P, Le Diguarher T, Hickman J, Stark J, Kotschy A, Geneste O, Hubbard RE.

ACS Omega. 2019 May 23;4(5):8892-8906. doi: 10.1021/acsomega.9b00611. eCollection 2019 May 31.


S29434, a Quinone Reductase 2 Inhibitor: Main Biochemical and Cellular Characterization.

Boutin JA, Bouillaud F, Janda E, Gacsalyi I, Guillaumet G, Hirsch EC, Kane DA, Nepveu F, Reybier K, Dupuis P, Bertrand M, Chhour M, Le Diguarher T, Antoine M, Brebner K, Da Costa H, Ducrot P, Giganti A, Goswami V, Guedouari H, Michel PP, Patel A, Paysant J, Stojko J, Viaud-Massuard MC, Ferry G.

Mol Pharmacol. 2019 Mar;95(3):269-285. doi: 10.1124/mol.118.114231. Epub 2018 Dec 19.


S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth.

Casara P, Davidson J, Claperon A, Le Toumelin-Braizat G, Vogler M, Bruno A, Chanrion M, Lysiak-Auvity G, Le Diguarher T, Starck JB, Chen I, Whitehead N, Graham C, Matassova N, Dokurno P, Pedder C, Wang Y, Qiu S, Girard AM, Schneider E, Gravé F, Studeny A, Guasconi G, Rocchetti F, Maïga S, Henlin JM, Colland F, Kraus-Berthier L, Le Gouill S, Dyer MJS, Hubbard R, Wood M, Amiot M, Cohen GM, Hickman JA, Morris E, Murray J, Geneste O.

Oncotarget. 2018 Apr 13;9(28):20075-20088. doi: 10.18632/oncotarget.24744. eCollection 2018 Apr 13.


Bax activation by engagement with, then release from, the BH3 binding site of Bcl-xL.

Gautier F, Guillemin Y, Cartron PF, Gallenne T, Cauquil N, Le Diguarher T, Casara P, Vallette FM, Manon S, Hickman JA, Geneste O, Juin P.

Mol Cell Biol. 2011 Feb;31(4):832-44. doi: 10.1128/MCB.00161-10. Epub 2010 Dec 20.


Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.

Le Diguarher T, Ortuno JC, Shanks D, Guilbaud N, Pierré A, Raimbaud E, Fauchère JL, Hickman JA, Tucker GC, Casara PJ.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):767-71.


Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.

Le Diguarher T, Chollet AM, Bertrand M, Hennig P, Raimbaud E, Sabatini M, Guilbaud N, Pierré A, Tucker GC, Casara P.

J Med Chem. 2003 Aug 28;46(18):3840-52.


Parallel liquid synthesis of N,N'-Disubstituted 3-amino azepin-2-ones as potent and specific farnesyl transferase inhibitors.

Le Diguarher T, Ortuno JC, Dorey G, Shanks D, Guilbaud N, Pierré A, Fauchère JL, Hickman JA, Tucker GC, Casara PJ.

Bioorg Med Chem. 2003 Jul 17;11(14):3193-204.


Solid-phase synthesis of alpha-substituted 3-bisarylthio N-hydroxy propionamides as specific MMP inhibitors.

Chollet AM, Le Diguarher T, Kucharczyk N, Loynel A, Bertrand M, Tucker G, Guilbaud N, Burbridge M, Pastoureau P, Fradin A, Sabatini M, Fauchère JL, Casara P.

Bioorg Med Chem. 2002 Mar;10(3):531-44.


General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.

Chollet AM, Le Diguarher T, Murray L, Bertrand M, Tucker GC, Sabatini M, Pierré A, Atassi G, Bonnet J, Casara P.

Bioorg Med Chem Lett. 2001 Feb 12;11(3):295-9.


Synthesis and physicochemical properties of oligonucleotides built with either alpha-L or beta-L nucleotides units and covalently linked to an acridine derivative.

Asseline U, Hau JF, Czernecki S, Le Diguarher T, Perlat MC, Valery JM, Thuong NT.

Nucleic Acids Res. 1991 Aug 11;19(15):4067-74.

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