G
Gaëlle Lysiak-Auvity
Publications - 4
Citations - 910
Gaëlle Lysiak-Auvity is an academic researcher. The author has contributed to research in topics: Leukemia & Cell killing. The author has an hindex of 4, co-authored 4 publications receiving 693 citations.
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Journal ArticleDOI
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models
András Kotschy,Szlávik Zoltán,James A. H. Murray,James Edward Paul Davidson,Ana Leticia Maragno,Gaëtane Le Toumelin-Braizat,Maïa Chanrion,Gemma L. Kelly,Gemma L. Kelly,Jia-Nan Gong,Jia-Nan Gong,Donia M Moujalled,Alain Bruno,Csékei Márton,Attila Paczal,Zoltán B. Szabó,Szabolcs Sipos,Gabor Radics,Proszenyák Ágnes,Balázs Bálint,Levente Ondi,Gábor Blasko,Alan P. Robertson,Allan E. Surgenor,Pawel Dokurno,Chen I-Jen,Natalia Matassova,Julia Smith,C. Pedder,Chris Graham,Aurélie Studeny,Gaëlle Lysiak-Auvity,Anne-Marie Girard,Fabienne Gravé,David J. Segal,David J. Segal,Chris D. Riffkin,Chris D. Riffkin,Giovanna Pomilio,Laura C. A. Galbraith,Laura C. A. Galbraith,Brandon J. Aubrey,Brandon J. Aubrey,Brandon J. Aubrey,Margs S. Brennan,Margs S. Brennan,Marco J Herold,Marco J Herold,Catherine Chang,Catherine Chang,Ghislaine Guasconi,Nicolas Cauquil,Fabien Melchiore,Nolwen Guigal-Stephan,Brian Lockhart,Frédéric Colland,John A. Hickman,Andrew W. Roberts,David C.S. Huang,David C.S. Huang,Andrew H. Wei,Andrew H. Wei,Andreas Strasser,Andreas Strasser,Guillaume Lessene,Guillaume Lessene,Olivier Geneste +66 more
TL;DR: It is demonstrated that S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway.
ComponentDOI
S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth.
P. Casara,James Edward Paul Davidson,Audrey Claperon,G. Le Toumelin-Braizat,Meike Vogler,Alain Bruno,Maïa Chanrion,Gaëlle Lysiak-Auvity,T. Le Diguarher,J.-B. Starck,Chen I-Jen,Neil Whitehead,Chris Graham,Natalia Matassova,Pawel Dokurno,C. Pedder,Y. Wang,Shumei Qiu,Anne-Marie Girard,E. Schneider,F. Gravé,Aurélie Studeny,Ghislaine Guasconi,Francesca Rocchetti,Sophie Maïga,J.-M. Henlin,Frédéric Colland,Laurence Kraus-Berthier,S. Le Gouill,Martin J. S. Dyer,Roderick E. Hubbard,Michael Wood,Martine Amiot,Gerald M. Cohen,J. Hickman,Erick Morris,James Murray,Olivier Geneste +37 more
TL;DR: S55746 administered by oral route daily in mice demonstrated robust anti-tumor efficacy in two hematological xenograft models with no weight lost and no change in behavior, demonstrating that S55746 is a novel, well-tolerated BH3-mimetic targeting selectively and potently the BCL-2 protein.
Journal ArticleDOI
Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor
Szlávik Zoltán,Csékei Márton,Attila Paczal,Zoltán B. Szabó,Szabolcs Sipos,Gabor Radics,Proszenyák Ágnes,Balázs Bálint,James Murray,James Edward Paul Davidson,Chen I-Jen,Pawel Dokurno,Allan E. Surgenor,Zoe Daniels,Roderick E. Hubbard,Gaëtane Le Toumelin-Braizat,Audrey Claperon,Gaëlle Lysiak-Auvity,Anne-Marie Girard,Alain Bruno,Maïa Chanrion,Frédéric Colland,Ana-Leticia Maragno,Didier Demarles,Olivier Geneste,András Kotschy +25 more
TL;DR: The discovery of the clinical candidate S64315 is reported, a selective small molecule inhibitor of Mcl-1, a antiapoptotic member of the Bcl-2 family of proteins, whose upregulation in human cancers is associated with high tumor grade, poor survival, and resistance to chemotherapy.
Proceedings ArticleDOI
Abstract 4482: S64315 (MIK665) is a potent and selective Mcl1 inhibitor with strong antitumor activity across a diverse range of hematologic tumor models
Ana Leticia Maragno,Prakash Mistry,András Kotschy,Szlávik Zoltán,James Murray,James Edward Paul Davidson,Gaëtane Le Toumelin-Braizat,Maïa Chanrion,Alain Bruno,Audrey Clapéron,Heiko Maacke,Erick Morris,Youzhen Wang,Alix Derreal,Csékei Márton,Attila Paczal,Zoltán B. Szabó,Szabolcs Sipos,Proszenyák Ágnes,Balázs Bálint,Allan E. Surgenor,Pawel Dokurno,Natalia Matassova,Chen I-Jen,Gaëlle Lysiak-Auvity,Anne-Marie Girard,Fabienne Grave,Frédéric Colland,Ensar Halilovic,Olivier Geneste +29 more
TL;DR: A fragment-based, structure-guided drug discovery effort led to the identification of S64315/MIK665 that binds to human Mcl-1 with a sub-nanomolar affinity and selectively over other anti-apoptotic Bcl-2 family members and shows strong cell killing activity in a diverse panel of human hematological tumor cell lines.