C
Celine Duquenne
Researcher at GlaxoSmithKline
Publications - 8
Citations - 1996
Celine Duquenne is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Histone methyltransferase & Bartoli indole synthesis. The author has an hindex of 5, co-authored 8 publications receiving 1814 citations.
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Journal ArticleDOI
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
Michael T. McCabe,Heidi M. Ott,Gopinath Ganji,Susan Korenchuk,Christine Thompson,Glenn S. Van Aller,Yan Liu,Alan P. Graves,Anthony Della Pietra,Elsie Diaz,Louis V. LaFrance,Mellinger Mark,Celine Duquenne,Xinrong Tian,Ryan G. Kruger,Charles F. McHugh,Martin Brandt,William H. Miller,Dashyant Dhanak,Sharad K. Verma,Peter J. Tummino,Caretha L. Creasy +21 more
TL;DR: GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes and markedly inhibits the growth of EzH2 mutant DLBCL xenografts in mice are demonstrated.
Journal ArticleDOI
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Sharad K. Verma,Xinrong Tian,Louis V. LaFrance,Celine Duquenne,Dominic Suarez,Kenneth A. Newlander,Stuart Paul Romeril,Joelle Lorraine Burgess,Seth W. Grant,Brackley James,Alan P. Graves,Daryl A. Scherzer,Art Shu,Christine Thompson,Heidi M. Ott,Glenn S. Van Aller,Carl A. Machutta,Elsie Diaz,Yong Jiang,Johnson Neil W,Steven D. Knight,Ryan G. Kruger,Michael T. McCabe,Dashyant Dhanak,Peter J. Tummino,Caretha L. Creasy,William H. Miller +26 more
TL;DR: This work has identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 and GSK343, which are small molecule chemical tools that would be useful to further explore the biology of EZh2.
Journal ArticleDOI
Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 2. Rational design of naphtho[1,2-d]imidazole thrombopoietin mimics.
Kevin J. Duffy,Price Alan T,Evelyne Delorme,Susan B. Dillon,Celine Duquenne,Connie L. Erickson-Miller,Leslie Giampa,Yifang Huang,Richard M. Keenan,Peter Lamb,Nannan Liu,Stephen G. Miller,Jon Rosen,Shaw Antony N,Heather Smith,Kenneth Wiggall,Lihua Zhang,Juan I. Luengo +17 more
TL;DR: The invention of a new class of naphtho[1,2-d]imidazole thrombopoietin mimics based on a pharmacophore hypothesis for small-molecule thrommethine agonists is discussed and parallel array synthesis and purification techniques allowed for the rapid exploration of structure-activity relationships.
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Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors.
Jesus R. Medina,Christopher Becker,Charles W. Blackledge,Celine Duquenne,Yanhong Feng,Seth W. Grant,Dirk A. Heerding,William Hoi Hong Li,William H. Miller,Stuart Paul Romeril,Daryl A. Scherzer,Arthur Shu,Mark A. Bobko,Antony Chadderton,Melissa Dumble,Christine M. Gardiner,Seth A. Gilbert,Qi Liu,Sridhar K. Rabindran,Valery Sudakin,Hong Xiang,Pat Brady,Nino Campobasso,Paris Ward,Jeffrey M. Axten +24 more
TL;DR: The most potent and selective inhibitors demonstrated submicromolar activity as measured by inhibition of phosphorylation of PDK1 substrates as well as antiproliferative activity against a subset of AML cell lines, demonstrating the utility of these molecules as tools to further delineate the biology ofPDK1 and the potential pharmacological uses of a PDK 1 inhibitor.
Journal ArticleDOI
Rapid synthesis of diversely functionalized 3,4,7-trisubstituted indoles
TL;DR: Two strategies were employed, highlighted by a Bartoli indole synthesis or a sequential and regioselective use of chlorosulfonyl isocyanate to install both the 3-cyano and 7-carboxamido groups.