E
Elsie Diaz
Researcher at GlaxoSmithKline
Publications - 12
Citations - 2669
Elsie Diaz is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: EZH2 & Histone H3. The author has an hindex of 7, co-authored 11 publications receiving 2386 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
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)
Michael T. McCabe,Alan P. Graves,Gopinath Ganji,Elsie Diaz,Wendy S. Halsey,Yong Jiang,Kimberly N. Smitheman,Heidi M. Ott,Melissa B. Pappalardi,Kimberly E. Allen,Stephanie Chen,Anthony Della Pietra,Edward Dul,Ashley M. Hughes,Seth A. Gilbert,Sara H. Thrall,Peter J. Tummino,Ryan G. Kruger,Martin Brandt,Benjamin J. Schwartz,Caretha L. Creasy +20 more
TL;DR: This mutation highlights the interplay between Y641 and A677 residues in the substrate specificity of EZH2 and identifies another lymphoma patient population that harbors an activating mutation of EzH2.
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
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
Aidan G. Gilmartin,Faitg Thomas H,Mark Richter,Arthur Groy,Mark A. Seefeld,Michael G. Darcy,Peng Xin,Kelly Federowicz,Jingsong Yang,Shu-Yun Zhang,Elisabeth A. Minthorn,Jon-Paul Jaworski,Michael D. Schaber,Stan F. Martens,Dean E. McNulty,Robert H. Sinnamon,Hong Zhang,Robert B. Kirkpatrick,Neysa Nevins,Guanglei Cui,Beth Pietrak,Elsie Diaz,Amber D. Jones,Martin Brandt,Benjamin Schwartz,Dirk A. Heerding,Rakesh Kumar +26 more
TL;DR: GSK2830371 is the first orally active, allosteric inhibitor of Wip1 phosphatase, an oncogenic phosphat enzyme common to multiple cancers and results in expected pharmacodynamic effects and causes inhibition of lymphoma xenograft growth.
Journal ArticleDOI
A Simple Assay for Detection of Small-Molecule Redox Activity
Leng A. Lor,Jessica L. Schneck,Dean E. McNulty,Elsie Diaz,Martin Brandt,Sara H. Thrall,Benjamin K. Schwartz +6 more
TL;DR: Direct proof of small-molecule oxidation of a cysteine protease by liquid chromatography/tandem mass spectrometry is described, a simple assay is developed to predict this oxidizing behavior by compounds, and the utility of this assay is shown by demonstrating its ability to distinguish nuisance redox compounds from well-behaved inhibitors in 3 historical GlaxoSmithKline drug discovery efforts.