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Heidi M. Ott
Researcher at GlaxoSmithKline
Publications - 9
Citations - 3188
Heidi M. Ott is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: EZH2 & Histone methyltransferase. The author has an hindex of 7, co-authored 9 publications receiving 2796 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
EZH2 Is Required for Germinal Center Formation and Somatic EZH2 Mutations Promote Lymphoid Transformation
Wendy Béguelin,Relja Popovic,Matt Teater,Yanwen Jiang,Karen L. Bunting,Monica Rosen,Hao Shen,Shao Ning Yang,Ling Wang,Teresa Ezponda,Eva Martinez-Garcia,Haikuo Zhang,Yupeng Zheng,Sharad K. Verma,Michael T. McCabe,Heidi M. Ott,Glenn S. Van Aller,Ryan G. Kruger,Yan Liu,Charles F. McHugh,David Scott,Young Rock Chung,Neil L. Kelleher,Rita Shaknovich,Caretha L. Creasy,Randy D. Gascoyne,Kwok-Kin Wong,Leandro Cerchietti,Ross L. Levine,Omar Abdel-Wahab,Jonathan D. Licht,Olivier Elemento,Ari Melnick +32 more
TL;DR: GC B cell (GCB)-type diffuse large B cell lymphomas (DLBCLs) are mostly addicted to EZH2 but not the more differentiated activated B cell(ABC)-type DLBCLS, thus clarifying the therapeutic scope of EZh2 targeting.
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
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.
Allison Drew,Oscar Moradei,Suzanne L. Jacques,Nathalie Rioux,Ann Boriack-Sjodin,Christina J. Allain,Margaret Porter Scott,Lei Jin,Alejandra Raimondi,Jessica L. Handler,Heidi M. Ott,Ryan G. Kruger,Michael T. McCabe,Christopher J. Sneeringer,Thomas V. Riera,Gideon Shapiro,Nigel J. Waters,Lorna Helen Mitchell,Kenneth W. Duncan,Mikel P. Moyer,Robert A. Copeland,Jesse Smith,Richard Chesworth,Scott Ribich +23 more
TL;DR: EZM2302 (GSK3359088) is an inhibitor of CARM1 enzymatic activity in biochemical assays (IC50 = 6 nM) with broad selectivity against other histone methyltransferases and is a validated chemical probe suitable for further understanding the biological roleCARM1 plays in cancer and other diseases.