R
Ryan G. Kruger
Researcher at GlaxoSmithKline
Publications - 62
Citations - 7484
Ryan G. Kruger is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Histone methyltransferase & EZH2. The author has an hindex of 32, co-authored 61 publications receiving 6265 citations. Previous affiliations of Ryan G. Kruger include University of Pennsylvania.
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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
The promise and peril of chemical probes.
Cheryl H. Arrowsmith,James E. Audia,Christopher M. Austin,Jonathan B. Baell,Jonathan Bennett,Julian Blagg,C. Bountra,Paul Brennan,Peter Brown,Mark E. Bunnage,Carolyn Buser-Doepner,Robert M. Campbell,Adrian Carter,Philip Cohen,Robert A. Copeland,Ben Cravatt,Jayme L. Dahlin,Dashyant Dhanak,Aled M. Edwards,Mathias Frederiksen,Stephen V. Frye,Nathanael S. Gray,Charles E. Grimshaw,David Hepworth,Trevor Howe,Kilian Huber,Jian Jin,Stefan Knapp,Joanne Kotz,Ryan G. Kruger,Derek B. Lowe,Mary M. Mader,Brian D. Marsden,Anke Mueller-Fahrnow,Susanne Müller,Ronan C. O'Hagan,John P. Overington,Dafydd R. Owen,Saul H Rosenberg,Bryan L. Roth,Ruth A. Ross,Matthieu Schapira,Stuart L. Schreiber,Brian K. Shoichet,Michael Sundström,Giulio Superti-Furga,Jack Taunton,Leticia Toledo-Sherman,Chris Walpole,Michael A. Walters,Timothy M. Willson,Paul Workman,Robert N. Young,William J. Zuercher +53 more
TL;DR: A community-driven wiki resource to improve quality and convey current best practice on chemical probes, and to help address shortcomings of poor quality or that are used incorrectly generate misleading results.
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
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
Elayne Chan-Penebre,Kristy G Kuplast,Christina R. Majer,P. Ann Boriack-Sjodin,Tim J. Wigle,L. Danielle Johnston,Nathalie Rioux,Michael John Munchhof,Lei Jin,Suzanne L. Jacques,Kip A West,Trupti Lingaraj,Kimberly Stickland,Scott Ribich,Alejandra Raimondi,Margaret Porter Scott,Nigel J. Waters,Roy M. Pollock,J. Joshua Smith,Olena Barbash,Melissa B. Pappalardi,Thau F. Ho,Kelvin Nurse,Khyati P Oza,Kathleen T. Gallagher,Ryan G. Kruger,Mikel P. Moyer,Robert A. Copeland,Richard Chesworth,Kenneth W. Duncan +29 more
TL;DR: EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity in biochemical assays with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases.