S
Stuart Paul Romeril
Researcher at GlaxoSmithKline
Publications - 21
Citations - 1665
Stuart Paul Romeril is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Absolute configuration & Cancer. The author has an hindex of 10, co-authored 21 publications receiving 1429 citations. Previous affiliations of Stuart Paul Romeril include University of Oxford & Harvard University.
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Journal ArticleDOI
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Jeffrey M. Axten,Jesus R. Medina,Yanhong Feng,Arthur Shu,Stuart Paul Romeril,Seth W. Grant,William Hoi Hong Li,Dirk A. Heerding,Elisabeth A. Minthorn,Thomas Mencken,Charity Atkins,Qi Liu,Sridhar K. Rabindran,Rakesh Kumar,Xuan Hong,Aaron S. Goetz,Thomas B. Stanley,J. David Taylor,Scott D Sigethy,Ginger H. Tomberlin,Annie M. Hassell,Kirsten M. Kahler,Lisa M. Shewchuk,Robert T. Gampe +23 more
TL;DR: Through screening and lead optimization using the human PERK crystal structure, compound 38 (GSK2606414), an orally available, potent, and selective PERK inhibitor is discovered, which inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice.
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On the Mechanism of the Palladium(II)-Catalyzed Decarboxylative Olefination of Arene Carboxylic Acids. Crystallographic Characterization of Non-Phosphine Palladium(II) Intermediates and Observation of Their Stepwise Transformation in Heck-like Processes
TL;DR: There are notable differences in reactivity between arylpalladium(II) intermediates generated by decarboxylative palladation and those produced in conventional Heck reactions, and it is found that more electron-rich alkenes react preferentially with an aryl group and trifluoroacetate intermediate formed by decarate palladium-based reactions, whereas an opposite trend is found inventional Heck reactions.
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
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development
Jeffrey M. Axten,Stuart Paul Romeril,Arthur Shu,Jeffrey M. Ralph,Jesus R. Medina,Yanhong Feng,William Hoi Hong Li,Seth W. Grant,Dirk A. Heerding,Elisabeth A. Minthorn,Thomas Mencken,Nathan Gaul,Aaron S. Goetz,Thomas B. Stanley,A.M. Hassell,Robert T. Gampe,Charity Atkins,Rakesh Kumar +17 more
TL;DR: In continuation of the drug discovery program, a strategy to decrease inhibitor lipophilicity is applied as a means to improve physical properties and pharmacokinetics and is selected for advancement to preclinical development.
Journal ArticleDOI
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Melissa B. Pappalardi,Kathryn Keenan,Mark Cockerill,Wendy A. Kellner,Alexandra Stowell,Christian S. Sherk,Kristen Wong,Sarath Pathuri,Jacques Briand,Michael Steidel,Phil Chapman,Arthur Groy,Ashley K. Wiseman,Charles F. McHugh,Nino Campobasso,Alan P. Graves,Emma E. Fairweather,Thilo Werner,Ali Raoof,Roger J. Butlin,Lourdes Rueda,John R. Horton,David T. Fosbenner,Cunyu Zhang,Jessica L. Handler,Morris Muliaditan,Makda Mebrahtu,Jon Paul Jaworski,Dean E. McNulty,Charlotte Burt,H. Christian Eberl,Amy N. Taylor,Thau F. Ho,Susan Merrihew,Shawn W. Foley,Anna Rutkowska,Mei Li,Stuart Paul Romeril,Kristin M. Goldberg,Xing Zhang,Christopher S. Kershaw,Marcus Bantscheff,Anthony J. Jurewicz,Elisabeth A. Minthorn,Paola Grandi,Mehul Patel,Andrew B. Benowitz,Helai P. Mohammad,Aidan G. Gilmartin,Rab K. Prinjha,Donald J. Ogilvie,Christopher L. Carpenter,Dirk A. Heerding,Stephen B. Baylin,Peter A. Jones,Xiaodong Cheng,Bryan W. King,Juan I. Luengo,Allan M. Jordan,Ian D. Waddell,Ryan G. Kruger,Michael T. McCabe +61 more
TL;DR: The discovery of GSK3685032 is reported, a potent first-in-class DNMT1-selective inhibitor that was shown via crystallographic studies to compete with the active-site loop ofDNMT1 for penetration into hemi-methylated DNA between two CpG base pairs.