O
Onkar M. P. Singh
Researcher at GlaxoSmithKline
Publications - 23
Citations - 1486
Onkar M. P. Singh is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: DNA gyrase & Ligand (biochemistry). The author has an hindex of 16, co-authored 23 publications receiving 1293 citations.
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Journal ArticleDOI
Type IIA topoisomerase inhibition by a new class of antibacterial agents.
Benjamin D. Bax,Pan F. Chan,Drake S. Eggleston,Drake S. Eggleston,Andrew P. Fosberry,Daniel R. Gentry,Fabrice Gorrec,Fabrice Gorrec,Ilaria Giordano,Michael M. Hann,Alan Joseph Hennessy,Martin Hibbs,Jianzhong Huang,Emma J. Jones,Jo J. Jones,Kristin K. Brown,Ceri J. Lewis,Earl May,Earl May,Martin R. Saunders,Onkar M. P. Singh,Claus Spitzfaden,Carol Shen,Anthony Shillings,Andrew J. Theobald,Alexandre Wohlkonig,Alexandre Wohlkonig,Neil D. Pearson,Michael N. Gwynn +28 more
TL;DR: This work provides new insights into the mechanism of topoisomerase action and a platform for structure-based drug design of a new class of antibacterial agents against a clinically proven, but conformationally flexible, enzyme class.
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The high-resolution crystal structure of a 24-kDa gyrase B fragment from E. coli complexed with one of the most potent coumarin inhibitors, clorobiocin
Francis T. F. Tsai,Onkar M. P. Singh,Tadeusz Skarzynski,Alan J. Wonacott,Simon A. Weston,Alec Tucker,Richard A. Pauptit,Alexander L. Breeze,J. Philip Poyser,Ronan O'Brien,John E. Ladbury,Dale B. Wigley +11 more
TL;DR: To understand the difference in affinity, the crystal structure of the 24‐kDa GyrB fragment in complex with clorobiocin was determined to high resolution and the results from isothermal titration calorimetry are presented.
Journal ArticleDOI
Optimization of Novel Acyl Pyrrolidine Inhibitors of Hepatitis C Virus RNA-Dependent RNA Polymerase Leading to a Development Candidate
Martin John Slater,E.M. Amphlett,David M. Andrews,G. Bravi,George Burton,Anne Cheasty,John Andrew Corfield,Malcolm Ellis,R. Fenwick,S. Fernandes,R. Guidetti,David Haigh,C.D. Hartley,Peter David Howes,Deborah Lynette Jackson,Richard L. Jarvest,V.L.H. Lovegrove,K.J. Medhurst,Nigel R. Parry,Helen Susanne Price,P. Shah,Onkar M. P. Singh,Richard Stocker,Pia Thommes,C. Wilkinson,Alan J. Wonacott +25 more
TL;DR: Optimization of a pyrrolidine-based template using structure-based design and physicochemical considerations has provided a development candidate 20b with submicromolar potency in the HCV replicon and good pharmacokinetic properties.
Journal ArticleDOI
Crystallizing Membrane Proteins in the Lipidic Mesophase. Experience with Human Prostaglandin E2 Synthase 1 and an Evolving Strategy.
Dianfan Li,Nicole Howe,Abhiram Dukkipati,Syed T. A. Shah,Benjamin D. Bax,Colin M. Edge,Angela Bridges,Phil Hardwicke,Onkar M. P. Singh,Ged Giblin,Alexander Pautsch,Roland Pfau,Gisela Schnapp,Meitian Wang,Vincent Olieric,Martin Caffrey +15 more
TL;DR: The crystallization strategy detailed here should prove useful for generating structures of other integral membrane proteins by the in meso method, especially with a new target type of α-helical microsomal prostaglandin E2 synthase 1.
Journal ArticleDOI
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxohexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 2. Potency and chirality.
Alan D. Borthwick,Andrew J Crame,Peter Franz Ertl,Anne M. Exall,Terry M. Haley,Graham J Hart,Andrew M. Mason,Andrew M K Pennell,Onkar M. P. Singh,Gordon G. Weingarten,James Michael Woolven +10 more
TL;DR: The crystal structure of HCMV protease was obtained and used to model the conformationally restricted, chiral (S)-proline-alpha-methyl-5,5-trans-lactams into the active site groove of the enzyme, enabling us to direct and rationalize the SAR in this series.