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Dive into the research topics where David Kendall Jung is active.

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Featured researches published by David Kendall Jung.


Journal of Medicinal Chemistry | 2016

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B

Peiling Chen; A. Chaikuad; Paul Bamborough; Marcus Bantscheff; C. Bountra; Chun Wa Chung; Oleg Fedorov; Paola Grandi; David Kendall Jung; Robert Lesniak; Matthew J Lindon; Susanne Müller; Martin Philpott; Rab K. Prinjha; Catherine Rogers; Carolyn Selenski; Cynthia Tallant; Thilo Werner; Timothy M. Willson; Stefan Knapp; David H. Drewry

Bromodomains are acetyl-lysine specific protein interaction domains that have recently emerged as a new target class for the development of inhibitors that modulate gene transcription. The two closely related bromodomain containing proteins BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. However, BAZ2 bromodomains have low predicted druggability and so far no selective inhibitors have been published. Here we report the development of GSK2801, a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains as well as the inactive control compound GSK8573. GSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively. Crystal structures demonstrated a canonical acetyl-lysine competitive binding mode. Cellular activity was demonstrated using fluorescent recovery after photobleaching (FRAP) monitoring displacement of GFP-BAZ2A from acetylated chromatin. A pharmacokinetic study in mice showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. Thus, GSK2801 represents a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.


Archive | 2001

Fused pyrazole derivatives bieng protein kinase inhibitors

Michael John Alberti; Ian Robert Baldwin; Mui Cheung; Stuart Cockerill; Philip A. Harris; David Kendall Jung; Gregory Peckham; Michael Robert Peel; Jennifer Gabriel Badiang; Kirk L. Stevens; James Marvin Veal


Archive | 2005

Benzamide compounds useful as rock inhibitors

David Kendall Drewry; David Kendall Jung; James Andrew Linn; Robert Neil Hunter; Dennis Lee; Robert A. Stavenger; Clark A. Sehon


Archive | 2003

Benzimidazoles and their use as mitogen-activated- and rho-kinase inhibitors

Michael John Alberti; Stephen GlaxoSmithKline Pharm. Garland; David Kendall Jung; James Marvin Veal; Jason GlaxoSmithKline Witherington


Archive | 2005

Pyrazolopyridines, process for their preparation and use as therapeutic compounds

Michael John Alberti; Stanley D. Chamberlain; Mui Cheung; Kristjan Gudmundsson; Philip A. Harris; Brian A. Johns; David Kendall Jung; Michael Robert Peel; Jennifer Badiang Stanford


Archive | 2006

PYRIDOPYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USES AS ANTI-CANCER AND ANTI-DIABETE DRUGS

David Kendall Jung; Michael John Alberti


Archive | 2004

Indazolo-tetrahydropyrimidine-carboxamide derivative kinase inhibitors

David H. Drewry; Brian L. Evans; Krista B. Goodman; Darren Victor Steven Green; David Kendall Jung; Dennis Lee; Robert A. Stavenger; Sjoerd Nocolaas Wadman


Archive | 2005

Benzodiazepine derivatives that inhibit rock

Michael John GlaxoSmithKline Alberti; David Kendall Jung


Archive | 2005

Benzodiazepine derivatives as ROCK kinases inhibitors

Michael John GlaxoSmithKline Alberti; David Kendall Jung


Archive | 2001

Pyrazolopyridinderivate Pyrazolopyridine derivatives

F. Leslie Boyd; Stanley D. Chamberlain; Mui Cheung; Kristjan Gudmundsson; Philip A. Harris; Brian A. Johns; David Kendall Jung; Michael Robert Peel; Jo Connie Sexton; G. Jennifer Stanford

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David H. Drewry

University of North Carolina at Chapel Hill

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