Chun-wa Chung

Chun-wa Chung

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Chun-wa Chung

Chun-wa Chung

Publications by authors named "Chun-wa Chung"

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71Publications

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Single-Domain Antibodies as Crystallization Chaperones to Enable Structure-Based Inhibitor Development for RBR E3 Ubiquitin Ligases.

Cell Chem Biol 2020 Jan 5;27(1):83-93.e9. Epub 2019 Dec 5.

Molecular Structure of Cell Signalling Laboratory, The Francis Crick Institute, 1 Midland Road, London NW1 1AT, UK. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2019.11.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6963773PMC
January 2020

Cryo-EM in drug discovery.

Biochem Soc Trans 2019 02 15;47(1):281-293. Epub 2019 Jan 15.

Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, U.K.

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http://dx.doi.org/10.1042/BST20180267DOI Listing
February 2019

Fragment-Based Covalent Ligand Screening Enables Rapid Discovery of Inhibitors for the RBR E3 Ubiquitin Ligase HOIP.

J Am Chem Soc 2019 02 4;141(6):2703-2712. Epub 2019 Feb 4.

Molecular Structure of Cell Signalling Laboratory , The Francis Crick Institute , 1 Midland Road , London NW1 1AT , United Kingdom.

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http://dx.doi.org/10.1021/jacs.8b13193DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6383986PMC
February 2019

Correction: Cryo-EM in drug discovery.

Biochem Soc Trans 2019 02;47(1):487

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http://dx.doi.org/10.1042/BST-2018-0267C_CORDOI Listing
February 2019

Integration of Lead Discovery Tactics and the Evolution of the Lead Discovery Toolbox.

SLAS Discov 2018 10 6;23(9):881-897. Epub 2018 Jun 6.

1 GlaxoSmithKline Drug Design and Selection, Platform Technology and Science, Stevenage, Hertfordshire, UK.

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http://journals.sagepub.com/doi/10.1177/2472555218778503
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http://dx.doi.org/10.1177/2472555218778503DOI Listing
October 2018

Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.

J Med Chem 2018 09 18;61(18):8321-8336. Epub 2018 Sep 18.

Molecular Discovery Research, Cellzome GmbH , GlaxoSmithKline , Meyerhofstrasse 1 , 69117 Heidelberg , Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.8b00862DOI Listing
September 2018

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.

J Med Chem 2018 05 3;61(10):4317-4334. Epub 2018 May 3.

WestCHEM, Department of Pure and Applied Chemistry , University of Strathclyde, Thomas Graham Building , 295 Cathedral Street , Glasgow , G1 1XL , U.K.

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http://dx.doi.org/10.1021/acs.jmedchem.7b01666DOI Listing
May 2018

Pac13 is a Small, Monomeric Dehydratase that Mediates the Formation of the 3'-Deoxy Nucleoside of Pacidamycins.

Angew Chem Int Ed Engl 2017 10 30;56(41):12492-12497. Epub 2017 Aug 30.

School of Chemistry, University of St Andrews, North Haugh, St Andrews, Fife, KY16 9ST, UK.

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http://dx.doi.org/10.1002/anie.201705639DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5656905PMC
October 2017

Structural and Functional Basis of C-Methylation of Coumarin Scaffolds by NovO.

ACS Chem Biol 2017 02 13;12(2):374-379. Epub 2017 Jan 13.

GlaxoSmithKline Medicines Research Centre , Gunnels Wood Road, Stevenage, SG1 2NY , United Kingdom.

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http://dx.doi.org/10.1021/acschembio.6b01053DOI Listing
February 2017

Getting the chemistry right: protonation, tautomers and the importance of H atoms in biological chemistry.

Acta Crystallogr D Struct Biol 2017 02 1;73(Pt 2):131-140. Epub 2017 Feb 1.

Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, England.

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http://dx.doi.org/10.1107/S2059798316020283DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5297916PMC
February 2017

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.

J Med Chem 2017 01 9;60(2):695-709. Epub 2017 Jan 9.

WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde , Thomas Graham Building, 295 Cathedral Street, Glasgow, G1 1XL, United Kingdom.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01566DOI Listing
January 2017

Biophysics in drug discovery: impact, challenges and opportunities.

Nat Rev Drug Discov 2016 10 12;15(10):679-98. Epub 2016 Aug 12.

Boehringer Ingelheim GmbH &Co. KG, Birkendorfer Strasse 65, 88400 Biberach, Germany.

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http://dx.doi.org/10.1038/nrd.2016.123DOI Listing
October 2016

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.

ACS Med Chem Lett 2016 Jun 9;7(6):552-7. Epub 2016 May 9.

Epinova Discovery Performance Unit, Quantitative Pharmacology, Experimental Medicine Unit, Flexible Discovery Unit, and Platform Technology and Science, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00092DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4904261PMC
June 2016

Autism-like syndrome is induced by pharmacological suppression of BET proteins in young mice.

J Exp Med 2015 Oct 21;212(11):1771-81. Epub 2015 Sep 21.

Department of Neuroscience and Department of Psychiatry, Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029 Department of Neuroscience and Department of Psychiatry, Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029

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http://dx.doi.org/10.1084/jem.20151271DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4612093PMC
October 2015

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

Nat Chem Biol 2015 Mar 26;11(3):189-91. Epub 2015 Jan 26.

1] EpiNova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline,Medicines Research Centre, Stevenage, Hertfordshire, UK. [2] AstraZeneca, Oncology iMed, Cambridge Science Park, Cambridge, UK (R.J.S. and D.M.W.); Virginia Polytechnic Institute and State University, Blacksburg, Virginia, USA (D.J.S.); University of Massachussetts Medical School, Worcester, Massachusetts, USA (P.R.T.).

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http://dx.doi.org/10.1038/nchembio.1735DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4397581PMC
March 2015

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.

ACS Med Chem Lett 2014 Nov 10;5(11):1190-5. Epub 2014 Sep 10.

Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

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http://dx.doi.org/10.1021/ml5002932DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4233354PMC
November 2014

Naphthyridines as novel BET family bromodomain inhibitors.

ChemMedChem 2014 Mar 2;9(3):580-9. Epub 2013 Sep 2.

Centre de Recherches François Hyafil, GlaxoSmithKline R&D, 25 Avenue du Québec, 91140 Villebon-sur-Yvette (France); Current address: Institut de Recherches Servier, 11 Rue des Moulineaux, 92150 Suresnes (France).

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http://dx.doi.org/10.1002/cmdc.201300259DOI Listing
March 2014

Small molecule bromodomain inhibitors: extending the druggable genome.

Authors:
Chun-Wa Chung

Prog Med Chem 2012 ;51:1-55

Computational and Structural Sciences, GlaxoSmithKline R&D, Stevenage, SG1 2NY, UK.

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http://dx.doi.org/10.1016/B978-0-12-396493-9.00001-7DOI Listing
August 2012

Enabling lead discovery for histone lysine demethylases by high-throughput RapidFire mass spectrometry.

J Biomol Screen 2012 Jan 21;17(1):39-48. Epub 2011 Aug 21.

Departments of Biological Reagents and Assay Development, Platform Technology and Science, GlaxoSmithKline,Stevenage, SG1 2NY, UK.

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http://dx.doi.org/10.1177/1087057111416660DOI Listing
January 2012

Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.

J Med Chem 2012 Jan 11;55(2):576-86. Epub 2012 Jan 11.

Computational & Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.

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http://dx.doi.org/10.1021/jm201320wDOI Listing
January 2012

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

J Med Chem 2012 Jan 11;55(2):587-96. Epub 2012 Jan 11.

Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.

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http://pubs.acs.org/doi/10.1021/jm201283q
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http://dx.doi.org/10.1021/jm201283qDOI Listing
January 2012

Progress in the discovery of small-molecule inhibitors of bromodomain--histone interactions.

J Biomol Screen 2011 Dec 28;16(10):1170-85. Epub 2011 Sep 28.

PTS, GlaxoSmithKline R&D, Stevenage, UK.

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http://dx.doi.org/10.1177/1087057111421372DOI Listing
December 2011

Selectivity of kinase inhibitor fragments.

J Med Chem 2011 Jul 23;54(14):5131-43. Epub 2011 Jun 23.

GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK.

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http://dx.doi.org/10.1021/jm200349bDOI Listing
July 2011

Structural basis of binding of fluorescent, site-specific dansylated amino acids to human serum albumin.

J Struct Biol 2011 Apr 19;174(1):84-91. Epub 2010 Oct 19.

Biophysics Section, Blackett Laboratory, Imperial College, Exhibition Road, London SW7 2AZ, United Kingdom.

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http://dx.doi.org/10.1016/j.jsb.2010.10.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3073228PMC
April 2011

Crystallographic analysis reveals the structural basis of the high-affinity binding of iophenoxic acid to human serum albumin.

BMC Struct Biol 2011 Apr 18;11:18. Epub 2011 Apr 18.

Biophysics Section, Blackett Laboratory, Imperial College, Exhibition Road, London, SW7 2AZ, UK.

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http://dx.doi.org/10.1186/1472-6807-11-18DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3104944PMC
April 2011

Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.

Bioorg Med Chem Lett 2008 Aug 12;18(15):4433-7. Epub 2008 Jun 12.

GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.

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http://dx.doi.org/10.1016/j.bmcl.2008.06.028DOI Listing
August 2008

The use of biophysical methods increases success in obtaining liganded crystal structures.

Authors:
Chun-wa Chung

Acta Crystallogr D Biol Crystallogr 2007 Jan 13;63(Pt 1):62-71. Epub 2006 Dec 13.

Structural and Biophysical Sciences, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnelswood Road, Stevenage SG1 2NY, England.

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http://dx.doi.org/10.1107/S0907444906051869DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2483471PMC
January 2007

Human macrophage migration inhibitory factor: a proven immunomodulatory cytokine?

J Biol Chem 2006 Oct 7;281(40):29641-51. Epub 2006 Aug 7.

Department of Disease Biology, Rheumatology, and Inflammation and Discovery Research, GlaxoSmithKline, Stevenage SG1 2NY, United Kingdom.

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http://dx.doi.org/10.1074/jbc.M601103200DOI Listing
October 2006

Effect of detergent on "promiscuous" inhibitors.

J Med Chem 2003 Jul;46(16):3448-51

Computational and Structural Sciences, GlaxoSmithKline, Gunnels Wood Road, Stevenage, SG1 2NY, UK.

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http://dx.doi.org/10.1021/jm0340896DOI Listing
July 2003