Rab K Prinjha

Rab K Prinjha

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Rab K Prinjha

Rab K Prinjha

Publications by authors named "Rab K Prinjha"

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Bromodomain inhibitor I-BET151 suppresses immune responses during fungal-immune interaction.

Eur J Immunol 2019 Jun 17. Epub 2019 Jun 17.

Department of Internal Medicine and Radboud Center for Infectious diseases (RCI), Radboud University Nijmegen Medical Centre, 6500HB, Nijmegen, the Netherlands.

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http://dx.doi.org/10.1002/eji.201848081DOI Listing
June 2019

Advancements in the Development of non-BET Bromodomain Chemical Probes.

ChemMedChem 2019 Feb 4;14(4):362-385. Epub 2019 Feb 4.

Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire, SG1 2NY, UK.

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http://doi.wiley.com/10.1002/cmdc.201800738
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http://dx.doi.org/10.1002/cmdc.201800738DOI Listing
February 2019

BET Inhibition Improves NASH and Liver Fibrosis.

Sci Rep 2018 Nov 22;8(1):17257. Epub 2018 Nov 22.

Computational Biology, GSK, 1250 S. Collegeville Road, UP12-100, Collegeville, PA, 19426-0989, USA.

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http://dx.doi.org/10.1038/s41598-018-35653-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6250695PMC
November 2018

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.

ACS Chem Biol 2018 10 18;13(10):2862-2867. Epub 2018 Sep 18.

Epigenetics DPU, Immuno-Inflammation and Oncology Therapy Area, GlaxoSmithKline , Medicines Research Centre , Stevenage SG1 2NY , United Kingdom.

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http://pubs.acs.org/doi/10.1021/acschembio.8b00705
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http://dx.doi.org/10.1021/acschembio.8b00705DOI 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

Drawing on disorder: How viruses use histone mimicry to their advantage.

J Exp Med 2018 07 22;215(7):1777-1787. Epub 2018 Jun 22.

Epigenetics DPU, Oncology and Immuno-inflammation TA Units, GlaxoSmithKline Medicines Research Centre, Stevenage, England, UK.

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http://dx.doi.org/10.1084/jem.20180099DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6028506PMC
July 2018

Selective inhibition of BET proteins reduces pancreatic damage and systemic inflammation in bile acid- and fatty acid ethyl ester- but not caerulein-induced acute pancreatitis.

Pancreatology 2017 Sep - Oct;17(5):689-697. Epub 2017 Jun 10.

Department of Molecular and Clinical Cancer Medicine, Institute of Translational Medicine, University of Liverpool, Liverpool, UK; NIHR Liverpool Pancreas Biomedical Research Unit, Royal Liverpool University Hospital, Institute of Translational Medicine, University of Liverpool, Liverpool, UK. Electronic address:

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http://dx.doi.org/10.1016/j.pan.2017.06.005DOI Listing
June 2018

BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo.

Antiviral Res 2018 06 11;154:158-165. Epub 2018 Apr 11.

The Jake Gittlen Cancer Research Foundation, H069, Department of Pathology, C7800, The Pennsylvania State University, College of Medicine, 500 University Drive, Hershey, PA 17033-0850, USA.

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https://linkinghub.elsevier.com/retrieve/pii/S01663542173063
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http://dx.doi.org/10.1016/j.antiviral.2018.03.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5955851PMC
June 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

Inhibition of histone H3K27 demethylases selectively modulates inflammatory phenotypes of natural killer cells.

J Biol Chem 2018 02 4;293(7):2422-2437. Epub 2018 Jan 4.

From the Botnar Research Center, Nuffield Department of Orthopedics, Rheumatology and Musculoskeletal Sciences, National Institute of Health Research Oxford Biomedical Research Unit (BRU), University of Oxford, Oxford OX3 7DQ, United Kingdom,

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http://dx.doi.org/10.1074/jbc.RA117.000698DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5818173PMC
February 2018

Ezh2 and Runx1 Mutations Collaborate to Initiate Lympho-Myeloid Leukemia in Early Thymic Progenitors.

Cancer Cell 2018 02;33(2):274-291.e8

Haematopoietic Stem Cell Biology Laboratory, MRC Weatherall Institute of Molecular Medicine, Radcliffe Department of Medicine, University of Oxford, Oxford OX3 9DS, UK; MRC Molecular Haematology Unit, MRC Weatherall Institute of Molecular Medicine, Radcliffe Department of Medicine, University of Oxford, Oxford OX3 9DS, UK; NIHR Biomedical Research Centre, Churchill Hospital, Oxford OX3 7LE, UK. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2018.01.006DOI Listing
February 2018

Small molecules and their role in effective preclinical target validation.

Future Med Chem 2017 09 22;9(14):1579-1582. Epub 2017 Aug 22.

Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, UK.

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http://dx.doi.org/10.4155/fmc-2017-0121DOI Listing
September 2017

Immune disease-associated variants in gene enhancers point to BET epigenetic mechanisms for therapeutic intervention.

Epigenomics 2017 04 7;9(4):573-584. Epub 2016 Dec 7.

Epigenetics DPU, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.

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http://dx.doi.org/10.2217/epi-2016-0144DOI Listing
April 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

Epigenetic drug discovery: breaking through the immune barrier.

Nat Rev Drug Discov 2016 12 21;15(12):835-853. Epub 2016 Oct 21.

Epinova Epigenetics Discovery Performance Unit, Immuno-Inflammation Therapy Area, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.

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http://dx.doi.org/10.1038/nrd.2016.185DOI Listing
December 2016

BET bromodomain inhibition reduces maturation and enhances tolerogenic properties of human and mouse dendritic cells.

Mol Immunol 2016 11 3;79:66-76. Epub 2016 Oct 3.

Tytgat Institute for Gastro-Intestinal and Liver Research, Academic Medical Center, Amsterdam, The Netherlands. Electronic address:

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http://dx.doi.org/10.1016/j.molimm.2016.09.010DOI Listing
November 2016

Clinical progress and pharmacology of small molecule bromodomain inhibitors.

Curr Opin Chem Biol 2016 08 10;33:58-66. Epub 2016 Jun 10.

Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, UK. Electronic address:

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http://dx.doi.org/10.1016/j.cbpa.2016.05.028DOI Listing
August 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

Progress in the Development of non-BET Bromodomain Chemical Probes.

ChemMedChem 2016 Mar 8;11(5):477-87. Epub 2016 Jan 8.

Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire, SG1 2NY, UK.

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http://dx.doi.org/10.1002/cmdc.201500540DOI Listing
March 2016

The bromodomain protein inhibitor I-BET151 suppresses expression of inflammatory genes and matrix degrading enzymes in rheumatoid arthritis synovial fibroblasts.

Ann Rheum Dis 2016 Feb 2;75(2):422-9. Epub 2014 Dec 2.

Department of Experimental Immunology and Department of Clinical Immunology and Rheumatology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands.

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http://dx.doi.org/10.1136/annrheumdis-2014-205809DOI Listing
February 2016

Epigenetic mechanisms and drug discovery in rheumatology.

Clin Med (Lond) 2015 Dec;15 Suppl 6:s64-71

Immuno-inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK

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http://dx.doi.org/10.7861/clinmedicine.15-6-s64DOI Listing
December 2015

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

A novel mouse model identifies cooperating mutations and therapeutic targets critical for chronic myeloid leukemia progression.

J Exp Med 2015 Sep 24;212(10):1551-69. Epub 2015 Aug 24.

Department of Haematology, Cambridge Institute for Medical Research and Addenbrooke's Hospital, University of Cambridge, Cambridge CB2 0XY, England, UK Wellcome Trust - Medical Research Council Cambridge Stem Cell Institute, University of Cambridge, Cambridge CB2 1TN, England, UK

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http://jem.rupress.org/content/212/10/1551.full.pdf
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http://www.jem.org/lookup/doi/10.1084/jem.20141661
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http://dx.doi.org/10.1084/jem.20141661DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4577832PMC
September 2015

Brd4 bridges the transcriptional regulators, Aire and P-TEFb, to promote elongation of peripheral-tissue antigen transcripts in thymic stromal cells.

Proc Natl Acad Sci U S A 2015 Aug 27;112(32):E4448-57. Epub 2015 Jul 27.

Division of Immunology, Department of Microbiology and Immunobiology, Harvard Medical School, Boston, MA 02115; Evergrande Center for Immunologic Diseases, Harvard Medical School and Brigham and Women's Hospital, Boston, MA 02115

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http://dx.doi.org/10.1073/pnas.1512081112DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4538633PMC
August 2015

The "histone mimicry" by pathogens.

Cold Spring Harb Symp Quant Biol 2013 14;78:81-90. Epub 2014 Apr 14.

Laboratory of Immune Cell Epigenetics and Signaling, The Rockefeller University, New York, New York 10065

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http://symposium.cshlp.org/cgi/doi/10.1101/sqb.2013.78.02033
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http://dx.doi.org/10.1101/sqb.2013.78.020339DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5406129PMC
March 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

BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes.

Eur J Immunol 2015 Jan 1;45(1):287-297. Epub 2014 Dec 1.

Arthritis and Tissue Degeneration Program and David Z. Rosensweig Center for Genomics Research, Hospital for Special Surgery, New York, New York, USA.

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http://dx.doi.org/10.1002/eji.201444862DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4293348PMC
January 2015

The epigenetic regulator I-BET151 induces BIM-dependent apoptosis and cell cycle arrest of human melanoma cells.

J Invest Dermatol 2014 Nov 6;134(11):2795-2805. Epub 2014 Jun 6.

Melanoma Research Group, Kolling Institute of Medical Research, University of Sydney, St Leonards, New South Wales, Australia; Melanoma Institute of Australia, North Sydney, New South Wales, Australia. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0022202X153655
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http://dx.doi.org/10.1038/jid.2014.243DOI Listing
November 2014

Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11.

Br J Pharmacol 2014 Nov;171(22):4981-5010

Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Epinova DPU, Stevenage, UK.

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http://dx.doi.org/10.1111/bph.12848DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4253452PMC
November 2014

Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulation.

Nat Commun 2014 Nov 13;5:5418. Epub 2014 Nov 13.

1] Arthritis and Tissue Degeneration Program and David C. Rosensweig Center for Genomics Research, Hospital for Special Surgery, New York, New York 10021, USA [2] Department of Medicine, Weill Cornell Medical College, New York, New York 10021, USA [3] Graduate Program in Immunology and Microbial Pathogenesis, Weill Cornell Graduate School of Medical Sciences, New York, New York 10021, USA.

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http://dx.doi.org/10.1038/ncomms6418DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4249944PMC
November 2014

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

Suppression of the antiviral response by an influenza histone mimic.

Nature 2012 Mar 14;483(7390):428-33. Epub 2012 Mar 14.

Laboratory of Immune Cell Epigenetics and Signaling, The Rockefeller University, 1230 York Avenue, New York, New York 10065, USA.

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http://dx.doi.org/10.1038/nature10892DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3598589PMC
March 2012

Abeta(1-42) reduces synapse number and inhibits neurite outgrowth in primary cortical and hippocampal neurons: a quantitative analysis.

J Neurosci Methods 2008 Oct 9;175(1):96-103. Epub 2008 Aug 9.

Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline Research and Development Limited, New Frontiers Science Park, Essex, United Kingdom.

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http://dx.doi.org/10.1016/j.jneumeth.2008.08.001DOI Listing
October 2008

Lipid rafts mediate the interaction between myelin-associated glycoprotein (MAG) on myelin and MAG-receptors on neurons.

Mol Cell Neurosci 2003 Mar;22(3):344-52

Neurology Centre of Excellence for Drug Discovery, Glaxo SmithKline, New Frontiers Science Park North, Harlow, UK.

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March 2003