Literature DB >> 19577000

Histone acetyl transferases as emerging drug targets.

Frank J Dekker1, Hidde J Haisma.   

Abstract

Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyl transferases (HATs) catalyze the acetylation of histones on specific lysine residues. A potential role of HATs in the pathology of cancer, asthma, COPD and viral infection has been described. This indicates that specific HAT inhibitors are potential tools for pharmacological research and might find therapeutic applications. This review focuses on the role of the HATs p300, CBP, PCAF and GCN5 in different diseases and the development of small-molecule inhibitors of these enzymes as potential drugs.

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Year:  2009        PMID: 19577000     DOI: 10.1016/j.drudis.2009.06.008

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  98 in total

1.  Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.

Authors:  Erin M Bowers; Gai Yan; Chandrani Mukherjee; Andrew Orry; Ling Wang; Marc A Holbert; Nicholas T Crump; Catherine A Hazzalin; Glen Liszczak; Hua Yuan; Cecilia Larocca; S Adrian Saldanha; Ruben Abagyan; Yan Sun; David J Meyers; Ronen Marmorstein; Louis C Mahadevan; Rhoda M Alani; Philip A Cole
Journal:  Chem Biol       Date:  2010-05-28

Review 2.  Epigenetic protein families: a new frontier for drug discovery.

Authors:  Cheryl H Arrowsmith; Chas Bountra; Paul V Fish; Kevin Lee; Matthieu Schapira
Journal:  Nat Rev Drug Discov       Date:  2012-04-13       Impact factor: 84.694

Review 3.  Chemical biology of histone acetyltransferase natural compounds modulators.

Authors:  Fabrizio Dal Piaz; Antonio Vassallo; Osmany Cuesta Rubio; Sabrina Castellano; Gianluca Sbardella; Nunziatina De Tommasi
Journal:  Mol Divers       Date:  2011-01-01       Impact factor: 2.943

4.  Application of a high-throughput fluorescent acetyltransferase assay to identify inhibitors of homocitrate synthase.

Authors:  Stacie L Bulfer; Thomas J McQuade; Martha J Larsen; Raymond C Trievel
Journal:  Anal Biochem       Date:  2010-11-10       Impact factor: 3.365

5.  PTEN activation through K163 acetylation by inhibiting HDAC6 contributes to tumour inhibition.

Authors:  Z Meng; L-F Jia; Y-H Gan
Journal:  Oncogene       Date:  2015-08-17       Impact factor: 9.867

6.  Heparanase-mediated loss of nuclear syndecan-1 enhances histone acetyltransferase (HAT) activity to promote expression of genes that drive an aggressive tumor phenotype.

Authors:  Anurag Purushothaman; Douglas R Hurst; Claudio Pisano; Shuji Mizumoto; Kazuyuki Sugahara; Ralph D Sanderson
Journal:  J Biol Chem       Date:  2011-07-11       Impact factor: 5.157

Review 7.  Epigenetic mechanisms in stroke and epilepsy.

Authors:  Jee-Yeon Hwang; Kelly A Aromolaran; R Suzanne Zukin
Journal:  Neuropsychopharmacology       Date:  2012-08-15       Impact factor: 7.853

8.  Creb1-Mecp2-(m)CpG complex transactivates postnatal murine neuronal glucose transporter isoform 3 expression.

Authors:  Yongjun Chen; Bo-Chul Shin; Shanthie Thamotharan; Sherin U Devaskar
Journal:  Endocrinology       Date:  2013-03-14       Impact factor: 4.736

9.  BET bromodomain inhibitors block growth of pancreatic cancer cells in three-dimensional collagen.

Authors:  Vaibhav Sahai; Krishan Kumar; Lawrence M Knab; Christina R Chow; Sania S Raza; David J Bentrem; Kazumi Ebine; Hidayatullah G Munshi
Journal:  Mol Cancer Ther       Date:  2014-05-07       Impact factor: 6.261

10.  Dietary, metabolic, and potentially environmental modulation of the lysine acetylation machinery.

Authors:  Go-Woon Kim; Goran Gocevski; Chao-Jung Wu; Xiang-Jiao Yang
Journal:  Int J Cell Biol       Date:  2010-10-05
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