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Literature DB >> 25408830

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

Emmanuel H Demont¹, Paul Bamborough¹, Chun-Wa Chung¹, Peter D Craggs¹, David Fallon¹, Laurie J Gordon¹, Paola Grandi², Clare I Hobbs¹, Jameed Hussain¹, Emma J Jones¹, Armelle Le Gall¹, Anne-Marie Michon², Darren J Mitchell¹, Rab K Prinjha¹, Andy D Roberts³, Robert J Sheppard¹, Robert J Watson¹.

Abstract

The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.

Entities: Chemical Gene

Keywords: BRD1; BRPF1; BRPF2; BRPF3; bromodomain; chemical probe; epigenetics; fragment; inhibitor

Year: 2014 PMID： 25408830 PMCID： PMC4233354 DOI： 10.1021/ml5002932

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

22 in total

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

Authors: Chun-Wa Chung; Anthony W Dean; James M Woolven; Paul Bamborough
Journal: J Med Chem Date: 2012-01-11 Impact factor: 7.446

Review 2. The MOZ histone acetyltransferase in epigenetic signaling and disease.

Authors: Samuel Carlson; Karen C Glass
Journal: J Cell Physiol Date: 2014-11 Impact factor: 6.384

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

Authors: Paul Bamborough; Hawa Diallo; Jonathan D Goodacre; Laurie Gordon; Antonia Lewis; Jonathan T Seal; David M Wilson; Michael D Woodrow; Chun-Wa Chung
Journal: J Med Chem Date: 2012-01-11 Impact factor: 7.446

4. 2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives.

Authors: I Tapia; L Alonso-Cires; P L López-Tudanca; R Mosquera; L Labeaga; A Innerárity; A Orjales
Journal: J Med Chem Date: 1999-07-29 Impact factor: 7.446

5. Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.

Authors: Lele Zhao; Danyan Cao; Tiantian Chen; Yingqing Wang; Zehong Miao; Yechun Xu; Wuyan Chen; Xin Wang; Yanlian Li; Zhiyan Du; Bing Xiong; Jian Li; Chunyan Xu; Naixia Zhang; Jianhua He; Jingkang Shen
Journal: J Med Chem Date: 2013-05-14 Impact factor: 7.446

6. Support of association between BRD1 and both schizophrenia and bipolar affective disorder.

Authors: Mette Nyegaard; Jacob E Severinsen; Thomas D Als; Anne Hedemand; Steen Straarup; Merete Nordentoft; Andrew McQuillin; Nicholas Bass; Jacob Lawrence; Srinivasa Thirumalai; Ana C P Pereira; Radhika Kandaswamy; Gregory J Lydall; Pamela Sklar; Edward Scolnick; Shaun Purcell; David Curtis; Hugh M D Gurling; Preben B Mortensen; Ole Mors; Anders D Børglum
Journal: Am J Med Genet B Neuropsychiatr Genet Date: 2010-03-05 Impact factor: 3.568

7. Molecular architecture of quartet MOZ/MORF histone acetyltransferase complexes.

Authors: Mukta Ullah; Nadine Pelletier; Lin Xiao; Song Ping Zhao; Kainan Wang; Cindy Degerny; Soroush Tahmasebi; Christelle Cayrou; Yannick Doyon; Siew-Lee Goh; Nathalie Champagne; Jacques Côté; Xiang-Jiao Yang
Journal: Mol Cell Biol Date: 2008-09-15 Impact factor: 4.272

Review 8. BET bromodomain inhibitors: a patent review.

Authors: Jean-Marc Garnier; Phillip P Sharp; Christopher J Burns
Journal: Expert Opin Ther Pat Date: 2013-11-22 Impact factor: 6.674

9. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.

Authors: Kevin G McLure; Emily M Gesner; Laura Tsujikawa; Olesya A Kharenko; Sarah Attwell; Eric Campeau; Sylwia Wasiak; Adam Stein; Andre White; Eric Fontano; Robert K Suto; Norman C W Wong; Gregory S Wagner; Henrik C Hansen; Peter R Young
Journal: PLoS One Date: 2013-12-31 Impact factor: 3.240

10. TET2 and TET3 regulate GlcNAcylation and H3K4 methylation through OGT and SET1/COMPASS.

Authors: Rachel Deplus; Benjamin Delatte; Marie K Schwinn; Matthieu Defrance; Jacqui Méndez; Nancy Murphy; Mark A Dawson; Michael Volkmar; Pascale Putmans; Emilie Calonne; Alan H Shih; Ross L Levine; Olivier Bernard; Thomas Mercher; Eric Solary; Marjeta Urh; Danette L Daniels; François Fuks
Journal: EMBO J Date: 2013-01-25 Impact factor: 11.598

21 in total

Review 1. Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development.

Authors: Victoria Jeffers; Chunlin Yang; Sherri Huang; William J Sullivan
Journal: Microbiol Mol Biol Rev Date: 2017-01-11 Impact factor: 11.056

2. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

Authors: Wylie S Palmer; Guillaume Poncet-Montange; Gang Liu; Alessia Petrocchi; Naphtali Reyna; Govindan Subramanian; Jay Theroff; Anne Yau; Maria Kost-Alimova; Jennifer P Bardenhagen; Elisabetta Leo; Hannah E Shepard; Trang N Tieu; Xi Shi; Yanai Zhan; Shuping Zhao; Michelle C Barton; Giulio Draetta; Carlo Toniatti; Philip Jones; Mary Geck Do; Jannik N Andersen
Journal: J Med Chem Date: 2015-07-06 Impact factor: 7.446

Review 3. Biological function and histone recognition of family IV bromodomain-containing proteins.

Authors: Jonathan T Lloyd; Karen C Glass
Journal: J Cell Physiol Date: 2017-06-13 Impact factor: 6.384

4. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesion.

Authors: Srikanth Appikonda; Kaushik N Thakkar; Parantu K Shah; Sharon Y R Dent; Jannik N Andersen; Michelle C Barton
Journal: J Biol Chem Date: 2018-03-09 Impact factor: 5.157

Review 5. Structural features and inhibitors of bromodomains.

Authors: Jamel Meslamani; Steven G Smith; Roberto Sanchez; Ming-Ming Zhou
Journal: Drug Discov Today Technol Date: 2016-09-22

6. Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.

Authors: Xiaoyang Li; Yingjie Zhang; Yuqi Jiang; Jingde Wu; Elizabeth S Inks; C James Chou; Shuai Gao; Jinning Hou; Qinge Ding; Jingyao Li; Xue Wang; Yongxue Huang; Wenfang Xu
Journal: Eur J Med Chem Date: 2017-03-30 Impact factor: 6.514