Literature DB >> 24900532

Bromodomains: are readers right for epigenetic therapy?

Stuart J Conway1.   

Abstract

There is intense interest in the development of small molecule inhibitors of the acetyl-lysine-reading bromodomain protein module. These inhibitors represent a way of interfering therapeutically in epigenetic processes, and there are currently two bromodomain inhibitors in clinical trials. The success of these compounds rests on safety aspects of epigenetic target modulation being addressed.

Year:  2012        PMID: 24900532      PMCID: PMC4025779          DOI: 10.1021/ml300221t

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


  15 in total

Review 1.  Acetylation: a regulatory modification to rival phosphorylation?

Authors:  T Kouzarides
Journal:  EMBO J       Date:  2000-03-15       Impact factor: 11.598

2.  The bromodomain: a conserved sequence found in human, Drosophila and yeast proteins.

Authors:  S R Haynes; C Dollard; F Winston; S Beck; J Trowsdale; I B Dawid
Journal:  Nucleic Acids Res       Date:  1992-05-25       Impact factor: 16.971

Review 3.  The bromodomain interaction module.

Authors:  Panagis Filippakopoulos; Stefan Knapp
Journal:  FEBS Lett       Date:  2012-05-03       Impact factor: 4.124

4.  Selective small molecules blocking HIV-1 Tat and coactivator PCAF association.

Authors:  Lei Zeng; Jiaming Li; Michaela Muller; Sherry Yan; Shiraz Mujtaba; Chongfeng Pan; Zhiyong Wang; Ming-Ming Zhou
Journal:  J Am Chem Soc       Date:  2005-03-02       Impact factor: 15.419

5.  BET bromodomain inhibition as a therapeutic strategy to target c-Myc.

Authors:  Jake E Delmore; Ghayas C Issa; Madeleine E Lemieux; Peter B Rahl; Junwei Shi; Hannah M Jacobs; Efstathios Kastritis; Timothy Gilpatrick; Ronald M Paranal; Jun Qi; Marta Chesi; Anna C Schinzel; Michael R McKeown; Timothy P Heffernan; Christopher R Vakoc; P Leif Bergsagel; Irene M Ghobrial; Paul G Richardson; Richard A Young; William C Hahn; Kenneth C Anderson; Andrew L Kung; James E Bradner; Constantine S Mitsiades
Journal:  Cell       Date:  2011-09-01       Impact factor: 41.582

6.  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

7.  Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

Authors:  Mark A Dawson; Rab K Prinjha; Antje Dittmann; George Giotopoulos; Marcus Bantscheff; Wai-In Chan; Samuel C Robson; Chun-wa Chung; Carsten Hopf; Mikhail M Savitski; Carola Huthmacher; Emma Gudgin; Dave Lugo; Soren Beinke; Trevor D Chapman; Emma J Roberts; Peter E Soden; Kurt R Auger; Olivier Mirguet; Konstanze Doehner; Ruud Delwel; Alan K Burnett; Phillip Jeffrey; Gerard Drewes; Kevin Lee; Brian J P Huntly; Tony Kouzarides
Journal:  Nature       Date:  2011-10-02       Impact factor: 49.962

8.  RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.

Authors:  Johannes Zuber; Junwei Shi; Eric Wang; Amy R Rappaport; Harald Herrmann; Edward A Sison; Daniel Magoon; Jun Qi; Katharina Blatt; Mark Wunderlich; Meredith J Taylor; Christopher Johns; Agustin Chicas; James C Mulloy; Scott C Kogan; Patrick Brown; Peter Valent; James E Bradner; Scott W Lowe; Christopher R Vakoc
Journal:  Nature       Date:  2011-08-03       Impact factor: 49.962

9.  Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites.

Authors:  Lewis R Vidler; Nathan Brown; Stefan Knapp; Swen Hoelder
Journal:  J Med Chem       Date:  2012-07-12       Impact factor: 7.446

10.  Selective inhibition of BET bromodomains.

Authors:  Panagis Filippakopoulos; Jun Qi; Sarah Picaud; Yao Shen; William B Smith; Oleg Fedorov; Elizabeth M Morse; Tracey Keates; Tyler T Hickman; Ildiko Felletar; Martin Philpott; Shonagh Munro; Michael R McKeown; Yuchuan Wang; Amanda L Christie; Nathan West; Michael J Cameron; Brian Schwartz; Tom D Heightman; Nicholas La Thangue; Christopher A French; Olaf Wiest; Andrew L Kung; Stefan Knapp; James E Bradner
Journal:  Nature       Date:  2010-09-24       Impact factor: 49.962

View more
  4 in total

1.  Inhibitors of BRD4 Protein from a Marine-Derived Fungus Alternaria sp. NH-F6.

Authors:  Hui Ding; Dashan Zhang; Biao Zhou; Zhongjun Ma
Journal:  Mar Drugs       Date:  2017-03-16       Impact factor: 5.118

2.  Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

Authors:  David S Hewings; Oleg Fedorov; Panagis Filippakopoulos; Sarah Martin; Sarah Picaud; Anthony Tumber; Christopher Wells; Monica M Olcina; Katherine Freeman; Andrew Gill; Alison J Ritchie; David W Sheppard; Angela J Russell; Ester M Hammond; Stefan Knapp; Paul E Brennan; Stuart J Conway
Journal:  J Med Chem       Date:  2013-04-05       Impact factor: 7.446

3.  Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor.

Authors:  Luiz Antonio Dutra; David Heidenreich; Gabriel Dalio Bernardes da Silva; Chung Man Chin; Stefan Knapp; Jean Leandro Dos Santos
Journal:  Nutrients       Date:  2017-10-27       Impact factor: 5.717

4.  Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.

Authors:  Michael Brand; James Clayton; Mustafa Moroglu; Matthias Schiedel; Sarah Picaud; Joseph P Bluck; Anna Skwarska; Hannah Bolland; Anthony K N Chan; Corentine M C Laurin; Amy R Scorah; Larissa See; Timothy P C Rooney; Katrina H Andrews; Oleg Fedorov; Gabriella Perell; Prakriti Kalra; Kayla B Vinh; Wilian A Cortopassi; Pascal Heitel; Kirsten E Christensen; Richard I Cooper; Robert S Paton; William C K Pomerantz; Philip C Biggin; Ester M Hammond; Panagis Filippakopoulos; Stuart J Conway
Journal:  J Med Chem       Date:  2021-07-13       Impact factor: 7.446

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.