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Literature DB >> 26735842

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.

Brigitt Raux¹, Yuliia Voitovich^1,2, Carine Derviaux¹, Adrien Lugari¹, Etienne Rebuffet¹, Sabine Milhas^1,3, Stéphane Priet³, Thomas Roux⁴, Eric Trinquet⁴, Jean-Claude Guillemot³, Stefan Knapp^5,6,7, Jean-Michel Brunel¹, Alexey Yu Fedorov², Yves Collette¹, Philippe Roche¹, Stéphane Betzi¹, Sébastien Combes¹, Xavier Morelli¹.

Abstract

A midthroughput screening follow-up program targeting the first bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor. This compound binds with an affinity in the low micromolar range yet exerts suitable unexpected selectivity in vitro against the other members of the bromodomain and extra-terminal domain (BET) family. A structure-based program pinpointed a role of the ZA loop, paving the way for the development of potent and selective BET-BRDi probes.

Entities: Chemical Gene Species

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Year: 2016 PMID： 26735842 DOI： 10.1021/acs.jmedchem.5b01708

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

24 in total

1. Fr-PPIChem: An Academic Compound Library Dedicated to Protein-Protein Interactions.

Authors: Nicolas Bosc; Christophe Muller; Laurent Hoffer; David Lagorce; Stéphane Bourg; Carine Derviaux; Marie-Edith Gourdel; Jean-Christophe Rain; Thomas W Miller; Bruno O Villoutreix; Maria A Miteva; Pascal Bonnet; Xavier Morelli; Olivier Sperandio; Philippe Roche
Journal: ACS Chem Biol Date: 2020-05-05 Impact factor: 5.100

Review 2. BET bromodomain proteins and epigenetic regulation of inflammation: implications for type 2 diabetes and breast cancer.

Authors: Dequina A Nicholas; Guillaume Andrieu; Katherine J Strissel; Barbara S Nikolajczyk; Gerald V Denis
Journal: Cell Mol Life Sci Date: 2016-08-04 Impact factor: 9.261

3. BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Authors: Alex M Ayoub; Laura M L Hawk; Ryan J Herzig; Jiewei Jiang; Andrea J Wisniewski; Clifford T Gee; Peiliang Zhao; Jin-Yi Zhu; Norbert Berndt; Nana K Offei-Addo; Thomas G Scott; Jun Qi; James E Bradner; Timothy R Ward; Ernst Schönbrunn; Gunda I Georg; William C K Pomerantz
Journal: J Med Chem Date: 2017-06-07 Impact factor: 7.446

4. Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.

Authors: Zhiqing Liu; Haiying Chen; Pingyuan Wang; Yi Li; Eric A Wold; Paul G Leonard; Sarah Joseph; Allan R Brasier; Bing Tian; Jia Zhou
Journal: J Med Chem Date: 2020-04-22 Impact factor: 7.446

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.

1. Fr-PPIChem: An Academic Compound Library Dedicated to Protein-Protein Interactions.

Review 2. BET bromodomain proteins and epigenetic regulation of inflammation: implications for type 2 diabetes and breast cancer.

3. BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

4. Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.

5. NMR-based platform for fragment-based lead discovery used in screening BRD4-targeted compounds.

Review 6. Structural features and inhibitors of bromodomains.

Review 7. Clinical trials for BET inhibitors run ahead of the science.

Review 8. Targeting Brd4 for cancer therapy: inhibitors and degraders.

Review 9. 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.

10. Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.