Literature DB >> 27530368

A Chemical Probe for the ATAD2 Bromodomain.

Paul Bamborough1, Chun-Wa Chung2, Emmanuel H Demont3, Rebecca C Furze2, Andrew J Bannister4, Ka Hing Che4, Hawa Diallo2, Clement Douault2, Paola Grandi5, Tony Kouzarides4, Anne-Marie Michon5, Darren J Mitchell2, Rab K Prinjha2, Christina Rau5, Samuel Robson4, Robert J Sheppard2,6, Richard Upton2, Robert J Watson2.   

Abstract

ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.
© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  bioisosteres; conformation analysis; epigenetics; fluorine; medicinal chemistry

Year:  2016        PMID： 27530368      PMCID： PMC7314595          DOI： 10.1002/anie.201603928

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN： 1433-7851            Impact factor:   15.336


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3.  Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.

Authors:  Emmanuel H Demont; Chun-wa Chung; Rebecca C Furze; Paola Grandi; Anne-Marie Michon; Chris Wellaway; Nathalie Barrett; Angela M Bridges; Peter D Craggs; Hawa Diallo; David P Dixon; Clement Douault; Amanda J Emmons; Emma J Jones; Bhumika V Karamshi; Kelly Locke; Darren J Mitchell; Bernadette H Mouzon; Rab K Prinjha; Andy D Roberts; Robert J Sheppard; Robert J Watson; Paul Bamborough
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