3, 5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

…, S Uttarkar, P Filippakopoulos, S Picaud…

Index: Hewings, David S.; Wang, Minghua; Philpott, Martin; Fedorov, Oleg; Uttarkar, Sagar; Filippakopoulos, Panagis; Picaud, Sarah; Vuppusetty, Chaitanya; Marsden, Brian; Knapp, Stefan; Conway, Stuart J.; Heightman, Tom D. Journal of Medicinal Chemistry, 2011 , vol. 54, # 19 p. 6761 - 6770

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Citation Number: 114

Abstract

Histone–lysine acetylation is a vital chromatin post-translational modification involved in the epigenetic regulation of gene transcription. Bromodomains bind acetylated lysines, acting as readers of the histone-acetylation code. Competitive inhibitors of this interaction have antiproliferative and anti-inflammatory properties. With 57 distinct bromodomains known, the discovery of subtype-selective inhibitors of the histone–bromodomain interaction is of ...