BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability

Ligands for the bromodomain and extra-terminal domain (BET) family of bromodomains have shown promise as useful therapeutic agents for treating a range of cancers and inflammation. Here we report that our previously developed 3,5-dimethylisoxazole-based BET bromodomain ligand (OXFBD02) inhibits inte...

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Bibliographic Details
Main Authors: Jennings, L, Schiedel, M, Hewings, D, Picaud, S, Laurin, C, Bruno, P, Bluck, J, Scorah, A, See, L, Reynolds, J, Moroglu, M, Mistry, I, Hicks, A, Guzanov, P, Clayton, J, Evans, C, Stazi, G, Biggin, P, Mapp, A, Hammond, E, Humphreys, P, Filippakopoulos, P, Conway, S
Format: Journal article
Language:English
Published: Elsevier 2018

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