Evaluation of linker length effects on a BET bromodomain probe

Fueled by the therapeutic potential of the epigenetic machinery, BET bromodomains have seen high interest as drug targets. Herein, we introduce different linkers to a BET bromodomain benzodiazepine ligand (I-BET762) to gauge its implications in the development of hybrid drugs, imaging probes and sma...

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Bibliographic Details
Main Authors: Traquete, R, Henderson, E, Picaud, S, Cal, P, Sieglitz, F, Rodrigues, T, Oliveira, R, Filippakopoulos, P, Bernardes, G
Format: Journal article
Language:English
Published: Royal Society of Chemistry 2019