179486-48-7Relevant academic research and scientific papers
Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins
Raux, Brigitt,Voitovich, Yuliia,Derviaux, Carine,Lugari, Adrien,Rebuffet, Etienne,Milhas, Sabine,Priet, Stéphane,Roux, Thomas,Trinquet, Eric,Guillemot, Jean-Claude,Knapp, Stefan,Brunel, Jean-Michel,Fedorov, Alexey Yu.,Collette, Yves,Roche, Philippe,Betzi, Stéphane,Combes, Sébastien,Morelli, Xavier
, p. 1634 - 1641 (2016/03/05)
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.
Aryl thioxanthines
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, (2008/06/13)
PCT No. PCT/US95/16723 Sec. 371 Date Aug. 18, 1997 Sec. 102(e) Date Aug. 18, 1997 PCT Filed Dec. 12, 1995 PCT Pub. No. WO96/18399 PCT Pub. Date Jun. 20, 1996The present invention relates to novel compounds of the formula (I): wherein Q3R3 and Q8R8 are des
