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BET bromodomain proteins

In vitro studies suggest inhibiting distinct bromodomains within BET bromodomain-containing proteins could have distinct therapeutic effects. Thermal shift assays, binding studies and crystallization of BET inhibitor RVX-208 with 44 human bromodomains found the compound targets bromodomain 2 vs. bromodomain 1 with about 20-fold selectivity and that it displaced BET proteins from chromatin. In cells treated with RVX-208 or pan-BET inhibitors that act on both domains, RVX-208 had a much weaker effect on gene expression than the pan-BET inhibitors, suggesting a distinct mechanism of action. Next steps could include further distinguishing the effect of inhibiting bromodomain 2 vs. bromodomain 1 in vivo.
Resverlogix Corp.'s selective BET inhibitor, RVX-208, has completed two Phase IIb trials to treat cardiovascular disease. The company has spun out Zenith Epigenetics Corp. to further develop selective BET inhibitors.
At least four companies have BET inhibitors in Phase I trials to treat cancer.

SciBX 7(1); doi:10.1038/scibx.2014.29
Published online Jan. 9, 2014

RVX-208 patented by Resverlogix; partnering status unavailable

Picaud, S. et al. Proc. Natl. Acad. Sci. USA; published online Nov. 18, 2013;
Contact: Panagis Filippakopoulos, University of Oxford, Oxford, U.K.
Contact: Stefan Knapp, same affiliation as above