A non-specific bromodomain inhibitor
Bromosporine is a broad spectrum inhibitor of bromodomains with IC50 value of 0.41 μM, 0.29μM, 0.122μM for BRD2, BRD4 and BRD9, respectively [1].
Bromodomains is a 110 amino acid protein domain which can recognize monoacetylated lysine residues and play a pivotal role in the targeting of chromatin-modifying enzymes to specific sites. It has been revealed that proteins contained BRDs involves in the development of many diseases, including cancers, inflammatory diseases and neurological diseases.
It is also reported that Bromosporine functioned on BAZ2A, BRPF3, CECR2, FALZ and TIF-1α with IC50 value of 9.36μM, 48.11μM, 0.017μM, 5.655μM and 12.38μM, respectively [1].
Reference:
[1].? University of Oxford. Structural Genomics Consortium Nuffield Dept. of Clinical Medicine. 15th Hellenic Symposium of Medicinal Chemistry Athens, 30, May, 2012.
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