Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces.

ABSTRACT: Epigenetics is a rapidly growing field in drug discovery. Of particular interest is the role of post-translational modifications to histones and the proteins that read, write, and erase such modifications. The development of inhibitors for reader domains has focused on single domains. One of the major difficulties of designing inhibitors for reader domains is that, with the notable exception of bromodomains, they tend not to possess a well-enclosed binding site amenable to small-molecule inhibition. As many of the proteins in epigenetic regulation have multiple domains, there are opportunities for designing inhibitors that bind at a domain-domain interface which provide a more suitable interaction pocket. Examination of X-ray structures of multiple domains involved in recognising and modif

SUBMITTER: Bowkett D 

PROVIDER: S-EPMC6001751 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature