Since acetylation plays a crucial role in the regulation of gene expression, interest has arisen as to how histone deacetylases (HDACs) may regulate anomalous gene expression in cancer. Small molecule inhibitors targeting HDACs have been developed as anti-cancer agents, but all known inhibitors target the enzymatic active site and lack isoform selectivity.
In the search for novel allosteric HDAC inhibitors, Nicole and her Broad colleagues identified candidates from two small molecule libraries. Future objectives are to evaluate binding kinetics of these candidates and perform in vitro activity and phenotypic assays to assess inhibitory capabilities.
PROJECT: Unbiased ligand discovery for histone deacetylases using small molecule microarrays
The Broad Institute is a truly unique place where scientists from different fields come together and look at the big picture of genomics. I was excited to have the opportunity to work with top-notch scientists.