Targeting on Epigenetic Proteins for Cancer Therapy
Jun Qi,
Lead Scientist,
Dana Farber Cancer Institute
Lysine Targeting acetyl-lysine recognition modules with small molecules have been successfully achieved a set of probe compounds, such as JQ1, IBET, with great selectivity for the BET-family of bromodomains. We have identified small molecule inhibitor for BET bromodomain inhibition several years ago. We have then significantly improved our chemical probe to produce a potent selective inhibitor, JQ35/Ten-010, with great pharmacokinetic properties. This compound has been fully characterized, evaluated and entered clinical investigation. With the excellent PK properties in human, the compound exhibited clinical efficacy in patients who had NUT midline carcinoma. Thus, we have further demonstrated the transformation of the chemical probes to potential drug candidate for human clinic investigation.
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