The proteolysis targeting chimera (PROTAC) has gained momentum for the disocvery and development of completely new classes of therapeutics for the treatment of human diseases. In this lecture, I will persent our latest advancement in the discovery and development of PROTAC molecules to target gene transcriptional factors. I will focus on targeting those traditionally undrugabble targets such as STAT3 protein. I will present our major findings in terms of key differences between small-molecule inhibitors and PROTAC degraders in terms of regulation of gene transcriptional and the major advantages for PROTAC degraders over traditional small-molecule inhibitors for transcriptional factors.

Targeting the undruggable: PROTAC approach to target transcriptional factors

2019 Spring National Meeting

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