UP1002

UP1002 is a small molecule targeted protein degrader (TPD) developed by UPPthera, designed to target and degrade Polo-like kinase 1 (PLK1). PLK1 is a key regulator of the cell cycle, particularly during mitosis, and is frequently overexpressed in various cancers, where it promotes tumor cell proliferation and survival. Unlike traditional small molecule inhibitors that only block the enzymatic activity of PLK1, UP1002 utilizes a PROTAC-like mechanism to recruit an E3 ubiquitin ligase to the target protein, leading to its ubiquitination and subsequent degradation by the proteasome. This approach potentially offers more complete inhibition of PLK1's multiple functions and may overcome resistance mechanisms associated with traditional inhibitors. UP1002 is currently being evaluated in Phase 1 clinical development for the treatment of oncology indications.

Other names

PLK1 PROTACPLK-1 PROTACPLK 1 PROTAC