coatomer inhibitor

Coatomer inhibitor (specifically targeting COPZ1) is a small-molecule therapeutic program developed by Senex Biotech for the treatment of various cancers. The drug targets the COPZ1 subunit of the coatomer protein complex I (COPI), which is responsible for retrograde vesicle transport from the Golgi apparatus to the endoplasmic reticulum (ER). The therapeutic strategy utilizes the concept of collateral lethality; many human tumors lose the expression of COPZ2, a functional paralog of COPZ1, rendering them uniquely dependent on COPZ1 for survival. By inhibiting COPZ1, the drug disrupts essential intracellular trafficking, leading to massive ER stress and selective apoptosis in tumor cells while sparing normal tissues that retain COPZ2 expression. The program is currently in preclinical development for multiple tumor types.

Other names

coatomer inhibitorCOPZ1 inhibitorCOPZ-1 inhibitorCOPZ 1 inhibitorCOPI complex inhibitor