desthiazolylmethyloxycarbonyl ritonavir

Desthiazolylmethyloxycarbonyl ritonavir (also known as M1) is a minor metabolite of the HIV protease inhibitor ritonavir. Developed by researchers at the University of Minnesota, it is being investigated as a potential therapeutic agent for breast cancer. Unlike ritonavir, desthiazolylmethyloxycarbonyl ritonavir acts as a proteasome activator, up-regulating the chymotryptic, tryptic, and caspase-like activities of the 20S proteasome. This activation leads to the down-regulation of survivin (BIRC5) and HER2 (ERBB2), inducing G0/G1 cell cycle arrest and apoptosis in breast cancer cells. It has demonstrated more potent in vitro and in vivo activity against estrogen receptor-positive (ER+), HER2-positive (HER2+), and triple-negative breast cancer (TNBC) cell lines compared to ritonavir.

Other names

des-ritonavirdesthiazolylmethyloxycarbonylritonavirritonavir metaboliteritonavir metabolite M1