Protease inhibitor: HIV-1 protease; Autophagy modulator. Inhibits SARS-CoV-2 in cells. Xu et al. ChemRxiv, Mar 31 2020, https://doi.org/10.26434/chemrxiv.12039888.v1; Ohashi et al. bioRxiv, Apr 15 2020, https://doi.org/10.1101/2020.04.14.039925.
Biochemicals & reagents
1) Olmo et al. (2006), A review of nelfinavir for the treatment of HIV infection; Expert Opin. Drug Metab. Toxicol., 2 285 2) Bruning et al. (2010), New prospects for nelfinavir in non-HIV-related diseases; Curr. Mol. Pharmacol., 3 91 3) Gills et al. (2007), Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo; Clin. Cancer Res, 13 5183 4) Shim et al. (2012), Selective inhibition of HER2-positive breast cancer cells by the HIV protease inhibitor nelfinavir; J. Natl. Cancer Inst,, 104 1576
Nelfinavir is a clinically relevant anti-HIV agent acting via inhibition of HIV-1 protease with a Ki=2 nM (1) and it also displays efficacy in cancer, malaria, tuberculosis and SARS (2). This compound displays broad spectrum anticancer activity and induces endoplasmic reticulum stress, autophagy and apoptosis in vitro and in vivo (3) and also inhibits the growth of HER2-positive breast cancer cells via inhibition of HSP90 through a novel mechanism (4).