Enzyme inhibitors

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 = 20 nM), DiFi humancolon cancer cells and MDA MB-468 human breast cancer cells.

It is produced by the strain of Bacillus cereus BMF 657-RF1. It can inhibit Dipeptidyl amino peptidase IV and immune enhancement effect.

1,1-Dimethylbiguanide hydrochloride is the hydrochloride salt of the biguanide metformin with antihyperglycemic and potential antineoplastic activities. It decreases hyperglycemia primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).

It is an unusual ester of two structurally related alkylresorcinols first isolated from fungus, cytonaema sp. It is a potent inhibitor of HIV-1.

It is an unusual ester of two structurally related alkylresorcinols first isolated from fungus, cytonaema sp. It is a potent inhibitor of HIV-1.

Deoxynojirimycin inhibits mammalian glucosidase 1. As well, it inhibits intestinal and lysosmal alpha-glucosidases, beta-glucosidase from sweet almonds, pancreatic alpha-amylase and amyloglucosidase.

gamma-Mangostin isolated from the fruit of Garcinia cambogia is an HIV protease inhibitor. gamma-Mangostin is cytotoxic to HL-60, SMMC-7721, A549, MCF-7, and SW480 cancer cells and BEAS-2B non-cancerous pulmonary epithelial cells in vitro (IC50s = 7.39, 6.57, 10.07, 5.33, 8.4, and 7.43 μM, respectively).

Rapamycin is an mTOR inhibitor immunosuppressant and kinase inhibitor with both antifungal and antineoplastic properties. It selectively inhibits the transcriptional activation of cytokines.

Plitidepsin is a cyclic depsipeptide isolated from the marine tunicate Aplidium albicans. Plitidepsin shows potent anticancer activity against a large variety of cultured human cancer cells, inducing apoptosis by triggering mitochondrial cytochrome c release, initiating the Fas/DC95, JNK pathway and activating caspase 3 activation. This agent also inhibits elongation factor 1-a, thereby interfering with protein synthesis, and induces G1 arrest and G2 blockade, thereby inhibiting tumor cell growth.

Exatecan mesylate is a semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting the religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogs.