Mammalian target of rapamycin (mTOR) Inhibitors.
Current efforts in anticancer drug development are targeting key factors in cell-cycle regulation. Mammalian target of rapamycin (mTOR) is one such protein kinase that facilitates cell growth by stimulating the cell to traverse the G1 to S phase of the cell cycle. Rapamycin is the first defined inhibitor of mTOR, and the demonstration of its antitumor activity has led to great interest in this pathway as an antitumor mechanism. Analogues with better pharmacologic properties have been developed and have entered clinical trials. Human cell lines of renal cell cancer, among several other tumors, are sensitive to growth inhibition via this pathway. Ongoing clinical trials are evaluating renal cell cancer and other malignancies using therapy with mTOR inhibitors. These agents are more likely to induce growth inhibition rather than tumor regression.
Dutcher
Janice P
JP
Our Lady of Mercy Cancer Center, New York Medical College, 600 East 233rd Street, Bronx, NY 10466, USA. jpd4401@aol.com
D000903:Antibiotics, Antineoplastic / Q000494:pharmacology / Q000627:therapeutic use*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; D020123:Sirolimus / Q000494:pharmacology / Q000627:therapeutic use*; D058570:TOR Serine-Threonine Kinases
D000903:Antibiotics, Antineoplastic; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; C546842:MTOR protein, human; D058570:TOR Serine-Threonine Kinases; D020123:Sirolimus