bms-186511

Description: BMS-186511 is a novel and potent Farnesyltransferase (FT) inhibitor with potential anticancer activity. BMS-186511 is a bisubstrate analogue inhibitor of FT, would inhibit the malignant growth properties of a cell line established from malignant schwannoma of an NF1 patient. Following treatment with BMS-186511 , ST88-14 cells became flat, nonrefractile, were contact-inhibited, and lost their ability to grow in soft agar. BMS-186511 was found to specifically inhibit FT, but not geranylgeranyltransferase I, a closely related enzyme. Thus, it is conceivable that FT inhibitors may ultimately become the first generation of drugs against the malignant phenotype in NF1 based on rational insights into the mechanism of action of neurofibromin.

References: Yan N, Ricca C, Fletcher J, Glover T, Seizinger BR, Manne V. Farnesyltransferase inhibitors block the neurofibromatosis type I (NF1) malignant phenotype. Cancer Res. 1995 Aug 15; 55(16):3569-75.