BMS-214662

Ligand id: 8026

Name: BMS-214662

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 1
Rotatable bonds 6
Topological polar surface area 129.71
Molecular weight 489.13
XLogP 5.32
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Mechanism Of Action and Pharmacodynamic Effects
FTIs inhibit the C-terminal prenylation of many proteins involved in signal transduction, but are being investigated mainly as inhibitors of deregulated RAS activity in transformed cells. Blocking prenylation of RAS oncogenic proteins prevents their correct membrane tethering, and thereby effects reduced RAS signalling activity and increased cancer cell apoptosis. However, the promise of FTIs has not been bourne out in clinical trials [1], perhaps due to redundancy in the system which sees geranylgeranyltransferase taking over the prenylation process, when farnesyltransferase is inhibited.