Synonyms: AZD 3409 | AZD-3409
Compound class:
Synthetic organic
Comment: AZD3409 is an an orally active double prodrug, peptidomimetic type farnesyltransferase inhibitor (FTI). It is a double prodrug in that it has its thiol and carboxylate groups blocked to reduce toxicity.
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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 [2], perhaps due to redundancy in the system which sees geranylgeranyltransferase taking over the prenylation process, when farnesyltransferase is inhibited. |