Delving into the Latest Updates on L-731734 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Ftase

Mechanism

Ftase inhibitors(Protein farnesyltransferase inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

Merck & Co., Inc.

Active Organization-

Inactive Organization

Merck & Co., Inc.

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

To acquire transforming potential, the precursor of the Ras oncoprotein must undergo farnesylation of the cysteine residue located in a carboxyl-terminal tetrapeptide. Inhibitors of the enzyme that catalyzes this modification, farnesyl protein transfe ras e (FPTase), have therefore been suggested as anticancer agents for tumors in which Ras contributes to transformation. The tetrapeptide analog L-731,735 is a potent and selective inhibitor of FPTase in vitro. A prodrug of this compound, L-731,734, inhibited Ras processing in cells transformed with v- ras . L-731,734 decreased the ability of v- ras -transformed cells to form colonies in soft agar but had no effect on the efficiency of colony formation of cells transformed by either the v- raf or v- mos oncogenes. The results demonstrate selective inhibition of ras -dependent cell transformation with a synthetic organic inhibitor of FPTase.

100 Deals associated with L-731734

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