Farnesyltransferase Inhibitors As Anticancer Agents

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 22006
Amount: $50,000.00
Phase: Phase I
Program: SBIR
Awards Year: 1993
Solicitation Year: N/A
Solicitation Topic Code: N/A
Solicitation Number: N/A
Small Business Information
5166 Campus Drive, Plymouth Meeting, PA, 19462
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 Robert E. Zipkin
 (610) 941-0430
Business Contact
Phone: () -
Research Institution
The goal of the research is to develop a potent, pharmacologically useful inhibitor of farnesyltransferase for use as a new therapeutic agent for cancer. The Ras family of oncogenes and proto-oncogenes encode guanine nucleotide binding proteins that participate in the control of eukaryotic cell proliferation. Ras proteins are modified posttranslationally by transfer of a farnesyl moiety to specific cysteine residues. This transformation is mediated by a farnesyl:protein transferase (farnesyltransferase). Farnesylation is a prerequisite for oncogenic transformation. There is a convincing body of evidence indicating that inhibition of Ras farnesylation is an important point for pharmacological intervention in Ras function. We will 1) Design and synthesize novel inhibitors of farnesyltransfer- ase, and 2) evaluate the new compounds as inhibitors of farnesyltransferase in an in vitro assay. The compounds developed in these studies will greatly increase our knowledge of the structure-activity relationships for farnesyltransferase inhibitors and may lead to the development of new cancer therapeutics.

* Information listed above is at the time of submission. *

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