Novel reverse-turn mimics inhibit farnesyl transferase

Liu, R., Dong, D. L., Sherlock, R., Nestler, H. P., Gennari, C., Mielgo, A., Scolastico, C. (March 1999) Novel reverse-turn mimics inhibit farnesyl transferase. Bioorganic and Medicinal Chemistry Letters , 9 (6). pp. 847-52. ISSN 0960-894X (Print)

URL: http://www.ncbi.nlm.nih.gov/pubmed/10206548
DOI: 10.1016/S0960-894X(99)00094-3

Abstract

Reverse-turn inducing bicyclic lactams were incorporated into the substrate sequence recognized by farnesyl transferase to create inhibitors of RAS farnesylation. While the free peptides did not show any effect on the farnesylation, their Fmoc-protected counterparts impede the transformation of RAS with IC50's in the low micromolar range.

Item Type: Paper
Uncontrolled Keywords: Alkyl and Aryl Transferases/ antagonists & inhibitors Dose-Response Relationship, Drug Inhibitory Concentration 50 Kinetics Lactams/ chemical synthesis/ metabolism Models, Chemical Protein Structure, Secondary Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.
Subjects: bioinformatics > genomics and proteomics > genetics & nucleic acid processing > protein structure, function, modification
bioinformatics > genomics and proteomics > genetics & nucleic acid processing > DNA, RNA structure, function, modification > genes, structure and function > genes: types > RAS
bioinformatics > genomics and proteomics > genetics & nucleic acid processing > DNA, RNA structure, function, modification > genes, structure and function > genes: types > p21
CSHL Authors:
Communities: CSHL labs > Nestler lab
CSHL labs > Wigler lab
Depositing User: Kathleen Darby
Date: 22 March 1999
Date Deposited: 28 Apr 2014 15:21
Last Modified: 07 May 2014 12:54
Related URLs:
URI: http://repository.cshl.edu/id/eprint/29810

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