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Potent inhibitor of N-myristoylation: a novel molecular target for cancer.

Authors :
Shrivastav A
Pasha MK
Selvakumar P
Gowda S
Olson DJ
Ross AR
Dimmock JR
Sharma RK
Source :
Cancer research [Cancer Res] 2003 Nov 15; Vol. 63 (22), pp. 7975-8.
Publication Year :
2003

Abstract

N-myristoyltransferase (NMT) is an essential eukaryotic enzyme that catalyzes the cotranslational and/or posttranslational transfer of myristate to the NH(2) terminus of the glycine residue of a number of important proteins that have diverse biological functions and thus have been proposed as potential targets for chemotherapeutic drug design. Earlier, we demonstrated that NMT is more active in colonic epithelial neoplasms than in corresponding normal-appearing colonic tissue. Furthermore, an increased expression of NMT was also observed in gallbladder carcinoma. In the present study, we report a novel protein inhibitor of NMT. This protein caused a potent concentration-dependent inhibition of human NMT with half-maximal inhibition at 4.5 +/- 0.35 nM. This study will serve as a template for further investigations in the area of protein myristoylation.

Details

Language :
English
ISSN :
0008-5472
Volume :
63
Issue :
22
Database :
MEDLINE
Journal :
Cancer research
Publication Type :
Academic Journal
Accession number :
14633729