Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase.
Publication
, Journal Article
Devadas, B; Freeman, SK; McWherter, CA; Kishore, NS; Lodge, JK; Jackson-Machelski, E; Gordon, JI; Sikorski, JA
Published in: J Med Chem
March 12, 1998
A new class of biologically active nonpeptidic inhibitors of Candida albicans NMT has been synthesized starting from the octapeptide ALYASKLS-NH2 (2). The synthetic strategy entailed the preparation of novel protected Ser-Lys mimics 9 and 12 from (S)- or (R)-3-iodotyrosine and then grafting key enzyme recognition elements in a stepwise manner. Like 2, compounds 16, 17, and 18 are competitive Candida NMT inhibitors that bind to the peptide recognition site of the enzyme. Moreover, 16-18 have an affinity comparable to that of 2 even though they are devoid of peptide bonds. In contrast to 2, these nonpeptidic inhibitors exhibit antifungal activity.
Duke Scholars
Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
March 12, 1998
Volume
41
Issue
6
Start / End Page
996 / 1000
Location
United States
Related Subject Headings
- Stereoisomerism
- Medicinal & Biomolecular Chemistry
- Imidazoles
- Humans
- Enzyme Inhibitors
- Candida albicans
- Antifungal Agents
- Acyltransferases
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
Citation
APA
Chicago
ICMJE
MLA
NLM
Devadas, B., Freeman, S. K., McWherter, C. A., Kishore, N. S., Lodge, J. K., Jackson-Machelski, E., … Sikorski, J. A. (1998). Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase. J Med Chem, 41(6), 996–1000. https://doi.org/10.1021/jm980001q
Devadas, B., S. K. Freeman, C. A. McWherter, N. S. Kishore, J. K. Lodge, E. Jackson-Machelski, J. I. Gordon, and J. A. Sikorski. “Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase.” J Med Chem 41, no. 6 (March 12, 1998): 996–1000. https://doi.org/10.1021/jm980001q.
Devadas B, Freeman SK, McWherter CA, Kishore NS, Lodge JK, Jackson-Machelski E, et al. Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase. J Med Chem. 1998 Mar 12;41(6):996–1000.
Devadas, B., et al. “Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase.” J Med Chem, vol. 41, no. 6, Mar. 1998, pp. 996–1000. Pubmed, doi:10.1021/jm980001q.
Devadas B, Freeman SK, McWherter CA, Kishore NS, Lodge JK, Jackson-Machelski E, Gordon JI, Sikorski JA. Novel biologically active nonpeptidic inhibitors of myristoylCoA:protein N-myristoyltransferase. J Med Chem. 1998 Mar 12;41(6):996–1000.
Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
March 12, 1998
Volume
41
Issue
6
Start / End Page
996 / 1000
Location
United States
Related Subject Headings
- Stereoisomerism
- Medicinal & Biomolecular Chemistry
- Imidazoles
- Humans
- Enzyme Inhibitors
- Candida albicans
- Antifungal Agents
- Acyltransferases
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry