1iyl
From Proteopedia
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'''Crystal Structure of Candida albicans N-myristoyltransferase with Non-peptidic Inhibitor''' | '''Crystal Structure of Candida albicans N-myristoyltransferase with Non-peptidic Inhibitor''' | ||
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[[Category: Sogabe, S.]] | [[Category: Sogabe, S.]] | ||
[[Category: Winkler, F K.]] | [[Category: Winkler, F K.]] | ||
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Revision as of 17:35, 2 May 2008
Crystal Structure of Candida albicans N-myristoyltransferase with Non-peptidic Inhibitor
Overview
Myristoyl-CoA:protein N-myristoyltransferase (Nmt) is a monomeric enzyme that catalyzes the transfer of the fatty acid myristate from myristoyl-CoA to the N-terminal glycine residue of a variety of eukaryotic and viral proteins. Genetic and biochemical studies have established that Nmt is an attractive target for antifungal drugs. We present here crystal structures of C. albicans Nmt complexed with two classes of inhibitor competitive for peptide substrates. One is a peptidic inhibitor designed from the peptide substrate; the other is a nonpeptidic inhibitor having a benzofuran core. Both inhibitors are bound into the same binding groove, generated by some structural rearrangements of the enzyme, with the peptidic inhibitor showing a substrate-like binding mode and the nonpeptidic inhibitor binding differently. Further, site-directed mutagenesis for C. albicans Nmt has been utilized in order to define explicitly which amino acids are critical for inhibitor binding. The results suggest that the enzyme has some degree of flexibility for substrate binding and provide valuable information for inhibitor design.
About this Structure
1IYL is a Single protein structure of sequence from Candida albicans. Full crystallographic information is available from OCA.
Reference
Crystal structures of Candida albicans N-myristoyltransferase with two distinct inhibitors., Sogabe S, Masubuchi M, Sakata K, Fukami TA, Morikami K, Shiratori Y, Ebiike H, Kawasaki K, Aoki Y, Shimma N, D'Arcy A, Winkler FK, Banner DW, Ohtsuka T, Chem Biol. 2002 Oct;9(10):1119-28. PMID:12401496 Page seeded by OCA on Fri May 2 20:35:20 2008
