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| {{STRUCTURE_1iyk| PDB=1iyk | SCENE= }} | | {{STRUCTURE_1iyk| PDB=1iyk | SCENE= }} |
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| '''CRYSTAL STRUCTURE OF CANDIDA ALBICANS N-MYRISTOYLTRANSFERASE WITH MYRISTOYL-COA AND PEPTIDIC INHIBITOR'''
| | ===CRYSTAL STRUCTURE OF CANDIDA ALBICANS N-MYRISTOYLTRANSFERASE WITH MYRISTOYL-COA AND PEPTIDIC INHIBITOR=== |
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| ==Overview==
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| 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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_12401496}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 12401496 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_12401496}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Winkler, F K.]] | | [[Category: Winkler, F K.]] |
| [[Category: Transferase]] | | [[Category: Transferase]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 20:35:13 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 14:13:45 2008'' |
