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| [[Image:2hfj.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_2hfj| PDB=2hfj | SCENE= }} | | {{STRUCTURE_2hfj| PDB=2hfj | SCENE= }} |
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| '''Pikromycin thioesterase with covalent pentaketide affinity label'''
| | ===Pikromycin thioesterase with covalent pentaketide affinity label=== |
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| ==Overview==
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| Polyketides are a class of biologically active microbial and plant-derived metabolites that possess a high degree of structural and functional diversity and include many human therapeutics, among them anti-infective and anti-cancer drugs, growth promoters and anti-parasitic agents. The macrolide antibiotics, characterized by a glycoside-linked macrolactone, constitute an important class of polyketides, including erythromycin and the natural ketolide anti-infective agent pikromycin. Here we describe new mechanistic details of macrolactone ring formation catalyzed by the pikromycin polyketide synthase thioesterase domain from Streptomyces venezuelae. A pentaketide phosphonate mimic of the final pikromycin linear chain-elongation intermediate was synthesized and shown to be an active site affinity label. The crystal structures of the affinity-labeled enzyme and of a 12-membered-ring macrolactone product complex suggest a mechanism for cyclization in which a hydrophilic barrier in the enzyme and structural restraints of the substrate induce a curled conformation to direct macrolactone ring formation.
| | The line below this paragraph, {{ABSTRACT_PUBMED_16969372}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 16969372 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_16969372}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Alpha/beta hydrolase]] | | [[Category: Alpha/beta hydrolase]] |
| [[Category: Thioesterase]] | | [[Category: Thioesterase]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:13:54 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:09:43 2008'' |
