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| [[Image:1u1c.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_1u1c| PDB=1u1c | SCENE= }} | | {{STRUCTURE_1u1c| PDB=1u1c | SCENE= }} |
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| '''Structure of E. coli uridine phosphorylase complexed to 5-benzylacyclouridine (BAU)'''
| | ===Structure of E. coli uridine phosphorylase complexed to 5-benzylacyclouridine (BAU)=== |
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| ==Overview==
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| Uridine phosphorylase (UP) catalyzes the reversible phosphorolysis of uridine to uracil and ribose 1-phosphate and is a key enzyme in the pyrimidine-salvage pathway. Escherichia coli UP is structurally homologous to E. coli purine nucleoside phosphorylase and other members of the type I family of nucleoside phosphorylases. The structures of 5-benzylacyclouridine, 5-phenylthioacyclouridine, 5-phenylselenenylacyclouridine, 5-m-benzyloxybenzyl acyclouridine and 5-m-benzyloxybenzyl barbituric acid acyclonucleoside bound to the active site of E. coli UP have been determined, with resolutions ranging from 1.95 to 2.3 A. For all five complexes the acyclo sugar moiety binds to the active site in a conformation that mimics the ribose ring of the natural substrates. Surprisingly, the terminal hydroxyl group occupies the position of the nonessential 5'-hydroxyl substituent of the substrate rather than the 3'-hydroxyl group, which is normally required for catalytic activity. Until recently, inhibitors of UP were designed with limited structural knowledge of the active-site residues. These structures explain the basis of inhibition for this series of acyclouridine analogs and suggest possible additional avenues for future drug-design efforts. Furthermore, the studies can be extended to design inhibitors of human UP, for which no X-ray structure is available.
| | The line below this paragraph, {{ABSTRACT_PUBMED_15983408}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 15983408 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_15983408}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Pyrimidine nucleoside phosphorylase]] | | [[Category: Pyrimidine nucleoside phosphorylase]] |
| [[Category: Uridine salvage]] | | [[Category: Uridine salvage]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:37:52 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 05:58:22 2008'' |