1az2

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{{Seed}}
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{{STRUCTURE_1az2| PDB=1az2 | SCENE= }}
{{STRUCTURE_1az2| PDB=1az2 | SCENE= }}
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'''CITRATE BOUND, C298A/W219Y MUTANT HUMAN ALDOSE REDUCTASE'''
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===CITRATE BOUND, C298A/W219Y MUTANT HUMAN ALDOSE REDUCTASE===
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==Overview==
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It is generally expected that only one inhibitor molecule will bind to an enzyme active site. In fact, specific drug design theories depend upon this assumption. Here, we report the binding of two molecules of an inhibitor to the same active site which we observed in the 1.8 A resolution structure of the drug Alrestatin bound to a mutant of human aldose reductase. The two molecules of Alrestatin bind to the active site in a stacked arrangement (a double-decker). This stack positions the carboxylic acid of one drug molecule near the NADP+ cofactor at a previously determined anion binding site and the carboxylic acid of the second drug molecule near the carboxy-terminal tail of the enzyme. We propose that interactions of inhibitors with the carboxy-terminal loop of aldose reductase are critical for the development of inhibitors that are able to discriminate between aldose reductase and other members of the aldo-keto reductase superfamily. This finding suggests a new direction for the introduction of specificity to aldose reductase-targeted drugs.
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(as it appears on PubMed at http://www.pubmed.gov), where 9405046 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9405046}}
==About this Structure==
==About this Structure==
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[[Category: Inhibitor binding]]
[[Category: Inhibitor binding]]
[[Category: Oxidoreductase]]
[[Category: Oxidoreductase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 10:52:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 17:53:34 2008''

Revision as of 14:53, 30 June 2008

Image:1az2.png

Template:STRUCTURE 1az2

CITRATE BOUND, C298A/W219Y MUTANT HUMAN ALDOSE REDUCTASE

Template:ABSTRACT PUBMED 9405046

About this Structure

1AZ2 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The alrestatin double-decker: binding of two inhibitor molecules to human aldose reductase reveals a new specificity determinant., Harrison DH, Bohren KM, Petsko GA, Ringe D, Gabbay KH, Biochemistry. 1997 Dec 23;36(51):16134-40. PMID:9405046

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