1u2y: Difference between revisions

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[[Image:1u2y.jpg|left|200px]]
{{Seed}}
[[Image:1u2y.png|left|200px]]


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{{STRUCTURE_1u2y|  PDB=1u2y  |  SCENE=  }}  
{{STRUCTURE_1u2y|  PDB=1u2y  |  SCENE=  }}  


'''In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing D-gluconhydroximo-1,5-lactam'''
===In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing D-gluconhydroximo-1,5-lactam===




==Overview==
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A new approach for the discovery and subsequent structural elucidation of oligosaccharide-based inhibitors of alpha-amylases based upon autoglucosylation of known alpha-glucosidase inhibitors is presented. This concept, highly analogous to what is hypothesized to occur with acarbose, is demonstrated with the known alpha-glucosidase inhibitor, d-gluconohydroximino-1,5-lactam. This was transformed from an inhibitor of human pancreatic alpha-amylase with a K(i) value of 18 mm to a trisaccharide analogue with a K(i) value of 25 mum. The three-dimensional structure of this complex was determined by x-ray crystallography and represents the first such structure determined with this class of inhibitors in any alpha-glycosidase. This approach to the discovery and structural analysis of amylase inhibitors should be generally applicable to other endoglucosidases and readily adaptable to a high throughput format.
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{{ABSTRACT_PUBMED_15304511}}


==About this Structure==
==About this Structure==
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[[Category: Human pancreatic alpha-amylase]]
[[Category: Human pancreatic alpha-amylase]]
[[Category: Inhibitor]]
[[Category: Inhibitor]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 10:41:34 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 18:23:37 2008''

Revision as of 15:23, 27 July 2008

File:1u2y.png

Template:STRUCTURE 1u2y

In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing D-gluconhydroximo-1,5-lactam

Template:ABSTRACT PUBMED 15304511

About this Structure

1U2Y is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

In situ extension as an approach for identifying novel alpha-amylase inhibitors., Numao S, Damager I, Li C, Wrodnigg TM, Begum A, Overall CM, Brayer GD, Withers SG, J Biol Chem. 2004 Nov 12;279(46):48282-91. Epub 2004 Aug 10. PMID:15304511

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