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1u33
From Proteopedia
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[[Image:1u33.gif|left|200px]] | [[Image:1u33.gif|left|200px]] | ||
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'''In situ extension as an approach for identifying novel alpha-amylase inhibitors''' | '''In situ extension as an approach for identifying novel alpha-amylase inhibitors''' | ||
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[[Category: Withers, S G.]] | [[Category: Withers, S G.]] | ||
[[Category: Wrodnigg, T M.]] | [[Category: Wrodnigg, T M.]] | ||
| - | [[Category: | + | [[Category: Acarbose]] |
| - | [[Category: | + | [[Category: Enzyme mechanism]] |
| - | [[Category: | + | [[Category: Glucosidase]] |
| - | [[Category: | + | [[Category: Glycosidase]] |
| - | [[Category: | + | [[Category: Human pancreatic alpha-amylase]] |
| - | [[Category: | + | [[Category: Inhibitor]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:42:00 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 07:42, 3 May 2008
In situ extension as an approach for identifying novel alpha-amylase inhibitors
Overview
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.
About this Structure
1U33 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 Page seeded by OCA on Sat May 3 10:42:00 2008
