1u2y
From Proteopedia
(New page: 200px<br /> <applet load="1u2y" size="450" color="white" frame="true" align="right" spinBox="true" caption="1u2y, resolution 1.95Å" /> '''In situ extension a...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:1u2y. | + | [[Image:1u2y.jpg|left|200px]]<br /><applet load="1u2y" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1u2y" size=" | + | |
caption="1u2y, resolution 1.95Å" /> | caption="1u2y, resolution 1.95Å" /> | ||
'''In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing D-gluconhydroximo-1,5-lactam'''<br /> | '''In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing D-gluconhydroximo-1,5-lactam'''<br /> | ||
| Line 8: | Line 7: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1U2Y is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NAG, CA, CL and GOX as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Alpha-amylase Alpha-amylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.1 3.2.1.1] Full crystallographic information is available from [http:// | + | 1U2Y is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NAG:'>NAG</scene>, <scene name='pdbligand=CA:'>CA</scene>, <scene name='pdbligand=CL:'>CL</scene> and <scene name='pdbligand=GOX:'>GOX</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Alpha-amylase Alpha-amylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.1 3.2.1.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1U2Y OCA]. |
==Reference== | ==Reference== | ||
| Line 34: | Line 33: | ||
[[Category: inhibitor]] | [[Category: inhibitor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:59:06 2008'' |
Revision as of 14:59, 15 February 2008
|
In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing D-gluconhydroximo-1,5-lactam
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
1U2Y is a Single protein structure of sequence from Homo sapiens with , , and as ligands. Active as Alpha-amylase, with EC number 3.2.1.1 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 Fri Feb 15 16:59:06 2008
Categories: Alpha-amylase | Homo sapiens | Single protein | Begum, A. | Brayer, G.D. | Damager, I. | Li, C. | Numao, S. | Overall, C.M. | Withers, S.G. | Wrodnigg, T.M. | CA | CL | GOX | NAG | Acarbose | Enzyme mechanism | Glucosidase | Glycosidase | Human pancreatic alpha-amylase | Inhibitor
