1u30: Difference between revisions
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New page: left|200px<br /> <applet load="1u30" size="450" color="white" frame="true" align="right" spinBox="true" caption="1u30, resolution 1.90Å" /> '''In situ extension a... |
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[[Image:1u30.gif|left|200px]]<br /> | [[Image:1u30.gif|left|200px]]<br /><applet load="1u30" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1u30" size=" | |||
caption="1u30, resolution 1.90Å" /> | caption="1u30, resolution 1.90Å" /> | ||
'''In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing maltosyl-alpha (1,4)-D-gluconhydroximo-1,5-lactam'''<br /> | '''In situ extension as an approach for identifying novel alpha-amylase inhibitors, structure containing maltosyl-alpha (1,4)-D-gluconhydroximo-1,5-lactam'''<br /> | ||
==Overview== | ==Overview== | ||
A new approach for the discovery and subsequent structural elucidation of | 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== | ==About this Structure== | ||
1U30 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, LAG, 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:// | 1U30 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=LAG:'>LAG</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=1U30 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Begum, A.]] | [[Category: Begum, A.]] | ||
[[Category: Brayer, G | [[Category: Brayer, G D.]] | ||
[[Category: Damager, I.]] | [[Category: Damager, I.]] | ||
[[Category: Li, C.]] | [[Category: Li, C.]] | ||
[[Category: Numao, S.]] | [[Category: Numao, S.]] | ||
[[Category: Overall, C | [[Category: Overall, C M.]] | ||
[[Category: Withers, S | [[Category: Withers, S G.]] | ||
[[Category: Wrodnigg, T | [[Category: Wrodnigg, T M.]] | ||
[[Category: CA]] | [[Category: CA]] | ||
[[Category: CL]] | [[Category: CL]] | ||
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[[Category: inhibitor]] | [[Category: inhibitor]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:20:05 2008'' | ||
