1u33

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[[Image:1u33.gif|left|200px]]
[[Image:1u33.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1u33 |SIZE=350|CAPTION= <scene name='initialview01'>1u33</scene>, resolution 1.95&Aring;
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The line below this paragraph, containing "STRUCTURE_1u33", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=LM2:4&#39;-O-METHYL-MALTOSYL-ALPHA+(1,4)-(Z,+3S,4S,5R,6R)-3,4,5-TRIHYDROXY-6-HYDROXYMETHYL-PIPERIDIN-2-ONE'>LM2</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PCA:PYROGLUTAMIC+ACID'>PCA</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= AMY2A ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1u33| PDB=1u33 | SCENE= }}
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|RELATEDENTRY=[[1u2y|1U2Y]], [[1u30|1U30]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1u33 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1u33 OCA], [http://www.ebi.ac.uk/pdbsum/1u33 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1u33 RCSB]</span>
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}}
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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.]]
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[[Category: acarbose]]
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[[Category: Acarbose]]
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[[Category: enzyme mechanism]]
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[[Category: Enzyme mechanism]]
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[[Category: glucosidase]]
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[[Category: Glucosidase]]
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[[Category: glycosidase]]
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[[Category: Glycosidase]]
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[[Category: human pancreatic alpha-amylase]]
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[[Category: Human pancreatic alpha-amylase]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:42:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:04:45 2008''
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Revision as of 07:42, 3 May 2008

Image:1u33.gif

Template:STRUCTURE 1u33

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

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OCA

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