1mar

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[[Image:1mar.gif|left|200px]]
[[Image:1mar.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1mar |SIZE=350|CAPTION= <scene name='initialview01'>1mar</scene>, resolution 1.8&Aring;
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The line below this paragraph, containing "STRUCTURE_1mar", 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=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene>, <scene name='pdbligand=ZST:3,4-DIHYDRO-4-OXO-3-((5-TRIFLUOROMETHYL-2-BENZOTHIAZOLYL)METHYL)-1-PHTHALAZINE+ACETIC+ACID'>ZST</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/Aldehyde_reductase Aldehyde reductase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.1.1.21 1.1.1.21] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1mar| PDB=1mar | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1mar FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mar OCA], [http://www.ebi.ac.uk/pdbsum/1mar PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1mar RCSB]</span>
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}}
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'''REFINED 1.8 ANGSTROMS STRUCTURE OF HUMAN ALDOSE REDUCTASE COMPLEXED WITH THE POTENT INHIBITOR ZOPOLRESTAT'''
'''REFINED 1.8 ANGSTROMS STRUCTURE OF HUMAN ALDOSE REDUCTASE COMPLEXED WITH THE POTENT INHIBITOR ZOPOLRESTAT'''
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[[Category: Quiocho, F A.]]
[[Category: Quiocho, F A.]]
[[Category: Wilson, D K.]]
[[Category: Wilson, D K.]]
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[[Category: oxidoreductase(nadp)]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:50:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:13:39 2008''
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Revision as of 21:50, 2 May 2008

Image:1mar.gif

Template:STRUCTURE 1mar

REFINED 1.8 ANGSTROMS STRUCTURE OF HUMAN ALDOSE REDUCTASE COMPLEXED WITH THE POTENT INHIBITOR ZOPOLRESTAT


Overview

As the action of aldose reductase (EC 1.1.1.21) is believed to be linked to the pathogenesis of diabetic complications affecting the nervous, renal, and visual systems, the development of therapeutic agents has attracted intense effort. We report the refined 1.8 A x-ray structure of the human holoenzyme complexed with zopolrestat, one of the most potent noncompetitive inhibitors. The zopolrestat fits snugly in the hydrophobic active site pocket and induces a hinge-flap motion of two peptide segments that closes the pocket. Excellent complementarity and affinity are achieved on inhibitor binding by the formation of 110 contacts (< or = 4 A) with 15 residues (10 hydrophobic), 13 with the NADPH coenzyme and 9 with four water molecules. The structure is key to understanding the mode of action of this class of inhibitors and for rational design of better therapeutics.

About this Structure

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

Reference

Refined 1.8 A structure of human aldose reductase complexed with the potent inhibitor zopolrestat., Wilson DK, Tarle I, Petrash JM, Quiocho FA, Proc Natl Acad Sci U S A. 1993 Nov 1;90(21):9847-51. PMID:8234324 Page seeded by OCA on Sat May 3 00:50:01 2008

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