1w75

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[[Image:1w75.gif|left|200px]]
[[Image:1w75.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1w75 |SIZE=350|CAPTION= <scene name='initialview01'>1w75</scene>, resolution 2.400&Aring;
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The line below this paragraph, containing "STRUCTURE_1w75", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Nag+Binding+Site+For+Chain+B'>AC1</scene>
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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=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</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/Acetylcholinesterase Acetylcholinesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.7 3.1.1.7] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1w75| PDB=1w75 | 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=1w75 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1w75 OCA], [http://www.ebi.ac.uk/pdbsum/1w75 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1w75 RCSB]</span>
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}}
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'''NATIVE ORTHORHOMBIC FORM OF TORPEDO CALIFORNICA ACETYLCHOLINESTERASE (ACHE)'''
'''NATIVE ORTHORHOMBIC FORM OF TORPEDO CALIFORNICA ACETYLCHOLINESTERASE (ACHE)'''
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[[Category: alzheimer's disease]]
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[[Category: Alzheimer's disease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 13:14:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:32:06 2008''
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Revision as of 10:15, 3 May 2008

Image:1w75.gif

Template:STRUCTURE 1w75

NATIVE ORTHORHOMBIC FORM OF TORPEDO CALIFORNICA ACETYLCHOLINESTERASE (ACHE)


Overview

Bifunctional derivatives of the alkaloid galanthamine, designed to interact with both the active site of the enzyme acetylcholinesterase (AChE) and its peripheral cation binding site, have been assayed with Torpedo californica AChE (TcAChE), and the three-dimensional structures of their complexes with the enzyme have been solved by X-ray crystallography. Differences were noted between the IC(50) values obtained for TcAChE and those for Electrophorus electricus AChE. These differences are ascribed to sequence differences in one or two residues lining the active-site gorge of the enzyme. The binding of one of the inhibitors disrupts the native conformation of one wall of the gorge, formed by the loop Trp279-Phe290. It is proposed that flexibility of this loop may permit the binding of inhibitors such as galanthamine, which are too bulky to penetrate the narrow neck of the gorge formed by Tyr121 and Phe330 as seen in the crystal structure.

About this Structure

1W75 is a Single protein structure of sequence from Torpedo californica. Full crystallographic information is available from OCA.

Reference

The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design., Greenblatt HM, Guillou C, Guenard D, Argaman A, Botti S, Badet B, Thal C, Silman I, Sussman JL, J Am Chem Soc. 2004 Dec 1;126(47):15405-11. PMID:15563167 Page seeded by OCA on Sat May 3 13:14:57 2008

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