1w75: Difference between revisions
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==Overview== | ==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 . | 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== | ==About this Structure== | ||
1W75 is a | 1W75 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Torpedo_californica Torpedo californica] with NAG as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1W75 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: synapse]] | [[Category: synapse]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 15:23:48 2007'' | ||
