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2bpw

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==Overview==
==Overview==
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The ability to replace an inhibitor bound to the HIV-1 protease in single, crystals with other potent inhibitors offers the possibility of, investigating a series of protease inhibitors rapidly and conveniently, with the use of X-ray crystallography. This approach affords a fast, turnaround of structural information for iterative rational drug designs, and obviates the need for studying the complex structures by, co-crystallization. The replacement approach has been successfully used, with single crystals of the HIV-1 protease complexed with a weak, inhibitor. The structures of the complexes obtained by the replacement, method are similar to those determined by co-crystallization.
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The ability to replace an inhibitor bound to the HIV-1 protease in single crystals with other potent inhibitors offers the possibility of investigating a series of protease inhibitors rapidly and conveniently with the use of X-ray crystallography. This approach affords a fast turnaround of structural information for iterative rational drug designs and obviates the need for studying the complex structures by co-crystallization. The replacement approach has been successfully used with single crystals of the HIV-1 protease complexed with a weak inhibitor. The structures of the complexes obtained by the replacement method are similar to those determined by co-crystallization.
==About this Structure==
==About this Structure==
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[[Category: hydrolase]]
[[Category: hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:16:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:40:19 2008''

Revision as of 14:40, 21 February 2008


2bpw, resolution 2.8Å

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HIV-1 PROTEASE-INHIBITOR COMPLEX

Overview

The ability to replace an inhibitor bound to the HIV-1 protease in single crystals with other potent inhibitors offers the possibility of investigating a series of protease inhibitors rapidly and conveniently with the use of X-ray crystallography. This approach affords a fast turnaround of structural information for iterative rational drug designs and obviates the need for studying the complex structures by co-crystallization. The replacement approach has been successfully used with single crystals of the HIV-1 protease complexed with a weak inhibitor. The structures of the complexes obtained by the replacement method are similar to those determined by co-crystallization.

About this Structure

2BPW is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Active as Deleted entry, with EC number 3.4.13.16 Full crystallographic information is available from OCA.

Reference

Rapid X-ray diffraction analysis of HIV-1 protease-inhibitor complexes: inhibitor exchange in single crystals of the bound enzyme., Munshi S, Chen Z, Li Y, Olsen DB, Fraley ME, Hungate RW, Kuo LC, Acta Crystallogr D Biol Crystallogr. 1998 Sep 1;54(Pt 5):1053-60. PMID:9757136

Page seeded by OCA on Thu Feb 21 16:40:19 2008

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