1a9m

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[[Image:1a9m.gif|left|200px]]
[[Image:1a9m.gif|left|200px]]
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{{Structure
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|PDB= 1a9m |SIZE=350|CAPTION= <scene name='initialview01'>1a9m</scene>, resolution 2.3&Aring;
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The line below this paragraph, containing "STRUCTURE_1a9m", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=U0E:N-[[1-[N-ACETAMIDYL]-[1-CYCLOHEXYLMETHYL-2-HYDROXY-4-ISOPROPYL]-BUT-4-YL]-CARBONYL]-GLUTAMINYL-ARGINYL-AMIDE'>U0E</scene>
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{{STRUCTURE_1a9m| PDB=1a9m | 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=1a9m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1a9m OCA], [http://www.ebi.ac.uk/pdbsum/1a9m PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1a9m RCSB]</span>
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'''G48H MUTANT OF HIV-1 PROTEASE IN COMPLEX WITH A PEPTIDIC INHIBITOR U-89360E'''
'''G48H MUTANT OF HIV-1 PROTEASE IN COMPLEX WITH A PEPTIDIC INHIBITOR U-89360E'''
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[[Category: Tang, J.]]
[[Category: Tang, J.]]
[[Category: Zhang, X J.]]
[[Category: Zhang, X J.]]
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[[Category: aspartyl protease]]
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[[Category: Aspartyl protease]]
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[[Category: drug resistant]]
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[[Category: Drug resistant]]
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[[Category: mutation]]
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[[Category: Mutation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 10:01:02 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 18:36:06 2008''
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Revision as of 07:01, 2 May 2008

Template:STRUCTURE 1a9m

G48H MUTANT OF HIV-1 PROTEASE IN COMPLEX WITH A PEPTIDIC INHIBITOR U-89360E


Overview

The crystal structure of human immunodeficiency virus type 1 (HIV-1) protease mutant G48H with peptidic inhibitor U-89360E is described. Comparison with wild-type protease-inhibitor complex shows that mutation of flap residue 48 to histidine allows stabilizing van der Waals contacts between the side chains of His48 and Phe53 as well as between His48 and the P2' and P3' inhibitor subsites. The flap region is less mobile than in the wild-type enzyme. A model of saquinavir-resistant mutant protease G48V in complex with saquinavir predicts interactions similar to those found in the G48H crystal. Energetic calculations confirm the similarity of the His48 and Val48 interactions.

About this Structure

1A9M is a Single protein structure of sequence from Human immunodeficiency virus. Full crystallographic information is available from OCA.

Reference

Structure of a G48H mutant of HIV-1 protease explains how glycine-48 replacements produce mutants resistant to inhibitor drugs., Hong L, Zhang XJ, Foundling S, Hartsuck JA, Tang J, FEBS Lett. 1997 Dec 22;420(1):11-6. PMID:9450540 Page seeded by OCA on Fri May 2 10:01:02 2008

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