1tcx

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{{STRUCTURE_1tcx| PDB=1tcx | SCENE= }}
{{STRUCTURE_1tcx| PDB=1tcx | SCENE= }}
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'''HIV TRIPLE MUTANT PROTEASE COMPLEXED WITH INHIBITOR SB203386'''
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===HIV TRIPLE MUTANT PROTEASE COMPLEXED WITH INHIBITOR SB203386===
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==Overview==
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To gain greater understanding of the structural basis of human immunodeficiency virus (HIV) protease ligand specificity, we have crystallized and determined the structures of the HIV-1 protease (Val32Ile, Ile47Val, Val82Ile) triple mutant and simian immunodeficiency virus (SIV) protease in complex with SB203386, a tripeptide analogue inhibitor containing a C-terminal imidazole substituent as an amide bond isostere. SB203386 is a potent inhibitor of HIV-1 protease (Ki = 18 nM) but shows decreased inhibition of the HIV-1 protease (Val32Ile, Ile47Val, Val82Ile) triple mutant (Ki = 112 nM) and SIV protease (Ki = 960 nM). Although SB203386 binds in the active site cavity of the triple mutant in a similar fashion to its binding to the wild-type HIV-1 protease [Abdel-Meguid et al. (1994) Biochemistry 33, 11671], it binds to SIV protease in an unexpected mode showing two inhibitor molecules each binding to half of the active site. Comparison of these two structures and that of the wild-type HIV-1 protease bound to SB203386 reveals that HIV protease ligand specificity is imparted by residues outside of the catalytic pocket, which causes subtle changes in its shape. Furthermore, this work illustrates the importance of structural studies in order to understand the structure-activity relationship (SAR) between related enzymes.
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(as it appears on PubMed at http://www.pubmed.gov), where 8756683 is the PubMed ID number.
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{{ABSTRACT_PUBMED_8756683}}
==About this Structure==
==About this Structure==
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[[Category: Polyprotein]]
[[Category: Polyprotein]]
[[Category: Rna-directed dna polymerase]]
[[Category: Rna-directed dna polymerase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 04:43:20 2008''

Revision as of 01:43, 29 July 2008

Image:1tcx.png

Template:STRUCTURE 1tcx

HIV TRIPLE MUTANT PROTEASE COMPLEXED WITH INHIBITOR SB203386

Template:ABSTRACT PUBMED 8756683

About this Structure

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

Reference

Human immunodeficiency virus protease ligand specificity conferred by residues outside of the active site cavity., Hoog SS, Towler EM, Zhao B, Doyle ML, Debouck C, Abdel-Meguid SS, Biochemistry. 1996 Aug 13;35(32):10279-86. PMID:8756683

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