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The 80's loop (residues 78 to 85) is important for the differential activity of retroviral proteases.

Abstract：

:The abundance of structural data available for retroviral proteases affords a unique opportunity to investigate structure activity relationships. Our approach attempts to genetically engineer an HIV (human immunodeficiency virus)-1 protease that is functionally equivalent to the HIV-2 and the SIV (simian immunodeficiency virus) enzymes and conversely to engineer an HIV-2 protease that is functionally equivalent to the HIV-1 enzyme. For this purpose, the HIV-2 and SIV proteases were cloned and characterized in an Escherichia coli (E. coli) assay system along with 33 engineered HIV-1 and HIV-2 enzymes. The results of these experiments show that a relatively large S1 or S1' subsite volume, which is likely determined by the conformation of the 80's loop (residues 78 to 85), is necessary to fully accommodate the HIV-1 protease specificity site AETF*YCDG (the asterisk indicates the location scissile bond) during productive binding.

journal_name

J Mol Biol

journal_title

Journal of molecular biology

authors

Stebbins J,Towler EM,Tennant MG,Deckman IC,Debouck C

doi

10.1006/jmbi.1997.0891

subject

Has Abstract

pub_date

1997-04-04 00:00:00

pages

467-75

issue

3

eissn

0022-2836

issn

1089-8638

pii

S0022-2836(97)90891-3

journal_volume

267

pub_type

杂志文章

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