PMID: 9165106Apr 25, 1997Paper

Escape mutants of HIV-1 proteinase: enzymic efficiency and susceptibility to inhibition

Biochimica Et Biophysica Acta
S I WilsonJ Kay

Abstract

Genes encoding a number of mutants of HIV-1 proteinase were sub-cloned and expressed in E. coli. The proteinases containing mutations of single residues (e.g., G48V, V82F, I84V and L90M) were purified and their catalytic efficiencies relative to that of wild-type proteinase were examined using a polyprotein (recombinant HIV-1 gag) substrate and several series of synthetic peptides based on the -Hydrophobic * Hydrophobic-, -Aromatic * Pro- and pseudo-symmetrical types of cleavage junction. The L90M proteinase showed only small changes, whereas the activity of the other mutant enzymes was compromised more severely, particularly towards substrates of the -Aromatic * Pro- and pseudo-symmetrical types. The susceptibility of the mutants and the wild-type proteinase to inhibition by eleven different compounds was compared. The L90M proteinase again showed only marginal changes in its susceptibility to all except one of the inhibitors examined. The K(i) values determined for one inhibitor (Ro31-8959) showed that its potency towards the V82F, L90M, I84V and G48V mutant proteinases respectively was 2-, 3-, 17- and 27-fold less than against the wild-type proteinase. Several of the other inhibitors examined form a systematic series with Ro...Continue Reading

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Citations

Mar 19, 1999·Protein Science : a Publication of the Protein Society·S W RickS K Burt
Jul 8, 2010·The Journal of Physical Chemistry. B·Ge-Fei HaoChang-Guo Zhan
Aug 16, 2002·European Journal of Biochemistry·Anita FehérJózsef Tözsér
Mar 19, 1999·AIDS Research and Human Retroviruses·M VaillancourtR Swanstrom
Aug 1, 1998·AIDS Research and Human Retroviruses·S C PettitR Swanstrom
Jan 27, 2011·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Rhian E WhiteColin Berry
Jan 16, 2002·Protein Science : a Publication of the Protein Society·Nancy M KingCelia A Schiffer
Dec 14, 1999·Protein Science : a Publication of the Protein Society·D XieA S Gulnik
Jan 26, 2012·Proteins·Nidhi SinghArieh Warshel
Feb 5, 2004·Clinical Microbiology and Infection : the Official Publication of the European Society of Clinical Microbiology and Infectious Diseases·C SuñéT Klimkait
Oct 23, 2015·Physical Chemistry Chemical Physics : PCCP·Zhanglong LiuGail E Fanucci
Jan 6, 1999·Antiviral Chemistry & Chemotherapy·A M VandammeE De Clercq
Sep 6, 2003·Biological Chemistry·Dieter HoffmannWerner Machleidt
Jul 9, 2004·Chembiochem : a European Journal of Chemical Biology·Lital AlfontaItamar Willner
Mar 1, 2007·Current Opinion in HIV and AIDS·Monique NijhuisCharles A B Boucher
Apr 20, 2014·The Journal of Biological Chemistry·Xi HuangGail E Fanucci
Aug 10, 2000·Journal of Acquired Immune Deficiency Syndromes : JAIDS·W J FesselT P Young
Aug 19, 2020·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Heng ZhangQun Liu
Nov 13, 2004·Journal of Medicinal Chemistry·Cynthia F ShumanU Helena Danielson
Apr 10, 2013·Biochemistry·Ian Mitchelle S de VeraGail E Fanucci

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