Literature DB >> 10708858

Targeting the HIV-protease in AIDS therapy: a current clinical perspective.

A G Tomasselli1, R L Heinrikson.   

Abstract

This review deals with clinical applications of compounds that inhibit the action of the protease encoded within the genome of human immunodeficiency virus (HIV). The HIV-protease is essential for viral maturation and represents an important therapeutic target in the fight against AIDS. Following a brief overview of the enzyme structure and function, the article focuses on a number of peptide and non-peptide based HIV-protease inhibitors that are in current clinical use. These drugs are discussed both with respect to their efficacy in treatment of AIDS, and to problems related to insurgence of viral resistance and side effects seen to date in patient populations.

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Year:  2000        PMID： 10708858     DOI： 10.1016/s0167-4838(99)00273-3

Source DB:  PubMed          Journal:  Biochim Biophys Acta        ISSN： 0006-3002


  19 in total

1.  Structure-based phenotyping predicts HIV-1 protease inhibitor resistance.

Authors:  Mark D Shenderovich; Ron M Kagan; Peter N R Heseltine; Kal Ramnarayan
Journal:  Protein Sci       Date:  2003-08       Impact factor: 6.725

2.  Design of HIV-1-PR inhibitors that do not create resistance: blocking the folding of single monomers.

Authors:  Ricardo A Broglia; Guido Tiana; Ludovico Sutto; Davide Provasi; Fabio Simona
Journal:  Protein Sci       Date:  2005-10       Impact factor: 6.725

3.  Synergistic interactions of the antiretroviral protease inhibitors saquinavir and ritonavir with chloroquine and mefloquine against Plasmodium falciparum in vitro.

Authors:  T S Skinner-Adams; K T Andrews; L Melville; J McCarthy; D L Gardiner
Journal:  Antimicrob Agents Chemother       Date:  2006-11-06       Impact factor: 5.191

4.  Novel method for probing the specificity binding profile of ligands: applications to HIV protease.

Authors:  Woody Sherman; Bruce Tidor
Journal:  Chem Biol Drug Des       Date:  2008-03-31       Impact factor: 2.817

5.  Protease Inhibitors for Patients With HIV-1 Infection: A Comparative Overview.

Authors:  Peter J Hughes; Erika Cretton-Scott; Ami Teague; Terri M Wensel
Journal:  P T       Date:  2011-06

6.  Cell-based fluorescence assay for human immunodeficiency virus type 1 protease activity.

Authors:  K Lindsten; T Uhlíková; J Konvalinka; M G Masucci; N P Dantuma
Journal:  Antimicrob Agents Chemother       Date:  2001-09       Impact factor: 5.191

7.  Insight into the folding inhibition of the HIV-1 protease by a small peptide.

Authors:  Massimiliano Bonomi; Francesco L Gervasio; Guido Tiana; Davide Provasi; Ricardo A Broglia; Michele Parrinello
Journal:  Biophys J       Date:  2007-06-15       Impact factor: 4.033

Review 8.  Resilience to resistance of HIV-1 protease inhibitors: profile of darunavir.

Authors:  Eric Lefebvre; Celia A Schiffer
Journal:  AIDS Rev       Date:  2008 Jul-Sep       Impact factor: 2.500

9.  Multiple routes and milestones in the folding of HIV-1 protease monomer.

Authors:  Massimiliano Bonomi; Alessandro Barducci; Francesco L Gervasio; Michele Parrinello
Journal:  PLoS One       Date:  2010-10-13       Impact factor: 3.240

10.  Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.

Authors:  Matthew D Cullen; York-Fong Cheung; Miles D Houslay; Tracy L Hartman; Karen M Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Journal:  Bioorg Med Chem Lett       Date:  2007-12-14       Impact factor: 2.823
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