Ultra-fast analysis of plasma and intracellular levels of HIV protease inhibitors in children: a clinical application of MALDI mass spectrometry. [PDF]
PLoS ONE, 2010 HIV protease inhibitors must penetrate into cells to exert their action. Differences in the intracellular pharmacokinetics of these drugs may explain why some patients fail on therapy or suffer from drug toxicity.
Jeroen J A van Kampen +10 more
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Lipopeptides as dimerization inhibitors of HIV-1 protease [PDF]
, 1999 In AIDS therapy, attempts have been made to inhibit the virus-encoded enzymes, e.g, HIV-1 protease, using active site-directed inhibitors. This approach is questionable, however, due to virus mutations and the high toxicity of the drugs, An alternative ...
Schramm, W. +5 more
core +1 more source
Rapid enzymatic test for phenotypic HIV protease drug resistance [PDF]
, 2003 A phenotypic resistance test based on recombinant expression of the active HIV protease in E. coli from patient blood samples was developed. The protease is purified in a rapid onestep procedure as active enzyme and tested for inhibition by five selected
Machleidt, Werner +5 more
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Higher Desolvation Energy Reduces Molecular Recognition in Multi-Drug Resistant HIV-1 Protease
Biology, 2012 Designing HIV-1 protease inhibitors that overcome drug-resistance is still a challenging task. In this study, four clinical isolates of multi-drug resistant HIV-1 proteases that exhibit resistance to all the US FDA-approved HIV-1 protease inhibitors and ...
Ladislau C. Kovari +6 more
doaj +1 more source
Naturally Occurring Mutations in HIV-1 Protease Gene Among People Living With HIV
Acta Medica Iranica, 2023 The emergence of resistance to antiretroviral drugs is the main problem in their long-term efficacy and by considering the wide use of protease inhibitors (PIs), monitoring drug resistance mutations is necessary.
Zahra Hasanshahi +6 more
doaj +1 more source
Protease mediated maturation of HIV: Inhibitors of protease and the maturation process [PDF]
, 2012 Protease-mediated maturation of HIV-1 virus particles is essential for virus infectivity. Maturation occurs concomitant with immature virus particle release and is mediated by the viral protease (PR), which sequentially cleaves the Gag and Gag-Pol ...
Catherine S. Adamson +1 more
core +1 more source
Sensors, 2013 To effectively fight against the human immunodeficiency virus infection/ acquired immunodeficiency syndrome (HIV/AIDS) epidemic, ongoing development of novel HIV protease inhibitors is required.
Rok Gaber +3 more
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Drug Reprofiling to Identify Potential HIV-1 Protease Inhibitors
Molecules, 2023 The use of protease inhibitors in human immunodeficiency virus type 1 (HIV-1) treatment is limited by adverse effects, including metabolic complications. To address these challenges, efforts are underway in the pursuit of more potent and less toxic HIV-1
Sunday N. Okafor +7 more
doaj +1 more source
The role of the HIV-1 protease substrate in therapy resistance [PDF]
, 2015 In Switzerland and Germany up to a half of the first-line regimens include protease inhibitors (PIs) [1, 2]. Although in the Swiss HIV Cohort Study (SHCS) most patients under antiretroviral therapy (ART) have suppressed viral loads [3], every third ...
Kletenkov, Konstantin
core +1 more source
Phenotypic hypersusceptibility to multiple protease inhibitors and low replicative capacity in patients who are chronically infected with human immunodeficiency virus type 1 [PDF]
, 2005 Increased susceptibility to the protease inhibitors saquinavir and amprenavir has been observed in human immunodeficiency virus type 1 (HIV-1) with specific mutations in protease (V82T and N88S).
Wrin, T +7 more
core +1 more source