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
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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
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Identification of semicarbazones, thiosemicarbazones and triazine nitriles as inhibitors of Leishmania mexicana cysteine protease CPB [PDF]
, 2013 Cysteine proteases of the papain superfamily are present in nearly all eukaryotes. They play pivotal roles in the biology of parasites and inhibition of cysteine proteases is emerging as an important strategy to combat parasitic diseases such as sleeping
Mottram, Jeremy C +5 more
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Inhibition Profiling of Retroviral Protease Inhibitors Using an HIV-2 Modular System
Viruses, 2015 Retroviral protease inhibitors (PIs) are fundamental pillars in the treatment of HIV infection and acquired immunodeficiency syndrome (AIDS). Currently used PIs are designed against HIV-1, and their effect on HIV-2 is understudied.
Mohamed Mahdi +3 more
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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
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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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A modular system to evaluate the efficacy of protease inhibitors against HIV-2.
PLoS ONE, 2014 The human immunodeficiency virus (HIV) protease is a homodimeric aspartyl protease that is crucial for the viral life-cycle, cleaving proviral polyproteins, hence creating mature protein components that are required for the formation of an infectious ...
Mohamed Mahdi +3 more
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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
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Universitas Scientiarum, 2019 The HIV-1 protease plays an essential role in the replication cycle of HIV-1; therefore there is a direct need to develop novel inhibitors of the HIV-1 protease, which can cease the viral replication.
Ammara Akhtar, Waqar Hussain, Nouman Rasool3
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