HIV Protease: Historical Perspective and Current Research
The retroviral protease of human immunodeficiency virus (HIV) is an excellent target for antiviral inhibitors for treating HIV/AIDS. Despite the efficacy of therapy, current efforts to control the disease are undermined by the growing threat posed by ...
Irene T. Weber+2 more
doaj +1 more source
Drug Reprofiling to Identify Potential HIV-1 Protease Inhibitors
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
Ultra-fast analysis of plasma and intracellular levels of HIV protease inhibitors in children: a clinical application of MALDI mass spectrometry. [PDF]
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
doaj +1 more source
HIV protease inhibitors and obesity [PDF]
To review the current scientific literature and recent clinical trials on HIV protease inhibitors and their potential role in the pathogenesis of lipodystrophy and metabolic disorders.HIV protease inhibitor treatment may affect the normal stimulatory effect of insulin on glucose and fat storage.
Lars Berglund+2 more
openaire +3 more sources
Phenotypic hypersusceptibility to multiple protease inhibitors and low replicative capacity in patients who are chronically infected with human immunodeficiency virus type 1 [PDF]
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).
Clotet, B+7 more
core +2 more sources
Inhibition Profiling of Retroviral Protease Inhibitors Using an HIV-2 Modular System
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
doaj +1 more source
Mass spectrometry captures off-target drug binding and provides mechanistic insights into the human metalloprotease ZMPSTE24. [PDF]
Off-target binding of hydrophobic drugs can lead to unwanted side effects, either through specific or non-specific binding to unintended membrane protein targets.
Carpenter, Elisabeth P+7 more
core +2 more sources
Rapid enzymatic test for phenotypic HIV protease drug resistance [PDF]
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
Assfalg-Machleidt, Irmgard+5 more
core +1 more source
A modular system to evaluate the efficacy of protease inhibitors against HIV-2.
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
doaj +1 more source
HIV protease inhibitors and atherosclerosis [PDF]
The advent of highly active antiretroviral therapy (HAART), including the use of HIV protease inhibitors (PIs) has significantly reduced the morbidity and mortality of AIDS in HIV infected patients. Unfortunately, the adverse effects of PIs, including dyslipidemia, lipodystrophy, insulin resistance, and premature atherosclerosis, are cause for concern ...
openaire +3 more sources