Results 11 to 20 of about 136,889 (307)

Lipopeptides as Dimerization Inhibitors of HIV-1 Protease [PDF]

Biological Chemistry, 1999
AbstractIn 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 method to inhibit the dimeric HIV protease is the targeting of the interface region of the ...
Schramm, H. J., de Rosny, E., Reboud-Ravaux, M., Büttner, J., Dick, A., Schramm, W.   +5 more
openaire   +5 more sources

Predicting HIV-1 Protease Cleavage Sites With Positive-Unlabeled Learning

Frontiers in Genetics, 2021
Understanding the substrate specificity of HIV-1 protease plays an essential role in the prevention of HIV infection. A variety of computational models have thus been developed to predict substrate sites that are cleaved by HIV-1 protease, but most of ...
Zhenfeng Li, Lun Hu, Zehai Tang, Cheng Zhao   +3 more
doaj   +1 more source

HIV-1 protease-induced apoptosis [PDF]

Retrovirology, 2014
Apoptosis is one of the presumptive causes of CD4+ T cell depletion during HIV infection and progression to AIDS. However, the precise role of HIV-1 in this process remains unexplained. HIV-1 protease (PR) has been suggested as a possible factor, but a direct link between HIV-1 PR enzymatic activity and apoptosis has not been established.Here, we show ...
Rumlová, Michaela, Křížová, Ivana, Keprová, Alena, Hadravová, Romana, Doležal, Michal, Strohalmová, Karolína, Pichová, Iva, Hájek, Miroslav, Ruml, Tomáš   +8 more
openaire   +2 more sources

Folded Monomer of HIV-1 Protease [PDF]

Journal of Biological Chemistry, 2001
The mature human immunodeficiency virus type 1 protease rapidly folds into an enzymatically active stable dimer, exhibiting an intricate interplay between structure formation and dimerization. We now show by NMR and sedimentation equilibrium studies that a mutant protease containing the R87K substitution (PR(R87K)) within the highly conserved Gly(86 ...
R, Ishima, R, Ghirlando, J, Tözsér, A M, Gronenborn, D A, Torchia, J M, Louis   +5 more
openaire   +2 more sources

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, Iulia A. Kovari, Joseph S. Brunzelle, Samuel J. Reiter, Zhigang Liu, Tamaria G. Dewdney, Yong Wang   +6 more
doaj   +1 more source

Liquid Chromatography-Mass Spectrometry Metabolomic Analysis of <i>Terminalia ferdinandiana</i> Exell. Fruit Extracts That Inhibit HIV-1 Cell Infection, HIV-1 Reverse Transcriptase and HIV-1 Protease. [PDF]

Molecules
The emergence of HIV strains resistant to the current anti-retroviral drugs has necessitated the search for new anti-retroviral medications. Methanolic and aqueous T.
Cock IE, Matthews B, Basson AE.
europepmc   +2 more sources

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, Hoffmann, D., Assfalg-Machleidt, Irmgard, Helm, K. von der, Nitschko, H., Koszinowski, U.   +5 more
core   +1 more source

HIV-1 Protease Inhibitors [PDF]

Clinical Infectious Diseases, 2000
Treatment of human immunodeficiency virus type 1 (HIV-1) infection with regimens that include protease inhibitors (PIs) has contributed to marked improvements in HIV-related disease progression and mortality. Five PIs are approved by the US Food and Drug Administration and have potent activity in vitro.
openaire   +2 more sources

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

Probing the Pharmacological Binding Properties, and Reactivity of Selective Phytochemicals as Potential HIV-1 protease Inhibitors

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
doaj   +1 more source