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Mechanism and Kinetics of HIV-1 Protease Activation [PDF]

open access: yesViruses
The HIV-1 protease is a critical enzyme for viral replication. Because protease activity is necessary to generate mature infectious virions, it is a primary target of antiretroviral treatment.
Caroline O. Tabler, John C. Tilton
doaj   +4 more sources

Drug Reprofiling to Identify Potential HIV-1 Protease Inhibitors [PDF]

open access: yesMolecules, 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   +2 more sources

Subtype-Specific HIV-1 Protease and the Role of Hinge and Flap Dynamics in Drug Resistance: A Subtype C Narrative [PDF]

open access: yesViruses
The HIV-1 aspartic protease is an effective target for the treatment of HIV/AIDS. Current therapy utilizes a selection of nine protease inhibitors (PIs) in combination with other classes of antiretroviral drugs.
Dean Sherry   +3 more
doaj   +2 more sources

Dynamozones are the most obvious sign of the evolution of conformational dynamics in HIV-1 protease [PDF]

open access: yesScientific Reports, 2023
Proteins are not static but are flexible molecules that can adopt many different conformations. The HIV-1 protease is an important target for the development of therapies to treat AIDS, due to its critical role in the viral life cycle.
Mohammad Rahimi   +2 more
doaj   +2 more sources

HIV-1 protease inhibitors and mechanisms of HIV-1's resistance. [PDF]

open access: yesGlob Health Med
Current anti-HIV drugs have significantly improved the prognosis of HIV infected patients so much so that it is now considered a chronic disease, and adherence to medications keeps non-detectable amounts of the virus in the body. However, HIV is still able to generate drug resistance substitutions.
Das D.
europepmc   +3 more sources

Molecular Basis for Drug Resistance in HIV-1 Protease

open access: yesViruses, 2010
HIV-1 protease is one of the major antiviral targets in the treatment of patients infected with HIV-1. The nine FDA approved HIV-1 protease inhibitors were developed with extensive use of structure-based drug design, thus the atomic details of how the ...
Celia A. Schiffer   +12 more
doaj   +3 more sources

Premature Activation of the HIV-1 Protease Is Influenced by Polymorphisms in the Hinge Region [PDF]

open access: yesViruses
HIV-1 protease inhibitors are an essential component of antiretroviral therapy. However, drug resistance is a pervasive issue motivating a persistent search for novel therapies.
Caroline O. Tabler   +4 more
doaj   +2 more sources

Infected cell killing by HIV-1 protease promotes NF-kappaB dependent HIV-1 replication. [PDF]

open access: yesPLoS ONE, 2008
Acute HIV-1 infection of CD4 T cells often results in apoptotic death of infected cells, yet it is unclear what evolutionary advantage this offers to HIV-1.
Gary D Bren   +6 more
doaj   +1 more source

Acquired HIV-1 Protease Conformational Flexibility Associated with Lopinavir Failure May Shape the Outcome of Darunavir Therapy after Antiretroviral Therapy Switch

open access: yesBiomolecules, 2021
Understanding the underlying molecular interaction during a therapy switch from lopinavir (LPV) to darunavir (DRV) is essential to achieve long-term virological suppression.
Simeon Eche   +3 more
doaj   +1 more source

A folding inhibitor of the HIV‐1 protease [PDF]

open access: yesProteins: Structure, Function, and Bioinformatics, 2005
AbstractBecause the human immunodeficiency virus type 1 protease (HIV‐1‐PR) is an essential enzyme in the viral life cycle, its inhibition can control AIDS. The folding of single‐domain proteins, like each of the monomers forming the HIV‐1‐PR homodimer, is controlled by local elementary structures (LES, folding units stabilized by strongly interacting,
R. A. Broglia   +5 more
openaire   +4 more sources

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