Results 51 to 60 of about 71,892 (273)
Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors
Viruses, 2010 The HIV-1 integrase enzyme is essential for integrating the viral DNA into the host chromosome. Infection is aborted in the absence of integration, making integrase an attractive antiviral target. Recently approved inhibitors of integrase bind tightly to
Robert Craigie, Zhiqi Yin
doaj +1 more source
The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function
mBio, 2023 Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer +14 more
doaj +1 more source
Optimal control of a delayed HIV model [PDF]
Discrete Contin. Dyn. Syst. Ser. B 23 (2018), no. 1, 443--458, 2017 We propose a model for the human immunodeficiency virus type 1 (HIV-1) infection with intracellular delay and prove the local asymptotical stability of the equilibrium points. Then we introduce a control function representing the efficiency of reverse transcriptase inhibitors and consider the pharmacological delay associated to the control. Finally, we
arxiv +1 more source
Integrase Strand Transfer Inhibitors in HIV Therapy [PDF]
Infectious Diseases and Therapy, 2013 HIV drug resistance has been one of the major obstacles to HIV eradication and has contributed to the need for the constant development of new antiretroviral drugs over the past 25 years. With the recent approval of dolutegravir for human therapy by the U.S.
Mark A. Wainberg +2 more
openaire +2 more sources
Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids
Molecules, 2015 HIV integrase, encoded at the 3′-end of the HIV pol gene, is essential for HIV replication. This enzyme catalyzes the incorporation of HIV DNA into human DNA, which represents the point of “no-return” in HIV infection.
Vasu Nair, Maurice Okello
doaj +1 more source
Quantifying the Sensitivity of HIV-1 Viral Entry to Receptor and Coreceptor Expression [PDF]
J. Phys. Chem. B, 2016, 120 (26), pp 6189-6199, 2018 Infection by many viruses begins with fusion of viral and cellular lipid membranes, followed by entry of viral contents into the target cell and ultimately, after many biochemical steps, integration of viral DNA into that of the host cell. The early steps of membrane fusion and viral capsid entry are mediated by adsorption to the cell surface, and ...
arxiv +1 more source
Nonhuman Primates and Humanized Mice for Studies of HIV-1 Integrase Inhibitors: A Review
Pathogens and Immunity, 2016 Since the discovery of the first inhibitors of HIV replication, drug resistance has been a major problem in HIV therapy, due, in part, to the high mutation rate of HIV.
Said A. Hassounah +2 more
doaj +1 more source
Measurement of binding kinetics using quantum plasmonic resonance sensing applied to HIV-1 [PDF]
arXiv, 2022 The work done in this paper is an extension of the work done by Mpofu et al in [1]. The motivation for this paper is to show the potential of quantum bio-sensing techniques in applications to complex viruses like the human immunodeficiency virus (HIV) and to show it's potential in binding reactions where the signal is small and can potentially be ...
arxiv
HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure
Retrovirology, 2009 In a recent summary of integrase sequences, primary integrase inhibitor mutations were rare. In a review of integrase inhibitor-naïve Australian HIV-1 sequences, primary mutations were not identified, although the accessory mutation G140S was detected. A
Wang Bin +5 more
doaj +1 more source
Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity
South African Journal of Science, 2018 Drug repurposing offers a validated approach to reduce drug attrition within the drug discovery and development pipeline through the application of known drugs and drug candidates to treat new indications.
Shaakira Abrahams +4 more
doaj +1 more source