Garcinol from Garcinia indica inhibits HIV‐1 reverse transcriptase‐associated ribonuclease H
Sign Up to like & getrecommendations! Published in 2021 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202100123
Abstract: The bioactive components of Garcinia indica, garcinol (camboginol), and isogarcinol (cambogin), are suitable drug candidates for the treatment of various human diseases. HIV‐1‐RNase H assay was used to study the RNase H inhibition by garcinol… read more here.
Keywords: garcinol; garcinia indica; reverse transcriptase; hiv reverse ... See more keywords
Relative domain orientation of the L289K HIV‐1 reverse transcriptase monomer
Sign Up to like & getrecommendations! Published in 2022 at "Protein Science"
DOI: 10.1002/pro.4307
Abstract: HIV‐1 reverse transcriptase (RT) is a heterodimer comprised p66 and p51 subunits (p66/p51). Several single amino acid substitutions in RT, including L289K, decrease p66/p51 dimer affinity, and reduce enzymatic functioning. Here, small‐angle X‐ray scattering (SAXS)… read more here.
Keywords: reverse transcriptase; hiv reverse; domain; p66 p51 ... See more keywords
Oxygen binding isotope effects of triazole-based HIV-1 reverse transcriptase inhibitors indicate the actual binding site.
Sign Up to like & getrecommendations! Published in 2017 at "Archives of biochemistry and biophysics"
DOI: 10.1016/j.abb.2017.10.017
Abstract: Binding isotope effects (BIEs) associated with binding of four triazole-based ligands to HIV-1 reverse transcriptase have been calculated at the QM/MM MD level of theory. Two main binding sites: allosteric cavity and RNase H active… read more here.
Keywords: hiv reverse; binding isotope; isotope; isotope effects ... See more keywords
Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.10.029
Abstract: In this work we report a parallel application of both docking- and shape-based virtual screening (VS) methods, followed by Molecular Dynamics simulations (MDs), for discovering new compounds able to inhibit the human immunodeficiency virus type… read more here.
Keywords: virtual screening; based virtual; nucleoside inhibitors; non nucleoside ... See more keywords
Exploring the dNTP -binding site of HIV-1 reverse transcriptase for inhibitor design.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113785
Abstract: HIV-1 reverse transcriptase (RT) plays a central role in the viral life cycle, and roughly half of the FDA-approved anti-HIV drugs are targeting RT. Nucleoside analogs (NRTIs) require cellular phosphorylation for binding to RT, and… read more here.
Keywords: reverse transcriptase; exploring dntp; hiv reverse;
Anti-HIV-1 reverse transcriptase property of some edible mushrooms in Asia
Sign Up to like & getrecommendations! Published in 2021 at "Saudi Journal of Biological Sciences"
DOI: 10.1016/j.sjbs.2021.02.012
Abstract: Human immunodeficiency virus (HIV) causes acquired immunodeficiency syndrome (AIDS), which is a serious health threat worldwide. One of its core enzymes, reverse transcriptase (RT), is a target for HIV inhibition. A number of bioactive compounds… read more here.
Keywords: hiv; transcriptase property; hiv reverse; anti hiv ... See more keywords
Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation.
Sign Up to like & getrecommendations! Published in 2019 at "Structure"
DOI: 10.1016/j.str.2019.08.004
Abstract: HIV-1 reverse transcriptase (RT) is translated as part of the Gag-Pol polyprotein that is proteolytically processed by HIV-1 protease (PR) to finally become a mature heterodimer, composed of a p66 and a p66-derived 51-kDa subunit,… read more here.
Keywords: conformational changes; hiv reverse; reverse transcriptase; p66 p66 ... See more keywords
eEF1A demonstrates paralog specific effects on HIV-1 reverse transcription efficiency.
Sign Up to like & getrecommendations! Published in 2019 at "Virology"
DOI: 10.1016/j.virol.2019.01.023
Abstract: The eukaryotic translation elongation factor 1A (eEF1A) has two cell-type specific paralogs, eEF1A1 and eEF1A2. Both paralogs undertake a canonical function in delivering aminoacyl-tRNA to the ribosome for translation, but differences in other functions are… read more here.
Keywords: transcription; eef1a1 eef1a2; reverse transcription; hiv reverse ... See more keywords
Scorpion-Shaped Zinc Porphyrins as Tetrafunctional TAR RNA Predators and HIV-1 Reverse Transcriptase Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Inorganic chemistry"
DOI: 10.1021/acs.inorgchem.2c00975
Abstract: HIV-1 reverse transcriptase (RT) inhibitors are fundamental to the discovery and development of anti-HIV drugs. Their main target is RT, and only a tiny number of them can bind to viral RNA. In this paper,… read more here.
Keywords: reverse transcriptase; hiv reverse; tar rna; rna ... See more keywords
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01104
Abstract: HIV-1 infection is typically treated using ≥2 drugs, including at least one HIV-1 reverse transcriptase (RT) inhibitor. Drugs targeting RT comprise nucleos(t)ide RT inhibitors (NRTIs) and non-nucleoside RT inhibitors (NNRTIs). NRTI-triphosphates bind at the polymerase… read more here.
Keywords: reverse transcriptase; hiv gp120; hiv reverse;
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
Sign Up to like & getrecommendations! Published in 2021 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00612
Abstract: Covalent inhibitors of wild-type HIV-1 reverse transcriptase (CRTIs) are reported. Three compounds derived from catechol diether non-nucleoside inhibitors (NNRTIs) with addition of a fluorosulfate warhead are demonstrated to covalently modify Tyr181 of HIV-RT. X-ray crystal… read more here.
Keywords: type hiv; fluorosulfate warhead; hiv; hiv reverse ... See more keywords