Search Results - "Debnath, Asim K"
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Development of Small-molecule HIV Entry Inhibitors Specifically Targeting gp120 or gp41
Published in Current topics in medicinal chemistry (01-01-2016)“…Human immunodeficiency virus type 1 (HIV-1) envelope (Env) glycoprotein surface subunit gp120 and transmembrane subunit gp41 play important roles in HIV-1…”
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Envelope Protein-Targeting Zika Virus Entry Inhibitors
Published in International journal of molecular sciences (30-08-2024)“…Zika virus (ZIKV; family, ), which causes congenital Zika syndrome, Guillain-Barré Syndrome, and other severe diseases, is transmitted mainly by mosquitoes;…”
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Identification of Novel Natural Products as Effective and Broad-Spectrum Anti-Zika Virus Inhibitors
Published in Viruses (02-11-2019)“…Zika virus (ZIKV) infection during pregnancy leads to severe congenital Zika syndrome, which includes microcephaly and other neurological malformations. No…”
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Identification of a Receptor-Binding Domain in the S Protein of the Novel Human Coronavirus Middle East Respiratory Syndrome Coronavirus as an Essential Target for Vaccine Development
Published in Journal of Virology (01-09-2013)“…Erratum ( vol. 87 , p. 11963 ) Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious…”
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Unliganded HIV-1 gp120 core structures assume the CD4-bound conformation with regulation by quaternary interactions and variable loops
Published in Proceedings of the National Academy of Sciences - PNAS (10-04-2012)“…The HIV-1 envelope (Env) spike (gp1203/gp413) undergoes considerable structural rearrangements to mediate virus entry into cells and to evade the host immune…”
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A gossypol derivative effectively protects against Zika and dengue virus infection without toxicity
Published in BMC biology (15-06-2022)“…Zika virus (ZIKV) and dengue virus (DENV) cause microcephaly and dengue hemorrhagic fever, respectively, leading to severe problems. No effective antiviral…”
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Antiviral Activity and Crystal Structures of HIV-1 gp120 Antagonists
Published in International journal of molecular sciences (15-12-2022)“…As part of our effort to discover drugs that target HIV-1 entry, we report the antiviral activity and crystal structures of two novel inhibitors in a complex…”
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Comparative Pharmacokinetics of a Dual Inhibitor of HIV-1, NBD-14189, in Rats and Dogs with a Proof-of-Concept Evaluation of Antiviral Potency in SCID-hu Mouse Model
Published in Viruses (01-10-2022)“…We earlier reported substantial progress in designing gp120 antagonists. Notably, we discovered that NBD-14189 is not only the most active gp120 antagonist but…”
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Discovery of Highly Potent Small Molecule Pan-Coronavirus Fusion Inhibitors
Published in Viruses (01-04-2023)“…The unprecedented pandemic of COVID-19, caused by a novel coronavirus, SARS-CoV-2, and its highly transmissible variants, led to massive human suffering,…”
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Design, Synthesis, and Structure−Activity Relationship of a Novel Series of 2-Aryl 5-(4-Oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans as HIV-1 Entry Inhibitors
Published in Journal of medicinal chemistry (10-12-2009)“…We previously identified two small molecules targeting the HIV-1 gp41, N-(4-carboxy-3-hydroxy)phenyl-2,5-dimethylpyrrole 12 (NB-2) and…”
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Solution Structure of a Hydrocarbon Stapled Peptide Inhibitor in Complex with Monomeric C-terminal Domain of HIV-1 Capsid
Published in The Journal of biological chemistry (13-06-2008)“…The human immunodeficiency virus type 1 (HIV-1) capsid protein plays a critical role in virus core particle assembly and is an important target for novel…”
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Binding mode characterization of NBD series CD4-mimetic HIV-1 entry inhibitors by X-ray structure and resistance study
Published in Antimicrobial agents and chemotherapy (01-09-2014)“…We previously identified two small-molecule CD4 mimetics--NBD-556 and NBD-557--and synthesized a series of NBD compounds that resulted in improved…”
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Design, synthesis and evaluation of small molecule CD4-mimics as entry inhibitors possessing broad spectrum anti-HIV-1 activity
Published in Bioorganic & medicinal chemistry (15-11-2016)“…Since our first discovery of a CD4-mimic, NBD-556, which targets the Phe43 cavity of HIV-1 gp120, we and other groups made considerable progress in designing…”
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Identification of Combinations of Protein Kinase C Activators and Histone Deacetylase Inhibitors That Potently Reactivate Latent HIV
Published in Viruses (03-06-2020)“…Combination antiretroviral therapy (cART) is successful in maintaining undetectable levels of HIV in the blood; however, the persistence of latent HIV…”
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Design, Synthesis, and Biological Activity of Novel 5-((Arylfuran/1H-pyrrol-2-yl)methylene)-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-4-ones as HIV-1 Fusion Inhibitors Targeting gp41
Published in Journal of medicinal chemistry (27-01-2011)“…On the basis of our earlier molecular docking analysis, we designed and synthesized…”
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Interaction between heptad repeat 1 and 2 regions in spike protein of SARS-associated coronavirus: implications for virus fusogenic mechanism and identification of fusion inhibitors
Published in The Lancet (British edition) (20-03-2004)“…Studies on the fusion-inhibitory peptides derived from the heptad repeat 1 and 2 (HR1 and HR2) regions of the HIV-1 envelope glycoprotein gp41 provided crucial…”
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N-Substituted Pyrrole Derivatives as Novel Human Immunodeficiency Virus Type 1 Entry Inhibitors That Interfere with the gp41 Six-Helix Bundle Formation and Block Virus Fusion
Published in Antimicrobial Agents and Chemotherapy (01-11-2004)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Crystal structures of HIV-1 gp120 envelope glycoprotein in complex with NBD analogues that target the CD4-binding site
Published in PloS one (28-01-2014)“…Efforts to develop therapeutic agents that inhibit HIV-1 entry have led to the identification of several small molecule leads. One of the most promising is the…”
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Virtual screening based identification of novel small-molecule inhibitors targeted to the HIV-1 capsid
Published in Bioorganic & medicinal chemistry (01-01-2011)“…The hydrophobic cavity of the C-terminal domain (CTD) of HIV-1 capsid has been recently validated as potential target for antiviral drugs by peptide-based…”
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Discovery of Highly Potent Fusion Inhibitors with Potential Pan-Coronavirus Activity That Effectively Inhibit Major COVID-19 Variants of Concern (VOCs) in Pseudovirus-Based Assays
Published in Viruses (31-12-2021)“…We report the discovery of several highly potent small molecules with low-nM potency against severe acute respiratory syndrome coronavirus (SARS-CoV; lowest…”
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