HIV-1 Entry and Membrane Fusion Inhibitors [PDF]
Viruses, 2021 HIV-1 (human immunodeficiency virus type 1) infection begins with the attachment of the virion to a host cell by its envelope glycoprotein (Env), which subsequently induces fusion of viral and cell membranes to allow viral entry.
Tianshu Xiao, Yongfei Cai, Bing Chen
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Design of Artificial Peptide Against HIV-1 Based on the Heptad-Repeat Rules and Membrane-Anchor Strategies [PDF]
PharmaceuticalsObjective: The six-helix bundle (6-HB) is critical for HIV-1 membrane fusion. To disrupt this process, peptide inhibitors have been meticulously designed to target interactions within the 6-HB regions, thereby blocking membrane fusion and exerting ...
Jiali Zhao +11 more
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Emerging Microbes and Infections, 2021 EK1 peptide is a membrane fusion inhibitor with broad-spectrum activity against human coronaviruses (CoVs). In the outbreak of COVID-19, we generated a lipopeptide EK1V1 by modifying EK1 with cholesterol, which exhibited significantly improved antiviral ...
Danwei Yu +5 more
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Structure-Guided Design of Peptide Inhibitors Targeting Class I Viral Fusion Proteins [PDF]
PathogensViral fusion proteins are indispensable mediators of viral entry that orchestrate the fusion of viral and host membranes, making them primary targets for antiviral interventions.
Narendra Kumar Gonepudi +4 more
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HIV Escape From Peptide Fusion Inhibitors [PDF]
Retrovirology, 2005 HIV envelope glycoprotein (Env) mediates infection by fusing virus with cellular membranes. Fusion inhibitors, a new class of antiretroviral drugs, inhibit HIV infection by binding to gp41 to form a peptide-gp41 6HB that is fusion-incompetent. To understand resistance mechanisms to peptide fusion inhibitors that will aid development of new drugs, we ...
Wingfield Paul +5 more
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Multimerized CHR-derived peptides as HIV-1 fusion inhibitors
Bioorganic and Medicinal Chemistry, 2013 To date, several HIV-1 fusion inhibitors based on the carboxy-terminal leucine/isoleucine heptad repeat (CHR) region of an HIV-1 envelope protein gp41 have been discovered. We have shown that a synthetic peptide mimetic of a trimer form of the CHR-derived peptide C34 has potent inhibitory activity against the HIV-1 fusion mechanism, compared to a ...
Wataru Nomura +2 more
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A Protein-Based, Long-Acting HIV-1 Fusion Inhibitor with an Improved Pharmacokinetic Profile
Pharmaceuticals, 2022 Recently, a series of highly effective peptide- or protein-based HIV fusion inhibitors have been identified. However, due to their short half-life, their clinical application is limited.
Wei Xu +8 more
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Role of Abl kinase and the Wave2 signaling complex in HIV-1 entry at a post-hemifusion step. [PDF]
PLoS Pathogens, 2010 Entry of human immunodeficiency virus type 1 (HIV-1) commences with binding of the envelope glycoprotein (Env) to the receptor CD4, and one of two coreceptors, CXCR4 or CCR5.
Brooke Harmon +2 more
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Survival of the fittest: positive selection of CD4+ T cells expressing a membrane-bound fusion inhibitor following HIV-1 infection. [PDF]
PLoS ONE, 2010 Although a variety of genetic strategies have been developed to inhibit HIV replication, few direct comparisons of the efficacy of these inhibitors have been carried out.
Janine Kimpel +12 more
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Sub-inhibitory concentrations of human α-defensin potentiate neutralizing antibodies against HIV-1 gp41 pre-hairpin intermediates in the presence of serum. [PDF]
PLoS Pathogens, 2013 Human defensins are at the forefront of the host responses to HIV and other pathogens in mucosal tissues. However, their ability to inactivate HIV in the bloodstream has been questioned due to the antagonistic effect of serum.
Lusine Demirkhanyan +3 more
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