Results 21 to 30 of about 1,959,868 (292)

A Peptide-Based HIV-1 Fusion Inhibitor with Two Tail-Anchors and Palmitic Acid Exhibits Substantially Improved In Vitro and Ex Vivo Anti-HIV-1 Activity and Prolonged In Vivo Half-Life

Molecules, 2019
Enfuvirtide (T20) is the first U.S. FDA-approved HIV fusion inhibitor-based anti-HIV drug. Its clinical application is limited because of its low potency and short half-life.
Shan Su, Giselle Rasquinha, Lanying Du, Qian Wang, Wei Xu, Weihua Li, Lu Lu, Shibo Jiang   +7 more
doaj   +1 more source

The Curious Case of Arenavirus Entry, and Its Inhibition

Viruses, 2012
Arenaviruses comprise a diverse family of enveloped negative-strand RNA viruses that are endemic to specific rodent hosts worldwide. Several arenaviruses cause severe hemorrhagic fevers in humans, including Junín and Machupo viruses in South America and ...
Joanne York, Jack H. Nunberg
doaj   +1 more source

Structural and Functional Characterization of the Secondary Mutation N126K Selected by Various HIV-1 Fusion Inhibitors

Viruses, 2020
Peptides derived from the C-terminal heptad repeat (CHR) region of HIV-1 gp41 is potent viral membrane fusion inhibitors, such as the first clinically approved peptide drug T20 and a group of newly-designed peptides.
Danwei Yu, Yang Su, Xiaohui Ding, Yuanmei Zhu, Bo Qin, Huihui Chong, Sheng Cui, Yuxian He   +7 more
doaj   +1 more source

Conserved Residue Asn-145 in the C-Terminal Heptad Repeat Region of HIV-1 gp41 is Critical for Viral Fusion and Regulates the Antiviral Activity of Fusion Inhibitors

Viruses, 2019
Entry of HIV-1 into target cells is mediated by its envelope (Env) glycoprotein composed of the receptor binding subunit gp120 and the fusion protein gp41. Refolding of the gp41 N- and C-terminal heptad repeats (NHR and CHR) into a six-helix bundle (6-HB)
Xiuzhu Geng, Zixuan Liu, Danwei Yu, Bo Qin, Yuanmei Zhu, Sheng Cui, Huihui Chong, Yuxian He   +7 more
doaj   +1 more source

SARS-CoV-2 fusion-inhibitory lipopeptides maintain high potency against divergent variants of concern including Omicron

Emerging Microbes and Infections, 2022
The emergence of SARS-CoV-2 Omicron and other variants of concern (VOCs) has brought huge challenges to control the COVID-19 pandemic, calling for urgent development of effective vaccines and therapeutic drugs. In this study, we focused on characterizing
Yuanmei Zhu, Xiaojing Dong, Nian Liu, Tong Wu, Huihui Chong, Xiaobo Lei, Lili Ren, Jianwei Wang, Yuxian He   +8 more
doaj   +1 more source

SERINC5 Restricts HIV-1 Infectivity by Promoting Conformational Changes and Accelerating Functional Inactivation of Env

Viruses, 2022
SERINC5 incorporates into HIV-1 particles and inhibits the ability of Env glycoprotein to mediate virus-cell fusion. SERINC5-resistance maps to Env, with primary isolates generally showing greater resistance than laboratory-adapted strains.
Junghwa Kirschman, Mariana Marin, Yen-Cheng Chen, Junhua Chen, Alon Herschhorn, Amos B. Smith, Gregory B. Melikyan   +6 more
doaj   +1 more source

Ginkgolic Acid Inhibits Coronavirus Strain 229E Infection of Human Epithelial Lung Cells

Pharmaceuticals, 2021
Since December 2019, the COVID-19 pandemic has affected more than 200 million individuals around the globe and caused millions of deaths. Although there are now multiple vaccines for SARS-CoV-2, their efficacy may be limited by current and future viral ...
Maimoona S. Bhutta, Daniel G. Sausen, Elisa S. Gallo, Harel Dahari, Gustavo F. Doncel, Ronen Borenstein   +5 more
doaj   +1 more source

A targeted covalent small molecule inhibitor of HIV-1 fusion

, 2021
We describe a low molecular weight covalent inhibitor targeting a conserved lysine residue within the hydrophobic pocket of HIV-1 glycoprotein-41. The inhibitor bound selectively to the hydrophobic pocket and exhibited an order of magnitude enhancement ...
Pedroso, Cássio C. S., Li, Kathy H., Gochin, Miriam, Zhou, Guangyan, He, Li, Miriam Gochin, Guangyan Zhou, Li He, Kathy H. Li, Cássio C. S. Pedroso   +9 more
core   +1 more source

Asymmetric deactivation of HIV-1 gp41 following fusion inhibitor binding. [PDF]

, 2009
Both equilibrium and nonequilibrium factors influence the efficacy of pharmaceutical agents that target intermediate states of biochemical reactions. We explored the intermediate state inhibition of gp41, part of the HIV-1 envelope glycoprotein complex ...
Kahle, Kristen M, Steger, H Kirby, Root, Michael J   +2 more
core   +3 more sources