Enfuvirtide is a new class of antiviral drug, fusion inhibitors, which interferate with penetration of HIV-1 in the cells. Enfuvirtide exhibits potent and selective inhibition of membrane of viral and cells. It specifically inhibits the function of the gp41 transmembrane glycoprotein of HIV-1. Enfurvitide showed significantly efficacy in the combination with other antiviral drugs in early stadium of HIV infection and in patients with antiretroviral resistention. Local injection site reactions are the most common adverse events associated with enfurvitide. However, the need for subcutaneous application of enfurvitide is a distinct disadvantage, especially in patients who are already burdened by complex oral therapy.
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J Pept Sci
December 2024
Department of Pharmacy, University of Salerno, Fisciano, Italy.
Protein Pept Lett
September 2024
State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, P.R. China.
Cureus
August 2023
Surgery/General Surgery, Montreal General Hospital/McGill University Health Centre, Montreal, ASM.
Enfuvirtide was the first marketed fusion inhibitor that worked by binding to glycoprotein 41 of the HIV envelope, preventing the conformational changes required for HIV fusion with CD4+ T cells. Due to its novel mechanisms of action, it was frequently used in the past as part of regimens for the indication of multi-class-resistant HIV until newer oral agents emerged. Here, we describe the case of a 40-year-old man who used enfuvirtide injections from 2012 to 2017 inclusive for multi-class-resistant HIV until he presented in 2021 with an abscess overlying a right lower quadrant mass requiring drainage via pigtail.
View Article and Find Full Text PDFCurr Pharm Biotechnol
July 2023
Tianjin Institute of Environmental and Operational Medicine, Tianjin, 300050, P. R. China.
Viral infection has become one of the worst human lethal diseases. In recent years, major gains have been made in the research of peptide-based antiviral agents on account of the mechanism of viral membrane fusion, among which the peptide Enfuvirtide has been listed for the treatment of AIDS. This paper reviewed a new way to design peptide-based antiviral agents by "bundling" superhelix with isopeptide bonds to construct the active advanced structure.
View Article and Find Full Text PDFInt J Mol Sci
June 2022
NHC Key Laboratory of Systems Biology of Pathogens, Institute of Pathogen Biology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100730, China.
In our previous work, we replaced the TRM (tryptophan-rich motif) of T20 (Enfuvirtide) with fatty acid (C16) to obtain the novel lipopeptide LP-40, and LP-40 displayed enhanced antiviral activity. In this study, we investigated whether the C16 modification could enhance the high-resistance barrier of the inhibitor LP-40. To address this question, we performed an in vitro simultaneous screening of HIV-1 resistance to T20 and LP-40.
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