Delving into the Latest Updates on 4HR-LBD-VIRIP with Synapse

Overview

Basic Info

Drug Type

Recombinant polypeptide

Synonyms-

Target

gp41

Action

inhibitors

Mechanism

gp41 inhibitors(Transmembrane glycoprotein gp41 inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV Infections

Originator Organization

Academy of Military Med Sci, Inst of Toxicology & Pharmacology

Active Organization-

Inactive Organization

Academy of Military Med Sci, Inst of Toxicology & Pharmacology

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

HIV-1 fusion with the target cell is initiated by the insertion of the gp41 fusion peptide (FP) into the target cell membrane and the interaction between the gp41 N- and C-terminal heptad repeats (NHR and CHR), followed by the formation of the six-helix bundle (6-HB) fusion core. Therefore, both FP and NHR are important targets for HIV-1 fusion inhibitors. Here, we designed and synthesized a dual-target peptidic HIV-1 fusion inhibitor, 4HR-LBD-VIRIP, in which 4HR-LBD is able to bind to the gp41 NHR domain, while VIRIP is able to interact with gp41 FP. We found that 4HR-LBD-VIRIP is about tenfold more potent than 4HR-LBD and VIRIP in inhibiting HIV-1_IIIB infection and HIV-1 envelope glycoprotein (Env)-mediated cell-cell fusion, suggesting that this dual-target HIV-1 fusion inhibitor possesses a strong synergistic antiviral effect. A biophysical analysis indicates that 4HR-LBD-VIRIP can interact with N70 peptide that contains the gp41 NHR and FP domains and binds with lipid membrane. This study provides a new approach for designing novel viral fusion inhibitors against HIV and other enveloped viruses with class I membrane fusion proteins.

100 Deals associated with 4HR-LBD-VIRIP

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Preclinical	China	Academy of Military Med Sci, Inst of Toxicology & Pharmacology	08 Sep 2016

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Biosimilar

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