Long Active Drug Targeting Capsid Protein Promising for HIV


A small molecule that disrupts the functions of the HIV capsid protein, GS-6207, shows plasma viral load reduction, and shows continuous plasma exposure. GS-6207, which disrupts HIV capsid protein functions and has high potency, low systemic clearance in vivo and slow release kinetics from the subcutaneous injection site, making it ideal for long-acting therapy. The GS-6207 was designed to bind tightly between capsid proteins monomers at a preserved interface where it interferes with capsid-protein-mediated interactions between the proteins required for the viral replication cycle. Researchers found that the GS-6207 exhibited antiviral activity at Pico molar concentrations against all tested HIV-1 subtypes, demonstrating high synergy and no cross-resistance with approved antiretroviral drugs. The favourable safety profile, extended pharmacokinetic exposure and observed human antiviral efficacy support the ongoing clinical development of GS-6207 as a long-acting antiretroviral agent for the treatment of HIV-1 infection, including those living with HIV who are highly experienced in treatment and have multidrug-resistant viruses. Present the small molecule GS-6207 which aims to disrupt viral replication by the HIV-1 capsid protein. In vitro, when combined with other antiretroviral agents, GS-6207 demonstrated picomolar antiviral activity against all HIV-1 subtypes tested and showed synergy, without cross-resistance or cytotoxicity. Comparative modelling suggests that GS-CA compounds have unique structural features which contribute to capsid interactions. We also report the design of a cyclic peptide which combines structural units from GS-CA compounds, host factors and previously reported capsid inhibitors to test their proposed binding mode. This peptide (Pep-1) has a docking score comparable to GS-CA compounds that binds CA-hexamer. The determination of affinity by MicroScale thermophoresis (MST) assays showed that CA binds Pep-1 with a ~7-fold better affinity than the well-studied PF74 capsid inhibitor, indicating it could be formed as a potential CA inhibitor. This review tells about the future scope of the new invention towards the field of HIV /AIDS and their medicinal treatment. People who are interested can send their article towards our journal for publication through this https://www.scholarscentral.org/submissions/hiv-aids-research.html