Integrating different approaches for the identification of new disruptors of HIV-1 capsid multimerization.

Human Immunodeficiency Virus (HIV) belongs to the Lentivirus genus, Retroviridae family, enveloped by a lipid bilayer within which the capsid protein encases the viral genome, reverse transcriptase, and integrase proteins, key components for viral replication. Viral capsid has been linked to key early and late stages of viral infection, including nuclear entry, promoting reverse transcription and assembly of new viral particles within target TCD4+ lymphocytes. Effective treatments for HIV involve multi drug therapy, which can reduce the patient's viral load to undetectable values, thus avoiding the appearance of Acquired Immunodeficiency Syndrome (AIDS).

Identification of 2-(4-N,N-Dimethylaminophenyl)-5-methyl-1-phenethyl-1H-benzimidazole targeting HIV-1 CA capsid protein and inhibiting HIV-1 replication in cellulo.

The capsid (CA) subunit of the HIV-1 Gag polyprotein is involved in several steps of the viral cycle, from the assembly of new viral particles to the protection of the viral genome until it enters into the nucleus of newly infected cells. As such, it represents an interesting therapeutic target to tackle HIV infection. In this study, we screened hundreds of compounds with a low cost of synthesis for their ability to interfere with Gag assembly in vitro.