A Small-Molecule CD4-Mimetic Compound Protects Bone Marrow–Liver–Thymus Humanized Mice From HIV-1 Infection. (29th March 2018)

• Record Type: Journal Article
• Authors: Princiotto, Amy M; Vrbanac, Vladimir D; Melillo, Bruno; Park, Jongwoo; Tager, Andrew M; Smith, Amos B; Sodroski, Joseph; Madani, Navid
• Is Part Of: Journal of infectious diseases. Volume 218:Number 3(2018)
• Page Start: 471
• Page End: 475
• Publication Date: 2018-03-29
• Subjects: HIV-1 -- prevention -- sexual transmission -- envelope glycoprotein; Communicable diseases -- Periodicals; Diseases -- Causes and theories of causation -- Periodicals; Medicine -- Periodicals; Communicable Diseases -- Periodicals; Electronic journals; 616.9
• DOI: 10.1093/infdis/jiy174
• Languages: English
• ISSNs: 0022-1899

Abstract

Abstract : A small molecule mimics the CD4 receptor for human immunodeficiency virus type 1, binds the viral envelope glycoprotein gp120, and blocks vaginal infection of BLT humanized mice. Abstract: Background: Small-molecule CD4-mimetic compounds (CD4mc) inhibit human immunodeficiency virus (HIV-1) entry by blocking binding to the CD4 receptor and by premature triggering of the viral envelope glycoprotein (Env) spike. Methods: The efficacy of a CD4mc in protecting bone marrow–liver–thymus (BLT) humanized mice from vaginal HIV-1 challenge was evaluated. Results: Intravaginal application of the CD4mc JP-III-48, either before or simultaneously with virus challenge, protected BLT humanized mice from HIV-1JR-CSF infection in a dose- dependent manner. Conclusion: The direct antiviral effects of a CD4mc prevent HIV-1 infection in a murine model of sexual transmission.