Recent Progress in the Development of HIV-1 Entry Inhibitors: From Small Molecules to Potent Anti-HIV Agents

Author(s): Khomson Suttisintong*, Narongpol Kaewchangwat, Eknarin Thanayupong, Chakkrapan Nerungsi, Onsiri Srikun, Pornpan Pungpo.

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 18 , 2019

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Graphical Abstract:


Abstract:

Viral entry, the first process in the reproduction of viruses, primarily involves attachment of the viral envelope proteins to membranes of the host cell. The crucial components that play an important role in viral entry include viral surface glycoprotein gp120, viral transmembrane glycoprotein gp41, host cell glycoprotein (CD4), and host cell chemokine receptors (CCR5 and CXCR4). Inhibition of the multiple molecular interactions of these components can restrain viruses, such as HIV-1, from fusion with the host cell, blocking them from reproducing. This review article specifically focuses on the recent progress in the development of small-molecule HIV-1 entry inhibitors and incorporates important aspects of their structural modification that lead to the discovery of new molecular scaffolds with more potency.

Keywords: HIV-1 entry inhibitors, Anti-HIV-1, CXCR4 antagonists, CCR5 antagonists, Fusion inhibitors, CD4 mimic molecules.

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