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Chemical synthesis of antibody-recruiting small molecule (ARM) HIV entry inhibitors
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Chemical synthesis of antibody-recruiting small molecule (ARM) HIV entry inhibitors

Ziyuan Ma
Master of Science (M.S.), Drexel University
May 2018
DOI:
https://doi.org/10.17918/70zx-n823
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Abstract

Chemistry, Organic HIV (Viruses) Pharmacology Physiology
HIV-1 accounts for the vast majority cause of AIDS in the world. Viral entry is the first phase of the HIV replication cycle which begins with the attachment of virus onto the surface of the host cell and ends with the injection of viral genetic materials into the infected cells after the fusion of the viral and cell membrane. In recent years, antibody therapies are playing an influential role in treating human diseases, especially for viral infections. Because the limitations of contemporary combination remedies and antibody-based therapies, patients need a cure medication to thoroughly eliminate HIV from their body. Now we introduce antibody-recruiting small molecules (ARMs) as a cutting-edge strategy to treat AIDS. ARMs are bifunctional small molecules which are able to simultaneously associate with target cells or pathogens and recruit endogenous antibodies. The immune-mediated clearance will activate once the ternary complexes are formed, thus leading to the apoptosis or lysis of the targeted pathogenic cells or virus. Here, this work introduced the synthesis of several CCR5- and gp120-binding ARMs which are not only can recruit antibodies to the cells and virus, but also able to block CCR5 and gp120 receptors to inhibit the entry of HIV into the host cells. Also, this study indicated the modification of current HIV inhibitors into ARMs would not discard their inhibitory effect.

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