Structure Based Drug Design: Clinically Relevant HIV-1 Integrase Inhibitors

Author(s): Maninder Kaur, Ravindra K. Rawal*, Goutam Rath, Amit K. Goyal*.

Journal Name: Current Topics in Medicinal Chemistry

Volume 18 , Issue 31 , 2018

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Abstract:

HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells. It has emerged as a potential target for developing anti-HIV agents. In the last two decades, a number of integrase inhibitors have been developed as potential anti-HIV therapeutics. Several integrase inhibitors have reached later stages of clinical trials including S-1360, L870,810, L870,812 and BMS-707035. Into the bargain, Raltegravir, Elvitegravir and Dolutegravir have been approved by FDA as anti-HIV agents. This review article summarizes the structural insights required for the inhibition of the HIV1 integrase in the context of clinically relevant HIV1 integrase inhibitors. Additionally, the structural features required for overcoming HIV resistance have been discussed. These insights will update the ongoing design of novel antiviral inhibitors.

Keywords: HIV resistance, HIV-1 integrase, Anti-HIV therapeutics, Novel antiviral inhibitors, Polynucleotidyl transferases, Viral DNA.

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Article Details

VOLUME: 18
ISSUE: 31
Year: 2018
Page: [2664 - 2680]
Pages: 17
DOI: 10.2174/1568026619666190119143239
Price: $58

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