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

[ Vol. 18 , Issue. 31 ]

Author(s):

Maninder Kaur, Ravindra K. Rawal*, Goutam Rath and Amit K. Goyal*   Pages 2664 - 2680 ( 17 )

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.

Affiliation:

ISF College of Pharmacy, Moga-142001, Punjab, Department of Chemistry, Maharishi Markandeshwar (Deemed to be University), Mullana-133207, Haryana, ISF College of Pharmacy, Moga-142001, Punjab, National Institute of Animal Biotechnology, Miyapur, Hyderabad 500049

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