Structure based drug design: Clinically relevant HIV-1 integrase inhibitors

Maninder Kaur, Ravindra K. Rawal, Goutam Rath, Amit K. Goyal

Research output: Contribution to journalArticlepeer-review

11 Scopus citations


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 HIV19 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.
Original languageEnglish (US)
Pages (from-to)2664-2680
Number of pages17
JournalCurrent Topics in Medicinal Chemistry
Issue number31
StatePublished - Jan 1 2018
Externally publishedYes

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Generated from Scopus record by KAUST IRTS on 2023-10-12


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