Guisen Zhao, Chao Wang, Chuan Liu, Hongxiang Lou, Guisen Zhao, Chao Wang, Chuan Liu and Hongxiang Lou Pages 707 - 725 ( 19 )
HIV-1 integrase is one of the three enzymes, which are critical for viral replication. It catalyzes the integration of the HIV genome into the cellular chromosome. Since there is no known human homolog to integrase, its inhibition is one of the most promising novel drug targets for anti-retroviral therapy with potential advantage over existing therapies. To date, numerous compounds with diverse structural features have been reported as integrase inhibitors, among which the diketo-containing inhibitors of HIV-1 integrase represent a major lead for anti-HIV drug development. The discovery of diketo acids plays an important role in validating integrase as a legitimate target for treatment of AIDS. In this review, we summarize several drug candidates in clinical trials and new diketo-containing inhibitors of HIV-1 integrase discovered recently.
Human immunodeficiency virus, integrase, inhibitors, diketo acids
College of Pharmacy, Shandong University, Jinan, Shandong 250012, PR China., College of Pharmacy, Shandong University, Jinan, Shandong 250012, PR China.