杜鲁特格拉维尔
整合酶
整合酶抑制剂
人类免疫缺陷病毒(HIV)
整合酶
病毒学
计算生物学
药品
生物
医学
药理学
抗逆转录病毒疗法
病毒载量
作者
Bawneet Narang,Gurpreet Kaur Grewal,Subhajit Roy,Jitender Bariwal,Manish Gupta,Ravindra K. Rawal
标识
DOI:10.2174/1570162x12666140807150753
摘要
Out of the 15 discrete proteins encoding the total amount of genetic information in the chromosomes of human immunodeficiency virus type 1; three perform the vital enzymatic functions i.e. a reverse transcription, an integration, and proteolysis. The HIV integrase is the new validated drug target against AIDS amongst all essential enzymes due to the lack of the human homologue. In last few years quite, a few but potent inhibitors inhibiting HIV-1 integrase have been recognized and hence have gained a state-of-the-art for treating the infection caused by HIV-1. The greater understanding of HIV-integrase biological structure has further lead to continuous efforts for the proposal of novel inhibitors targeting diverse steps in the progression of integration with the primary goal to overcome resistance due to the rapid occurrence of integrase mutations in the treated patients. This review is focused on various aspects of the recently approved HIV integrase inhibitor "dolutegravir", its efficacy, safety profiles with the clinical data and molecular modeling studies highlighting its importance over the already approved HIV-integrase inhibitors.
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