A novel integrase targeting agent to explore the future prospective of HIV eradication: dolutegravir.

Abstract

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.

• Authors: Bawneet K Narang, Gurpreet K Grewal, Subhajit Roy, Jitender Bariwal, Manish K Gupta, Ravindra K Rawal
• Journal: Current HIV research (Curr HIV Res) Vol. 12 Issue 5 Pg. 325-38 ( 2014) ISSN: 1873-4251 [Electronic] Netherlands
• PMID: 25106411 (Publication Type: Journal Article, Review)

Chemical References

• HIV Integrase Inhibitors
• Heterocyclic Compounds, 3-Ring
• Oxazines
• Piperazines
• Pyridones
• dolutegravir

Topics

• Drug Resistance, Viral (genetics)
• HIV Infections (drug therapy)
• HIV Integrase Inhibitors (pharmacology, therapeutic use)
• HIV-1 (drug effects)
• Heterocyclic Compounds, 3-Ring (pharmacology, therapeutic use)
• Humans
• Oxazines
• Piperazines
• Prospective Studies
• Pyridones