Targeting Integrase enzyme: A Therapeutic Approach to combat HIV resistance.

Targeting Integrase enzyme: A Therapeutic Approach to combat HIV resistance. Mini Rev Med Chem. 2019 Oct 15;: Authors: Komal D, Joshi K, Sethi A, Soukya L, Alvala M Abstract Global HIV statistics by World Health Organization (WHO) for the year 2017 was estimated to be 36.9 (31.1-43.9) million. Antiviral drug resistance poses a serious threat to the public health and requires immediate action. Retroviral integrase (IN) a component enzyme in the retroviral pre-integration complex (PIC) enables a retrovirus to incorporate its genetic material into the host DNA. Development of resistance to the current integrases invites immediate attention of the drug discovery community for the development of new second-generation INtegrase Strand Transfer Inhibitors (INSTIs), the need of hour that will exhibit greater efficacy against Elvitegravir (EVG) and Raltegravir (RAL) resistant strains of HIV. This review focuses on mechanism, importance of integrase structure, function and current research on small molecule inhibitors of integrase to overcome drug resistance. The molecular mechanism of retroviral integrase inhibition and evolution of resistance is also explored. PMID: 31613727 [PubMed - as supplied by publisher]
Source: Mini Reviews in Medicinal Chemistry - Category: Chemistry Authors: Tags: Mini Rev Med Chem Source Type: research