Global Human Immunodeficiency Virus (HIV) statistics by the 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 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 by the current integrases invites immediate attention
of the drug discovery community for the development of new second-generation Integrase
Strand Transfer Inhibitors (INSTIs). It will exhibit greater efficacy against Elvitegravir (EVG) and
Raltegravir (RAL) resistant strains of HIV. This review focuses on the 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 the evolution of resistance
are also explored.
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