Integrase: An important therapeutic target in the fight against HIV/AIDS infection

Abstract

The acquired immunodeficiency syndrome (AIDS) is caused by the human immunodeficiency virus (HIV) that infects cells of the immune system, destroying them or causing damage to its operation. Among all the HIV enzymes, integrase is responsible for the insertion of viral DNA in the host DNA. The aim of this article is to describe the integrase inhibitors drugs and report cases of resistance, in addition to discussing new promising compounds that are being evaluated as integrase inhibitors. Currently, there are only three drugs in clinical use that belong to the class of integrase inhibitors: raltegravir (a pirimidinone carboxamide derivative, elvitegravir (a quinoline derivative) and dolutegravir (a diazatricyclo carboxamide derivative). However, several cases of resistance to drugs of this class are described in the literature, and the mutations of the enzyme responsible for such profile are known. Many compounds with integrase inhibitory action are under development. The use of the integrase enzyme as a target against HIV/AIDS infection is promising. In addition, the integration is a complex stage of the viral replication cycle, and new details of this process are being discovered every minute, which encourages the accomplishment of more studies for the development of new drugs of this class.