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Recent Advances in the Development of Integrase Inhibitors for HIV Treatment

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Published:20th Jan 2020
Author: Trivedi J, Mahajan D, Jaffe RJ, Acharya A, Mitra D, Byrareddy SN.
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Ref.:Curr HIV/AIDS Rep. 2020 Feb;17(1):63-75.
Recent Advances in the Development of Integrase Inhibitors for HIV Treatment

Purpose of the review:
The complex multistep life cycle of HIV allows it to proliferate within the host and integrate its genome in to the host chromosomal DNA. This provirus can remain dormant for an indefinite period. The process of integration, governed by integrase (IN), is highly conserved across the Retroviridae family. Hence, targeting integration is not only expected to block HIV replication but may also reveal new therapeutic strategies to treat HIV as well as other retrovirus infections.

Recent findings: HIV integrase (IN) has gained attention as the most promising therapeutic target as there are no equivalent homologues of IN that has been discovered in humans. Although current nano-formulated long-acting IN inhibitors have demonstrated the phenomenal ability to block HIV integration and replication with extraordinary half-life, they also have certain limitations. In this review, we have summarized the current literature on clinically established IN inhibitors, their mechanism of action, the advantages and disadvantages associated with their therapeutic application, and finally current HIV cure strategies using these inhibitors.

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