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PLoS One. 2017 Jun 28;12(6):e0179100. doi: 10.1371/journal.pone.0179100. eCollection 2017.

Identification of benzazole compounds that induce HIV-1 transcription.

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PTC Therapeutics, Inc., South Plainfield, New Jersey, United States of America.
Department of Medicine and Microbiology, Section of Infectious Diseases, Boston University School of Medicine, Boston, Massachusetts, United States of America.
Department of Pediatrics, Neonatology, School of Medicine and Dentistry, University of Rochester Medical Center, Rochester, New York, United States of America.


Despite advances in antiretroviral therapy, HIV-1 infection remains incurable in patients and continues to present a significant public health burden worldwide. While a number of factors contribute to persistent HIV-1 infection in patients, the presence of a stable, long-lived reservoir of latent provirus represents a significant hurdle in realizing an effective cure. One potential strategy to eliminate HIV-1 reservoirs in patients is reactivation of latent provirus with latency reversing agents in combination with antiretroviral therapy, a strategy termed "shock and kill". This strategy has shown limited clinical effectiveness thus far, potentially due to limitations of the few therapeutics currently available. We have identified a novel class of benzazole compounds effective at inducing HIV-1 expression in several cellular models. These compounds do not act via histone deacetylase inhibition or T cell activation, and show specificity in activating HIV-1 in vitro. Initial exploration of structure-activity relationships and pharmaceutical properties indicates that these compounds represent a potential scaffold for development of more potent HIV-1 latency reversing agents.

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