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Updated: Feb 27, 2026

High Throughput In Vitro Assessment of Latency Reversing Agents on HIV Transcription and Splicing

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Diseño racional e identificación de agonistas de TLR8 altamente selectivos como potentes agentes de reversión de la

Zhisong Wang^1,2, Yangyang Li^3,4,5, Jie Wang²

¹State Key Laboratory of Molecular Oncology, School of Pharmaceutical Sciences, Tsinghua-Peking Center for Life Science, Tsinghua University, Beijing 100084, China.

Journal of medicinal chemistry

|February 25, 2026

Abstract:

Highly active antiretroviral therapy (HAART) for HIV-1 infection suppresses but does not cure the disease due to persistent latent viral reservoirs. The "shock and kill" strategy aims to eradicate these reservoirs completely. In exploring the role of TLR8 activation in this context, extensive efforts have been devoted to identify compound 23a, a potent and selective TLR8 agonist with strong agonistic activity (EC₅₀ = 19 nM) and high selectivity (∼1300-fold) over TLR7. Notably, compound 23a exhibits potent reactivation of latent HIV-1 reservoirs in both infected cell lines and primary PBMCs from HAART-treated patients, demonstrating superior efficacy compared to the TLR7 agonist GS-9620 (NCT05281510). Additionally, 23a (SV-128) effectively activated innate cytolytic effectors, including natural killer (NK) cells, which targeted HIV-infected CD4⁺ T cells. These findings demonstrate the promising therapeutic potential of TLR8 agonists for HIV-1 eradication, combining both "shock" (latency reversal) and "kill" (immune-mediated clearance) mechanisms.

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