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Nicotinamide activates latent HIV-1 ex vivo in ART suppressed individuals, revealing higher potency than the association of two methyltransferase inhibitors, chaetocin and BIX01294

Sadia Samer, Muhammad Arif, Leila B. Giron, Jean Paulo Lopes Zukurov, James Hunter, Bruna Tereso Santillo, Gislene Mitsue Namiyama, Juliana Galinskas, Shirley Vasconcelos Komninakis, Telma Miyuki Oshiro, Maria Cecília Araripe Sucupira, Luiz Mário Janini, Ricardo Sobhie Diaz

2020The Brazilian Journal of Infectious Diseases21 citationsDOIOpen Access PDF

Abstract

BACKGROUND: Latent HIV-1 is a major hurdle in obtaining HIV-1 sustained virological remission (SVR). Here we explored histone deacetylation inhibition property of nicotinamide (NAM; n=17) for the first time in comparison to a combination of methyltransferase inhibitors (MTIs; Chaetocin and BIX01294; n=25) to reactivate latent HIV ex vivo in CD8-depleted PBMCs from antiretroviral treated aviremic individuals. RESULTS: RNA copies/mL, respectively (p=0.004). Mean purging time after NAM and MTIs stimulation was 5.1 and 6.75 days, respectively (p=0.73). Viral purging in autologous cultures exhibited blunted HIV recovery with fluctuating VLs followed by a complete viral extinction when expanded in allogenic system. Electron microscopy from five supernatants revealed anomalous viral particles, with lack of complete viral genomes when characterized by ultradeep sequencing through metagenomics approach (n=4). CONCLUSION: NAM alone was more potent HIV-1 activator than combination of MTIs, with potential of clinical use.

Topics & Concepts

Ex vivoNicotinamideViral loadBiologyPotencyVirologyHuman immunodeficiency virus (HIV)Peripheral blood mononuclear cellIn vivoMethyltransferasePharmacologyChemistryBiochemistryEnzymeIn vitroMethylationGeneticsGeneHIV Research and TreatmentHIV/AIDS drug development and treatmentHIV-related health complications and treatments