[HTML][HTML] Reactivation of latent HIV-1 by new semi-synthetic ingenol esters

DP José, K Bartholomeeusen, RD da Cunha… - Virology, 2014 - Elsevier
DP José, K Bartholomeeusen, RD da Cunha, CM Abreu, J Glinski, TBF da Costa
Virology, 2014Elsevier
The ability of HIV to establish long-lived latent infection is mainly due to transcriptional
silencing of viral genome in resting memory T lymphocytes. Here, we show that new semi-
synthetic ingenol esters reactivate latent HIV reservoirs. Amongst the tested compounds, 3-
caproyl-ingenol (ING B) was more potent in reactivating latent HIV than known activators
such as SAHA, ingenol 3, 20-dibenzoate, TNF-α, PMA and HMBA. ING B activated PKC
isoforms followed by NF-κB nuclear translocation. As virus reactivation is dependent on …
Abstract
The ability of HIV to establish long-lived latent infection is mainly due to transcriptional silencing of viral genome in resting memory T lymphocytes. Here, we show that new semi-synthetic ingenol esters reactivate latent HIV reservoirs. Amongst the tested compounds, 3-caproyl-ingenol (ING B) was more potent in reactivating latent HIV than known activators such as SAHA, ingenol 3,20-dibenzoate, TNF-α, PMA and HMBA. ING B activated PKC isoforms followed by NF-κB nuclear translocation. As virus reactivation is dependent on intact NF-κB binding sites in the LTR promoter region ING B, we have shown that. ING B was able to reactivate virus transcription in primary HIV-infected resting cells up to 12 fold and up to 25 fold in combination with SAHA. Additionally, ING B promoted up-regulation of P-TEFb subunits CDK9/Cyclin T1. The role of ING B on promoting both transcription initiation and elongation makes this compound a strong candidate for an anti-HIV latency drug combined with suppressive HAART.
Elsevier