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Can I read Prodrugs of PKC modulators show enhanced HIV latency reversal and an expanded therapeutic window on EtoBox?
Prodrugs of PKC modulators show enhanced HIV latency reversal and an expanded therapeutic window by Jack L. Sloane; Nancy L. Benner; Katherine N. Keenan; Xiaoyu Zang; Mohamed S. A. Soliman; Xiaomeng Wu; Melanie Dimapasoc; Tae-Wook Chun; Matthew D. Marsden; Jerome A. Zack; Paul A. Wender is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Prodrugs of PKC modulators show enhanced HIV latency reversal and an expanded therapeutic window about?
AIDS is a pandemic disease caused by HIV that affects 37 million people worldwide. Current antiretroviral therapy slows disease progression but does not eliminate latently infected cells, which resupply active virus, thus necessitating lifelong treatment with associated compliance, cost, and chemoexposure issues. Latency-reversing agents (LRAs) activate these cells, allowing for their potential clearance, thus presenting a strategy to eradicate the infection. Protein kinase C (PKC) modulators-including prostratin, ingenol esters, bryostatin, and their analogs-are potent LRAs in various stages of development for several clinical indications. While LRAs are promising, a major challenge associated with their clinical use is sustaining therapeutically meaningful levels of the active agent while minimizing side effects. Here we describe a strategy to address this problem based on LRA prodrugs, designed for controllable release of the active LRA after a single injection. As intended, these prodrugs exhibit comparable or superior in vitro activity relative to the parent compounds. Selected compounds induced higher in vivo expression of CD69, an activation biomarker, and, by releasing free
Who reads Prodrugs of PKC modulators show enhanced HIV latency reversal and an expanded therapeutic window?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Jack L. Sloane; Nancy L. Benner; Katherine N. Keenan; Xiaoyu Zang; Mohamed S. A. Soliman; Xiaomeng Wu; Melanie Dimapasoc; Tae-Wook Chun; Matthew D. Marsden; Jerome A. Zack; Paul A. Wender
- Publisher
- National Academy of Sciences; Proceedings of the National Academy of Sciences; Oxford University Press (OUP); Publons; ScienceOpen (ISSN 0027-8424)
- Published
- 2020
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)