On September 16, 2022, Moore, Keith P.; Schwaid, Adam G.; Tudor, Matthew; Park, Sangho; Beshore, Douglas C.; Converso, Antonella; Shipe, William D.; Anand, Rajan; Lan, Ping; Moningka, Remond; Rothman, Deborah M.; Sun, Wanying; Chi, An; Cornella-Taracido, Ivan; Adam, Gregory C.; Bahnck-Teets, Carolyn; Carroll, Steven S.; Fay, John F.; Goh, Shih Lin; Lusen, Jeffrey; Quan, Shuo; Rodriguez, Silveria; Xu, Min; Andrews, Christine L.; Song, Cheng; Filzen, Tracey; Li, Jing; Hollenstein, Kaspar; Klein, Daniel J.; Lammens, Alfred; Lim, U-Ming; Fang, Zhiyu; McHale, Carolyn; Li, Yuan; Lu, Meiqing; Diamond, Tracy L.; Howell, Bonnie J.; Zuck, Paul; Balibar, Carl J. published an article.Quality Control of H-Phg(4-OH)-OH The title of the article was A Phenotypic Screen Identifies Potent DPP9 Inhibitors Capable of Killing HIV-1 Infected Cells. And the article contained the following:
Although current antiretroviral therapy can control HIV-1 replication and prevent disease progression, it is not curative. Identifying mechanisms that can lead to eradication of persistent viral reservoirs in people living with HIV-1 (PLWH) remains an outstanding challenge to achieving cure. Utilizing a phenotypic screen, we identified a novel chem. class capable of killing HIV-1 infected peripheral blood mononuclear cells. Tool compounds ICeD-1 and ICeD-2 (“inducer of cell death-1 and 2”), optimized for potency and selectivity from screening hits, were used to deconvolute the mechanism of action using a combination of chemoproteomic, biochem., pharmacol., and genetic approaches. We determined that these compounds function by modulating dipeptidyl peptidase 9 (DPP9) and activating the caspase recruitment domain family member 8 (CARD8) inflammasome. Efficacy of ICeD-1 and ICeD-2 was dependent on HIV-1 protease activity and synergistic with efavirenz, which promotes premature activation of HIV-1 protease at high concentrations in infected cells. This in vitro synergy lowers the efficacious cell kill concentration of efavirenz to a clin. relevant dose at concentrations of ICeD-1 or ICeD-2 that do not result in complete DPP9 inhibition. These results suggest engagement of the pyroptotic pathway as a potential approach to eliminate HIV-1 infected cells. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Quality Control of H-Phg(4-OH)-OH
The Article related to screening preparation dpp9 inhibitor hiv1 infected leukocyte, Placeholder for records without volume info and other aspects.Quality Control of H-Phg(4-OH)-OH
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