2020
DOI: 10.1016/j.ejmech.2019.111991
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A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects

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Cited by 13 publications
(3 citation statements)
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References 33 publications
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“…In addition, Huang et al. 113 utilized 18b-glycyrrhetinic acid (GA) as the HyT warhead to synthesize a novel series of HDAC-targeting HyT degraders that tethered SAHA and GA via different linkers. Compound 28 , bearing a piperazine fragment, exhibited the most potent HDAC3/6 degradation activity.…”
Section: Hdac-targeting Degradersmentioning
confidence: 99%
“…In addition, Huang et al. 113 utilized 18b-glycyrrhetinic acid (GA) as the HyT warhead to synthesize a novel series of HDAC-targeting HyT degraders that tethered SAHA and GA via different linkers. Compound 28 , bearing a piperazine fragment, exhibited the most potent HDAC3/6 degradation activity.…”
Section: Hdac-targeting Degradersmentioning
confidence: 99%
“…Some studies suggest that simultaneously affecting HDAC3 and HDAC6 via the survivin and tubulin axes may have a synergistic effect on the treatment of cancer cells [43,44]. A novel hybrid of vorinostat and glycyrrhetinic acid has been shown to reduce protein levels of HDAC3 and HDAC6 that induce death of PC-3 and HL-60 cells [142].…”
Section: Dual Hdac6/3 Inhibitorsmentioning
confidence: 99%
“…To obtain a more specific effect of short-chain fatty acids, HDAC3 or HDAC9 specific inhibitors might show inhibitory effects on angioedema development. Although there is no specific inhibitor for HDAC3 and HDAC9, and almost all HDAC inhibitors have multitargeted HDAC suppression, vorinostat and entinostat have HDAC3 suppressive effects [112,113]. Although there is no clinically available HDAC9 inhibitor, TMP269 shows HDAC9 suppressive function.…”
Section: Therapeutic Potential For Fatty Acids Involving Angioedemamentioning
confidence: 99%