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000291284 1001_ $$aLiang, Ting$$b0
000291284 245__ $$aMultimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease.
000291284 260__ $$aAmsterdam [u.a.]$$bElsevier Science$$c2024
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000291284 520__ $$aWith the intensive research on the pathogenesis of Alzheimer's disease (AD), inhibition of HDAC6 appears to be a potential therapeutic approach for AD. In this paper, a series of tetrahydro-β-carboline derivatives with hydroxamic acid group were fast synthesized. Among all, the most potent 15 selectively inhibited HDAC6 with IC50 of 15.2 nM and markedly increased acetylated alpha-tubulin levels. In cellular assay, 15 showed excellent neurotrophic effect by increasing the expression of GAP43 and Beta-3 tubulin markers. Besides, 15 showed neuroprotective effects in PC12 or SH-SY5Y cells against H2O2 and 6-OHDA injury through activation of Nrf2, catalase and Prx II, and significantly reduced H2O2-induced reactive oxygen species (ROS) production. In vivo, 15 significantly attenuated zebrafish anxiety-like behaviour and memory deficits in a SCOP-induced zebrafish model of AD. To sum up, multifunctional 15 might be a good lead to develop novel tetrahydrocarboline-based agents for the treatment of AD.
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000291284 650_7 $$2Other$$aAlzheimer's disease
000291284 650_7 $$2Other$$aHDAC6 inhibitor
000291284 650_7 $$2Other$$aMultimechanism
000291284 650_7 $$2Other$$aSelectivity
000291284 650_7 $$2Other$$aTetrahydrocarboline
000291284 7001_ $$aLiu, Shiru$$b1
000291284 7001_ $$aDang, Baiyun$$b2
000291284 7001_ $$aLuan, Xiaofa$$b3
000291284 7001_ $$aGuo, Yifan$$b4
000291284 7001_ $$0P:(DE-He78)3568511512db56dcce22bfd8cd010c01$$aSteimbach, Raphael$$b5
000291284 7001_ $$0P:(DE-He78)f0af962ddbc82430e947390b2f3f6e49$$aMiller, Aubry$$b6$$udkfz
000291284 7001_ $$aHu, Jiadong$$b7
000291284 7001_ $$aLu, Long$$b8
000291284 7001_ $$aYue, Peiyu$$b9
000291284 7001_ $$aWang, Ruotian$$b10
000291284 7001_ $$aZheng, Meng$$b11
000291284 7001_ $$aGao, Jinming$$b12
000291284 7001_ $$aYin, Xia$$b13
000291284 7001_ $$aChen, Xin$$b14
000291284 773__ $$0PERI:(DE-600)2005170-0$$a10.1016/j.ejmech.2024.116624$$gVol. 275, p. 116624 -$$p116624$$tEuropean journal of medicinal chemistry$$v275$$x0009-4374$$y2024
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