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@ARTICLE{Liang:291284,
author = {T. Liang and S. Liu and B. Dang and X. Luan and Y. Guo and
R. Steimbach$^*$ and A. Miller$^*$ and J. Hu and L. Lu and
P. Yue and R. Wang and M. Zheng and J. Gao and X. Yin and X.
Chen},
title = {{M}ultimechanism biological profiling of
tetrahydro-β-carboline analogues as selective {HDAC}6
inhibitors for the treatment of {A}lzheimer's disease.},
journal = {European journal of medicinal chemistry},
volume = {275},
issn = {0009-4374},
address = {Amsterdam [u.a.]},
publisher = {Elsevier Science},
reportid = {DKFZ-2024-01367},
pages = {116624},
year = {2024},
abstract = {With 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.},
keywords = {Alzheimer's disease (Other) / HDAC6 inhibitor (Other) /
Multimechanism (Other) / Selectivity (Other) /
Tetrahydrocarboline (Other)},
cin = {A390},
ddc = {610},
cid = {I:(DE-He78)A390-20160331},
pnm = {311 - Zellbiologie und Tumorbiologie (POF4-311)},
pid = {G:(DE-HGF)POF4-311},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:38925015},
doi = {10.1016/j.ejmech.2024.116624},
url = {https://inrepo02.dkfz.de/record/291284},
}