Structural basis for efonidipine block of a voltage-gated Ca2+ channel
Тип публикации: Journal Article
Дата публикации: 2019-06-01
scimago Q2
wos Q3
БС1
SJR: 0.748
CiteScore: 4.9
Impact factor: 2.2
ISSN: 0006291X, 10902104
PubMed ID:
30981510
Biochemistry
Molecular Biology
Cell Biology
Biophysics
Краткое описание
Efonidipine is a dual L-/T- type calcium channel blocker with a slow onset of action and a long lasting effect that exibihits antihypertensive and nephroprotective effects. differs from most other DHPs which can induce reflex tachycardia. Efonidipine reduces blood pressure without decreasing cardiac output and exerts organ-protective effects on the heart and kidney. In order to investigate how efonidipine block voltage-gated Ca2+ channel, we determined the crystal structure of CaVAb in complex with efonidipine at atomic resolution using x-ray crystallography. Our results reveal that efonidipine targets the central cavity of a model voltage-gated calcium channel underneath its selectivity filter and occlude the channel in an inactivated state. Binding of efonidipine does not break down the fourfold symmetry of the quaternary structure and its pore structure. Our work provides the structural basis for efonidipine block of a voltage-gated Ca2+ channel at the molecular level.
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Xu F. et al. Structural basis for efonidipine block of a voltage-gated Ca2+ channel // Biochemical and Biophysical Research Communications. 2019. Vol. 513. No. 3. pp. 631-634.
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Xu F., Xiong W., Huang Y., Shen J., Zhou D., Tang L. Structural basis for efonidipine block of a voltage-gated Ca2+ channel // Biochemical and Biophysical Research Communications. 2019. Vol. 513. No. 3. pp. 631-634.
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TY - JOUR
DO - 10.1016/j.bbrc.2019.03.176
UR - https://doi.org/10.1016/j.bbrc.2019.03.176
TI - Structural basis for efonidipine block of a voltage-gated Ca2+ channel
T2 - Biochemical and Biophysical Research Communications
AU - Xu, Fuyan
AU - Xiong, Weixi
AU - Huang, Yiman
AU - Shen, Jianghua
AU - Zhou, Dong
AU - Tang, Lin
PY - 2019
DA - 2019/06/01
PB - Elsevier
SP - 631-634
IS - 3
VL - 513
PMID - 30981510
SN - 0006-291X
SN - 1090-2104
ER -
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@article{2019_Xu,
author = {Fuyan Xu and Weixi Xiong and Yiman Huang and Jianghua Shen and Dong Zhou and Lin Tang},
title = {Structural basis for efonidipine block of a voltage-gated Ca2+ channel},
journal = {Biochemical and Biophysical Research Communications},
year = {2019},
volume = {513},
publisher = {Elsevier},
month = {jun},
url = {https://doi.org/10.1016/j.bbrc.2019.03.176},
number = {3},
pages = {631--634},
doi = {10.1016/j.bbrc.2019.03.176}
}
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Xu, Fuyan, et al. “Structural basis for efonidipine block of a voltage-gated Ca2+ channel.” Biochemical and Biophysical Research Communications, vol. 513, no. 3, Jun. 2019, pp. 631-634. https://doi.org/10.1016/j.bbrc.2019.03.176.