Tubeimoside I Antagonizes Yoda1-Evoked Piezo1 Channel Activation

Frontiers in Pharmacology
Silin LiuJing Li

Abstract

Piezo1, a mechanosensitive Ca2+-permeable non-selective cationic ion channel protein, is involved in a wide range of biological processes and plays crucial roles in vascular development. However, the pharmacology of this protein is in its infancy. Yoda1, the first specific chemical activator of Piezo1 channels, can activate Piezo1 in absence of mechanical stimulation. Hence, we sought to identify inhibitors of Yoda1 from Traditional Chinese Medicine (TCM). Intracellular Ca2+ measurements were conducted in human umbilical vein endothelial cells (HUVECs), HEK 293T cells overexpressing TRPC5 and TRPM2 channels, as well as in CHO K1 cells overexpressing TRPV4 channels. We identified tubeimoside I (TBMS1) as a strong inhibitor of the Yoda1 response and demonstrated its selectivity for the Piezo1 channels. Similarly, Yoda1-induced inhibitory results were obtained in Piezo1 wild-type overexpressed cells, murine liver endothelial cells (MLECs), and macrophages. The physiological responses of TBMS1 were identified by isometric tension, which can inhibit Yoda1 relaxation of aortic rings. Our results demonstrated that TBMS1 can effectively antagonize Yoda1 induced Piezo1 channel activation. This study sheds light on the existence of Yoda1...Continue Reading

References

Dec 1, 2007·Circulation Research·Claudie M HecquetAsrar B Malik
Feb 22, 2012·Nature·Bertrand CosteArdem Patapoutian
Jun 25, 2014·Proceedings of the National Academy of Sciences of the United States of America·Sanjeev S RanadeArdem Patapoutian
Feb 25, 2015·Angewandte Chemie·Yasemin AkbulutHerbert Waldmann
May 23, 2015·ELife·Ruhma SyedaArdem Patapoutian
Sep 22, 2015·Nature·Jingpeng GeMaojun Yang
Oct 17, 2016·Trends in Biochemical Sciences·Jason WuJörg Grandl
Nov 2, 2016·Haematologica·Immacolata AndolfoAchille Iolascon
Dec 13, 2017·ELife·Yusong R Guo, Roderick MacKinnon
Dec 21, 2017·Nature·Kei SaotomeAndrew B Ward
Feb 23, 2018·Nature·Qiancheng ZhaoBailong Xiao
Mar 3, 2018·British Journal of Pharmacology·Elizabeth L EvansDavid J Beech
Aug 18, 2018·Journal of Analytical Methods in Chemistry·Lianguo ChenYunfang Zhou
Nov 16, 2018·European Journal of Medicinal Chemistry·Md Sodrul IslamHongxiang Sun

❮ Previous
Next ❯

Citations

Aug 6, 2021·Journal of Inflammation Research·Shafiu A Umar ShingeFengxu Yu
Jan 6, 2022·Science Translational Medicine·Wandi ZhuCalum A MacRae
Dec 3, 2020·Journal of Ethnopharmacology·Xiyang YangJianghong Yan

❮ Previous
Next ❯

Methods Mentioned

BETA
FCS
magnetically
PCR
protein assay

Software Mentioned

Image Quant
Origin Pro

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.