Pharmacological modulation of ion channels and transporters

Cell Calcium ◽  
2004 ◽  
Vol 35 (6) ◽  
pp. 575-582 ◽  
Author(s):  
Ursula Ravens ◽  
Erich Wettwer ◽  
Ottó Hála
2016 ◽  
Vol 23 (11) ◽  
pp. R517-R525 ◽  
Author(s):  
Iman Azimi ◽  
Gregory R Monteith

A variety of studies have suggested that epithelial to mesenchymal transition (EMT) may be important in the progression of cancer in patients through metastasis and/or therapeutic resistance. A number of pathways have been investigated in EMT in cancer cells. Recently, changes in plasma membrane ion channel expression as a consequence of EMT have been reported. Other studies have identified specific ion channels able to regulate aspects of EMT induction. The utility of plasma membrane ion channels as targets for pharmacological modulation make them attractive for therapeutic approaches to target EMT. In this review, we provide an overview of some of the key plasma membrane ion channel types and highlight some of the studies that are beginning to define changes in plasma membrane ion channels as a consequence of EMT and also their possible roles in EMT induction.


2020 ◽  
Author(s):  
Nina Braun ◽  
Søren Friis ◽  
Christian Ihling ◽  
Andrea Sinz ◽  
Jacob Andersen ◽  
...  

AbstractIncorporation of non-canonical amino acids (ncAAs) can endow proteins with novel functionalities, such as crosslinking or fluorescence. In ion channels, the function of these variants can be studied with great precision using standard electrophysiology, but this approach is typically labor intensive and low throughput. Here, we establish a high-throughput protocol to conduct functional and pharmacological investigations of ncAA-containing hASIC1a (human acid-sensing ion channel 1a) variants in transiently transfected mammalian cells. We introduce three different photocrosslinking ncAAs into 103 positions and assess the function of the resulting 309 variants with automated patch-clamp (APC). We demonstrate that the approach is efficient and versatile, as it is amenable to assessing even complex pharmacological modulation by peptides. The data show that the acidic pocket is a major determinant for current decay and live-cell crosslinking provides insight into the hASIC1a-psalmotoxin-1 interaction. Overall, this protocol will enable future APC-based studies of ncAA-containing ion channels in mammalian cells.


2021 ◽  
Vol Volume 13 ◽  
pp. 693-723
Author(s):  
Madalena C Pinto ◽  
Iris AL Silva ◽  
Miriam F Figueira ◽  
Margarida D Amaral ◽  
Miquéias Lopes-Pacheco

2019 ◽  
Vol 176 (22) ◽  
pp. 4258-4283 ◽  
Author(s):  
Luigi Leanza ◽  
Vanessa Checchetto ◽  
Lucia Biasutto ◽  
Andrea Rossa ◽  
Roberto Costa ◽  
...  

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