
Structural insight into the allosteric inhibition of human sodium ...
Dec 15, 2023 · We speculate that the enhanced sensitivity of SEA0400 to NCX1 via XIP is due to the fact that XIP stabilizes TM2ab of NCX1.3 IF at a certain conformation that preferentially binds with SEA0400, and thus the XIP and SEA0400 synergistically inhibit Ca 2+ …
A New Cell-penetrating Peptide That Blocks the Autoinhibitory XIP ...
Jun 11, 2014 · The plasma membrane Na + /Ca 2+ exchanger (NCX) is a high-capacity ionic transporter that exchanges three Na + ions for one Ca 2+ ion. Depending on electrochemical gradients and membrane potential, NCX functions in either the Ca 2+ -efflux (forward) or the Ca 2+ -influx (reverse) mode.
Cardiac Sodium-Calcium Exchanger Is Regulated by Allosteric …
Nov 18, 2004 · In the present study, we use adenoviral gene transfer technology and mutational analysis of NCX to identify a region on the C-terminal domain of the f-loop that is critically involved in regulation of the NCX by XIP, but not allosteric Ca …
Partial Inhibition of Sodium/Calcium Exchange Restores Cellular Calcium ...
Aug 6, 2004 · We studied the effect of partially correcting the NCX overexpression (by applying an exchange inhibitory peptide [XIP]) in a canine model of heart failure.
20 Years from NCX Purification and Cloning: Milestones
The peptide is known as XIP (exchanger inhibitory peptide). It appears that the endogenous XIP region of NCX is involved in autoregulation though the exact role of the XIP region is still not fully defined.
New perspectives for selective NCX activators in neurodegenerative ...
May 1, 2020 · Since the binding between P1 and XIP domains, respectively located on the N- and C-terminal portion of f-loop, inhibits NCX activity a new pharmacological strategy is represented by drugs able to block the XIP domain on NCX1.
A new cell-penetrating peptide that blocks the autoinhibitory XIP ...
The plasma membrane Na (+)/Ca (2+) exchanger (NCX) is a high-capacity ionic transporter that exchanges 3Na (+) ions for 1Ca (2+) ion. The first 20 amino acids of the f-loop, named exchanger inhibitory peptide (XIP (NCX1)), represent an autoinhibitory region involved in the Na (+)-dependent inactivation of …
Structural insight into the allosteric inhibition of human sodium ...
In addition to the CBD1/2, the exchanger inhibitory peptide (XIP) region located within the f-loop has also been determined to block NCX activity in response to high concentration of cytosolic sodium ion ( [Na +] in) (Li et al, 1991; Matsuoka et al, 1997b).
Cardiac sodium-calcium exchanger is regulated by allosteric ... - PubMed
Jan 7, 2005 · The sarcolemmal Na+-Ca2+ exchanger (NCX) is the main Ca2+ extrusion mechanism in cardiac myocytes and is thus essential for the regulation of Ca2+ homeostasis and contractile function.
Structure-Function Studies of the XIP Regions of the Na+-Ca2 ...
The Na + -Ca 2+ exchanger (NCX) is an integral protein essential for cellular Ca 2+ homeostasis. Previous structure-function studies have identified regulatory regions within the exchanger's cytoplasmic domain, of which the XIP region shown to be involved in the rate and extent of Na + -dependent inactivation (I 1 ).