Matches in SemOpenAlex for { <https://semopenalex.org/work/W2594927333> ?p ?o ?g. }
- W2594927333 endingPage "1326" @default.
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- W2594927333 abstract "For many voltage-gated ion channels (VGICs), creation of a properly functioning ion channel requires the formation of specific protein–protein interactions between the transmembrane pore-forming subunits and cystoplasmic accessory subunits. Despite the importance of such protein–protein interactions in VGIC function and assembly, their potential as sites for VGIC modulator development has been largely overlooked. Here, we develop meta-xylyl (m-xylyl) stapled peptides that target a prototypic VGIC high affinity protein–protein interaction, the interaction between the voltage-gated calcium channel (CaV) pore-forming subunit α-interaction domain (AID) and cytoplasmic β-subunit (CaVβ). We show using circular dichroism spectroscopy, X-ray crystallography, and isothermal titration calorimetry that the m-xylyl staples enhance AID helix formation are structurally compatible with native-like AID:CaVβ interactions and reduce the entropic penalty associated with AID binding to CaVβ. Importantly, electrophysiological studies reveal that stapled AID peptides act as effective inhibitors of the CaVα1:CaVβ interaction that modulate CaV function in an CaVβ isoform-selective manner. Together, our studies provide a proof-of-concept demonstration of the use of protein–protein interaction inhibitors to control VGIC function and point to strategies for improved AID-based CaV modulator design." @default.
- W2594927333 created "2017-03-16" @default.
- W2594927333 creator A5006621344 @default.
- W2594927333 creator A5014388355 @default.
- W2594927333 creator A5021623971 @default.
- W2594927333 creator A5041077365 @default.
- W2594927333 creator A5045437602 @default.
- W2594927333 creator A5051886871 @default.
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- W2594927333 creator A5072508690 @default.
- W2594927333 creator A5075337100 @default.
- W2594927333 creator A5079960105 @default.
- W2594927333 date "2017-03-17" @default.
- W2594927333 modified "2023-10-03" @default.
- W2594927333 title "Stapled Voltage-Gated Calcium Channel (Ca<sub>V</sub>) α-Interaction Domain (AID) Peptides Act As Selective Protein–Protein Interaction Inhibitors of Ca<sub>V</sub> Function" @default.
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