Assays for detecting arrestin interaction with GPCRs
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Assays for detecting arrestin interaction with GPCRs. / Perry-Hauser, Nicole A.; Asher, Wesley B.; Hauge Pedersen, Maria; Javitch, Jonathan A.
Biomolecular Interactions Part A. ed. / Arun K. Shukla. Academic Press, 2021. p. 43-65 (Methods in Cell Biology, Vol. 166).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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TY - CHAP
T1 - Assays for detecting arrestin interaction with GPCRs
AU - Perry-Hauser, Nicole A.
AU - Asher, Wesley B.
AU - Hauge Pedersen, Maria
AU - Javitch, Jonathan A.
N1 - Publisher Copyright: © 2021 Elsevier Inc.
PY - 2021
Y1 - 2021
N2 - The four vertebrate arrestins play a key role in the desensitization and internalization of G protein-coupled receptors (GPCRs) and also mediate receptor-dependent signaling. Recent work has shown that bias for arrestin vs G protein signaling could offer certain therapeutic advantages (or disadvantages) in different systems, making assays that measure arrestin binding to receptors important for drug discovery efforts. Herein, we briefly review several commonly used techniques for measuring arrestin binding to receptors, as well as provide an in-depth and methodologically focused review of two methods that do not require receptor modification. The first approach measures direct binding between purified arrestin and rhodopsin, and the second measures the recruitment of arrestin to receptors in living cells.
AB - The four vertebrate arrestins play a key role in the desensitization and internalization of G protein-coupled receptors (GPCRs) and also mediate receptor-dependent signaling. Recent work has shown that bias for arrestin vs G protein signaling could offer certain therapeutic advantages (or disadvantages) in different systems, making assays that measure arrestin binding to receptors important for drug discovery efforts. Herein, we briefly review several commonly used techniques for measuring arrestin binding to receptors, as well as provide an in-depth and methodologically focused review of two methods that do not require receptor modification. The first approach measures direct binding between purified arrestin and rhodopsin, and the second measures the recruitment of arrestin to receptors in living cells.
KW - Arrestin
KW - Cell signaling
KW - G protein-coupled receptors (GPCRs)
KW - Unmodified receptor
U2 - 10.1016/bs.mcb.2021.06.007
DO - 10.1016/bs.mcb.2021.06.007
M3 - Book chapter
C2 - 34752339
AN - SCOPUS:85110557952
SN - 9780128233511
T3 - Methods in Cell Biology
SP - 43
EP - 65
BT - Biomolecular Interactions Part A
A2 - Shukla, Arun K.
PB - Academic Press
ER -
ID: 298039741