Structural mechanism of GPCR-arrestin interaction: recent breakthroughs
- Authors
- Park, JY[Park, Ji Young]; Lee, SY[Lee, Su Youn]; Kim, HR[Kim, Hee Ryung]; Seo, MD[Seo, Min-Duk]; Chung, KY[Chung, Ka Young]
- Issue Date
- Mar-2016
- Publisher
- PHARMACEUTICAL SOC KOREA
- Citation
- ARCHIVES OF PHARMACAL RESEARCH, v.39, no.3, pp.293 - 301
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- ARCHIVES OF PHARMACAL RESEARCH
- Volume
- 39
- Number
- 3
- Start Page
- 293
- End Page
- 301
- URI
- https://scholarworks.bwise.kr/skku/handle/2021.sw.skku/37593
- DOI
- 10.1007/s12272-016-0712-1
- ISSN
- 0253-6269
- Abstract
- G protein-coupled receptors (GPCRs) are a major membrane receptor family with important physiological and pathological functions. In the classical signaling pathway, ligand-activated GPCRs couple to G proteins, thereby inducing G protein-dependent signaling pathways and phosphorylation by G protein-coupled receptor kinases (GRKs). This leads to an interaction with arrestins, which results in GPCR desensitization. Recently, non-classical GPCR signaling pathways, mediated by GPCR-bound arrestins, have been identified. Consequently, arrestins play important roles in GPCR signaling not only with respect to desensitization but also in relation to G protein-independent signal transduction. These findings have led to efforts to develop functionally biased (i.e. signal transduction biased) GPCR-targeting drugs. One of these efforts is aimed at understanding the structural mechanism of functionally biased GPCR signaling, which includes understanding the G protein-selectivity or arrestin-selectivity of GPCRs. This goal has not yet been achieved; however, great progress has been made during the last 3 years toward understanding the structural mechanism of GPCR-mediated arrestin activation. This review will discuss the recent breakthroughs in the conformational understanding of GPCR-arrestin interaction.
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