Abstract:
:The G protein-coupled receptor kinase (GRK) family consists of seven cytosolic serine/threonine (Ser/Thr) protein kinases, and among them, GRK2 is involved in the regulation of an enormous range of both G protein-coupled receptors (GPCRs) and non-GPCR substrates that participate in or regulate many critical cellular processes. GRK2 dysfunction is associated with multiple diseases, including cancers, brain diseases, cardiovascular and metabolic diseases, and therefore GRK2-specific substrates/inhibitors are needed not only for studies of GRK2-mediated cellular functions but also for GRK2-targeted drug development. Here, we first review the structure, regulation and functions of GRK2, and its synthetic substrates and inhibitors. We then highlight recent work on synthetic peptide substrates/inhibitors as promising tools for fundamental studies of the physiological functions of GRK2, and as candidates for applications in clinical diagnostics.
journal_name
Amino Acidsjournal_title
Amino acidsauthors
Kang JH,Toita R,Kawano T,Murata M,Asai Ddoi
10.1007/s00726-020-02864-xsubject
Has Abstractpub_date
2020-07-01 00:00:00pages
863-870issue
6-7eissn
0939-4451issn
1438-2199pii
10.1007/s00726-020-02864-xjournal_volume
52pub_type
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