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Overview

Uniprot IDF1LMA4
Protein NameG protein-coupled receptor kinase
Gene NameGrk2
OrganismRattus norvegicus

Kla Sites from experimental identification

Position Flanking peptide
563 ARKKAKNKQLGHEED

Function

Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Phosphorylates catecholamine-activated ADRB2 to regulate physiological cardiomyocyte contraction rate responses. Also phosphorylates ligand-bound C3a and C5a anaphylatoxin receptors (C3AR1 and C5AR1, respectively), leading to receptor desensitization. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner. Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by facilitating the trafficking of SMO into the cilium and the stimulation of SMO activity. Inhibits relaxation of airway smooth muscle in response to blue light

Protein Sequence

10 MADLEAVLAD 20 VSYLMAMEKS 30 KATPAARASK 40 KILLPEPSIR 50 SVMQKYLEDR 60 GEVTFEKIFS 70 QKLGYLLFRD 80 FCLNHLEEAK 90 PLVEFYEEIK 100 KYEKLETEEE 110 RVVRSREIFD 120 SYIMKELLAC 130 SHPFSKNATE 140 HVQGHLVKKQ 150 VPPDLFQPYI 160 EEICQNLRGD 170 VFHKFIESDK 180 FTRFCQWKNV 190 ELNIHLTMND 200 FSVHRIIGRG 210 GFGEVYGCRK 220 ADTGKMYAMK 230 CLDKKRIKMK 240 QGETLALNER 250 IMLSLVSTGD 260 CPFIVCMSYA 270 FHTPDKLSFI 280 LDLMNGGDLH 290 YHLSQHGVFS 300 EADMRFYAAE 310 IILGLEHMHN 320 RFVVYRDLKP 330 ANILLDEHGH 340 VRISDLGLAC 350 DFSKKKPHAS 360 VGTHGYMAPE 370 VLQKGVAYDS 380 SADWFSLGCM 390 LFKLLRGLPY 400 LLPASSIILP 410 HFSHSCFLTL 420 HKTKDKHEID 430 RMTLTMVSVR 440 LPDSFSPELR 450 SLLEGLLQRD 460 VNRRLGCLGR 470 GAQEVKESPF 480 FRSLDWQMVF 490 LQKYPPPLIP 500 PRGEVNAADA 510 FDIGSFDEED 520 TKGIKLLDSD 530 QELYRNFPLT 540 ISERWQQEVA 550 ETVFDTINAE 560 TDRLEARKKA 570 KNKQLGHEED 580 YALGKDCIMH 590 GYMSKMGNPF 600 LTQWQRRYFY 610 LFPNRLEWRG 620 EGEAPQSLLT 630 MEEIQSVEET 640 QIKERKCLLL 650 KIRGGKQFVL 660 QCDSDPELVQ 670 WKKELRDAYR 680 EAQQLVQRVP 690 KMKNKPRSPV 700 VELSKVPLIQ RGSANGL

Gene Ontology

Classification GO ID Description
Cellular Component GO:0032473 cytoplasmic side of mitochondrial outer membrane
Biological Process GO:0060048 cardiac muscle contraction
Biological Process GO:0002029 desensitization of G protein-coupled receptor signaling pathway
Biological Process GO:1901081 negative regulation of relaxation of smooth muscle
Biological Process GO:0045988 negative regulation of striated muscle contraction
Biological Process GO:0003108 negative regulation of the force of heart contraction by chemical signal
Biological Process GO:0031623 receptor internalization
Biological Process GO:0046718 symbiont entry into host cell
Biological Process GO:0007217 tachykinin receptor signaling pathway
Biological Process GO:0019079 viral genome replication
Cellular Component GO:0005829 cytosol
Cellular Component GO:0005886 plasma membrane
Cellular Component GO:0098794 postsynapse
Cellular Component GO:0098793 presynapse
Molecular Function GO:0005524 ATP binding
Molecular Function GO:0047696 beta-adrenergic receptor kinase activity
Molecular Function GO:0031755 Edg-2 lysophosphatidic acid receptor binding
Molecular Function GO:0004703 G protein-coupled receptor kinase activity

Reference

[1] Chen Y, Sun W, Sun Z, Zhao H, Wu T et al.. Effect of electroacupuncture on hippocampal protein lactylation in a rat model of vascular dementia.. Front Neurol 16:1629474. 2025. PMID: 40963935.