+ |
GRK3 | down-regulates activity
phosphorylation
|
TBXA2R (isoform 2) |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-274090 |
Ser239 |
AQQRPRDsEVEMMAQ |
Homo sapiens |
|
pmid |
sentence |
16956790 |
These data suggest a model whereby agonist-induced PKC phosphorylation of Ser(145) partially impairs TPbeta signalling while GRK2/3 phosphorylation at both Ser(239) and Ser(357) within its IC(3) and C-tail domains, respectively, sterically inhibits G-protein coupling, profoundly desensitizing signalling, and promotes beta-arrestin association and, in turn, facilitates TPbeta internalization. |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-274091 |
Ser357 |
RLPGSSDsRASASRA |
Homo sapiens |
|
pmid |
sentence |
16956790 |
These data suggest a model whereby agonist-induced PKC phosphorylation of Ser(145) partially impairs TPbeta signalling while GRK2/3 phosphorylation at both Ser(239) and Ser(357) within its IC(3) and C-tail domains, respectively, sterically inhibits G-protein coupling, profoundly desensitizing signalling, and promotes beta-arrestin association and, in turn, facilitates TPbeta internalization. |
|
Publications: |
2 |
Organism: |
Homo Sapiens |
+ |
GRK3 | down-regulates activity
phosphorylation
|
CCR5 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-251463 |
Ser336 |
QEAPERAsSVYTRST |
Chlorocebus aethiops |
COS-7 Cell |
pmid |
sentence |
10085131 |
Serine residues at positions 336, 337, 342, and 349 represent GRK phosphorylation sites on CCR5. CCR5 phosphorylation and desensitization through a GRK-mediated mechanism |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-251464 |
Ser337 |
EAPERASsVYTRSTG |
Chlorocebus aethiops |
COS-7 Cell |
pmid |
sentence |
10085131 |
Serine residues at positions 336, 337, 342, and 349 represent GRK phosphorylation sites on CCR5. CCR5 phosphorylation and desensitization through a GRK-mediated mechanism |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-249675 |
Ser342 |
ASSVYTRsTGEQEIS |
Chlorocebus aethiops |
COS-7 Cell |
pmid |
sentence |
10085131 |
Phosphoamino acid analysis revealed that RANTES-induced CCR5 phosphorylation selectively occurs on serine residues. Our findings with receptor mutants indicate that serine residues at positions 336, 337, 342, and 349 represent GRK phosphorylation sites on CCR5. |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-249679 |
Ser349 |
STGEQEIsVGL |
Chlorocebus aethiops |
COS-7 Cell |
pmid |
sentence |
10085131 |
Phosphoamino acid analysis revealed that RANTES-induced CCR5 phosphorylation selectively occurs on serine residues. Our findings with receptor mutants indicate that serine residues at positions 336, 337, 342, and 349 represent GRK phosphorylation sites on CCR5. |
|
Publications: |
4 |
Organism: |
Chlorocebus Aethiops |
+ |
GRK3 | down-regulates activity
phosphorylation
|
BDKRB2 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-251460 |
Ser366 |
EPIQMENsMGTLRTS |
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
11517230 |
Ligand-induced phosphorylation is found at Ser339 and Ser346/Ser348 that could be executed by several G protein-coupled receptor kinases. 32P labeling of peptide 3 containing pS346/pS348 was enhanced 1.5–3-fold as compared with mock-transfected cells in the order GRK6 < GRK5 < GRK2 < GRK4α < GRK3. several endogenous GRKs may phosphorylate the B2R and that the various GRKs, even without apparent effect on total GPCR phosphorylation levels, may induce distinct phosphorylation patterns with possible functional consequences for receptor desensitization and sequestration. |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-249658 |
Ser373 |
SMGTLRTsISVERQI |
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
11517230 |
...expression of GRK4 drastically increased the basal level of32P incorporation into B2R.[]a clustered phosphorylation around Ser(346) is necessary for desensitization of the B2 receptor-induced phospholipase C activation. |
|
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-251462 |
Ser375 |
GTLRTSIsVERQIHK |
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
11517230 |
Ligand-induced phosphorylation is found at Ser339 and Ser346/Ser348 that could be executed by several G protein-coupled receptor kinases. 32P labeling of peptide 3 containing pS346/pS348 was enhanced 1.5–3-fold as compared with mock-transfected cells in the order GRK6 < GRK5 < GRK2 < GRK4α < GRK3. several endogenous GRKs may phosphorylate the B2R and that the various GRKs, even without apparent effect on total GPCR phosphorylation levels, may induce distinct phosphorylation patterns with possible functional consequences for receptor desensitization and sequestration. |
|
Publications: |
3 |
Organism: |
Homo Sapiens |
+ |
GRK3 | down-regulates activity
phosphorylation
|
OPRM1 |
0.2 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-247915 |
Thr182 |
VKALDFRtPRNAKII |
Xenopus laevis |
|
pmid |
sentence |
11060299 |
These results demonstrate that the T180A mutation probably blocks GRK3- and arr3-mediated desensitization of MOR by preventing a critical agonist-dependent receptor phosphorylation and suggest a novel GRK3 site of regulation not yet described for other G-protein-coupled receptors |
|
Publications: |
1 |
Organism: |
Xenopus Laevis |
Tissue: |
Primary Oocyte |