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Phosphorylation of intracellular serine and threonine residues is the most important post translational modification of G protein-coupled receptors (GPCRs) also called heptahelical or seven transmembrane receptors (7TMR). After agonist exposure, these receptors acquire an active conformation, which is recognized by a family of highly specialized GPCR kinases (GRKs). Agonist-driven phosphorylation by GRKs regulates acute receptor desensitization, arrestin recruitment, internalization, post-activation signaling, long-term tolerance and drug addiction. Phosphosite-specific 7TM antibodies are designed to specifically detect agonist-activated GPCRs. In fact, recent work shows that ligand profiling using phosphosite-specific 7TM antibodies provides valuble information on ligand bias beyond that obtained with conventional ß-arrestin recruitment assays. Phosphosite-specific 7TM antibodies are novel tools for GPCR research that can be used to:

  • profile agonist properties of novel GPCR ligands
  • decipher the phosphorylation barcode of GPCRs
  • determine the spatial and temporal dynamics of receptor phosphorylation
  • identify relevant kinases and phosphatases for GPCR phosphorylation and dephosphoryation

Lifecycle3

Schematic representation of the G protein-coupled receptor phosphorylation / dephosphorylation cycle. GRK, G protein-coupled receptor kinase; PKC, protein kinase C; cPP1, catalytic subunit of protein phosphatase 1; R*, activated GPCR; CCP, clathrin-coated pit. 

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Agonist-induced Serine364/Threonine365 phosphorylation of the TRH1-Receptor
pS364/pT365-TRH1 (phospho-Thyrotropin-Releasing...
Serine364/Threonine365 (S364/T365) is a major phosphorylation site of the TRH1 receptor. The pS364/pT365-TRH1 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S364/T365...
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Agonist-induced Threonine371 phosphorylation of the TRH1-Receptor
pT371-TRH1 (phospho-Thyrotropin-Releasing...
Threonine371 (T371) is a major phosphorylation site of the TRH1 receptor. The pT371-TRH1 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. T371 phosphorylation is primarily...
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Agonist-induced Threonine389/Threonine390 phosphorylation of the NK3 Receptor3.
pT389/pT390-NK3 (phospho-Tachykinin Receptor 3...
Threonine389/Threonine390 (T389/T390) is a major phosphorylation site of the NK3 receptor. The pT389/pT390-NK3 antibody detects phosphorylation in response to high-efficacy agonists. T389/T390 phosphorylation is a key regulator of NK3...
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Agonist-induced Serine398/Serine399 phosphorylation of the NK 3 Recept
pS398/pS399-NK3 (phospho-Tachykinin Receptor 3...
Serine398/Serine399 (S398/S399) is major phosphorylation site of the Tachykinin Receptor 3 (NK3). The pS398/pS399-NK3 antibody detects phosphorylation in response to agonists. S398/S399 phosphorylation is likely to be involved in...
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Agonist-induced Threonine402/Threonine404 phosphorylation of the NK 3 Receptor.
pT402/pT404-NK3 (phospho-Tachykinin Receptor 3...
Threonine402/Threonine404 (T402/T404) is a major phosphorylation site of the NK3 receptor. The pT402/pT404-NK3 antibody detects phosphorylation in response to high-efficacy agonists. T402/T404 phosphorylation is a key regulator of NK3...
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Agonist-induced Serine345 phosphorylation of the Sphingosine 1-Phosphate Receptor 5
pS345-S1P5 (phospho-Sphingosine 1-Phosphate...
Serine345 (S345) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 5 (S1P5). The pS345-S1P5 antibody detects phosphorylation in response to agonists. S345 phosphorylation is likely to be involved in efficient ligand...
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Agonist-induced Serine359/Serine361/Serine363 phosphorylation of the Sphingosine 1-Phosphate Receptor 5
pS359/pS361/pS363-S1P5 (phospho-Sphingosine...
Serine359/Serine361/Serine363 (S359/S361/S363) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 5 (S1P5). The pS359/pS361/pS363-S1P5 antibody detects phosphorylation in response to agonists. S359/S361/S363...
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Agonist-induced Serine366/Serine367 phosphorylation of the Sphingosine 1-Phosphate Receptor 5
pS366/pS367-S1P5 (phospho-Sphingosine...
Serine366/Ser367 (S366/S367) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 5 (S1P5). The pS366/pS367-S1P5 antibody detects phosphorylation in response to agonists. S366/S367 phosphorylation is likely to be...
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Agonist-induced Serine364/Serine366/Serine368 phosphorylation of the Sphingosine 1-Phosphate Receptor 4
pS364/pS366/pS368-S1P4 (phospho-Sphingosine...
Serine364/Serine366/Serine368 (S364/S366/S368) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 4 (S1P4). The pS364/pS366/pS368-S1P4 antibody detects phosphorylation in response to agonists. S364/S366/S368...
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Agonist-induced Serine330/Serine331 phosphorylation of the Sphingosine 1-Phosphate Receptor 2
pS330/pS331-S1P2 (phospho-Sphingosine...
Serine330/Serine331 (S330/S331) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 2 (S1P2). The pS330/pS331-S1P2 antibody detects phosphorylation in response to agonists. S330/S331 phosphorylation is likely to be...
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pT342/pS343/pT345-S1P2 (phospho-Sphingosine 1-Phosphate Receptor 2 Antibody)
pT342/pS343/pT345-S1P2 (phospho-Sphingosine...
Threonine342Serine343/Threonine345 (T342/S343/T345) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 2 (S1P2). The pT342/pS343/pT345-S1P2 antibody detects phosphorylation in response to agonists. T342/S343/T345...
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Agonist-induced Serine351/Serine353 phosphorylation of the Sphingosine 1-Phosphate Receptor 1
pS351/pS353-S1P1 (phospho-Sphingosine...
Serine351/Serine353 (S351/S353) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 1 (S1P1). The pS351/pS353-S1P1 antibody detects phosphorylation in response to agonists. S351/S353 phosphorylation is likely to be...
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Agonist-induced Serine353/Serine355 phosphorylation of the Sphingosine 1-Phosphate Receptor 1
pS353/pS355-S1P1 (phospho-Sphingosine...
Serine353/Serine355 (S353/S355) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 1 (S1P1). The pS353/pS355-S1P1 antibody detects phosphorylation in response to agonists. S353/S355 phosphorylation is likely to be...
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Agonist-induced Serine358/Serine359 phosphorylation of the Sphingosine 1-Phosphate Receptor 1
pS358/pS359-S1P1 (phospho-Sphingosine...
Serine358/Serine359 (S358/S359) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 1 (S1P1). The pS358/pS359-S1P1 antibody detects phosphorylation in response to agonists. S358/S359 phosphorylation is likely to be...
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Agonist-induced Serine594/Threonine597/Serine599 phosphorylation of the SMO Receptor
pS594/pT597/pS599-SMO (phospho-SMO Receptor...
Serine594/Threonine597/Serine599 (S594/S597/S599) is major GRK2 phosphorylation site of the SMO receptor. The pS594/pT597/pS599-SMO antibody detects phosphorylation in response to agonists. The pS594/pT597/pS599-SMO antibody can be used...
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Agonist-induced Threonine375/Serine376 phosphorylation of the Proteinase-Activated Receptor 2
pT375/pS376-PAR2 (phospho-Proteinase-Activated...
Threonine375/Serine376 (T375/S376) is major phosphorylation site of the Proteinase-Activated Receptor 2 (PAR2). The pT375/pS376-PAR2 antibody detects phosphorylation in response to agonists. T375/S376 phosphorylation is likely to be...
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2 From 18

For further reading refer to:

Kliewer A, Reinscheid RK, Schulz S. Emerging Paradigms of G Protein-Coupled Receptor Dephosphorylation. Trends Pharmacol Sci. 2017 Jul;38(7):621-636. doi:10.1016/j.tips.2017.04.002. Epub 2017 May 4. Review. PubMed PMID: 28478994.

Miess E, Gondin AB, Yousuf A, Steinborn R, Mösslein N, Yang Y, Göldner M, Ruland JG, Bünemann M, Krasel C, Christie MJ, Halls ML, Schulz S, Canals M. Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid μ-opioid receptor desensitization. Sci Signal. 2018 Jul 17;11(539). pii: eaas9609. doi: 10.1126/scisignal.aas9609. PubMed PMID: 30018083.

Kliewer A, Schmiedel F, Sianati S, Bailey A, Bateman JT, Levitt ES, Williams JT, Christie MJ, Schulz S. Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects. Nat Commun. 2019 Jan 21;10(1):367. doi: 10.1038/s41467-018-08162-1. PubMed PMID: 30664663; PubMed Central PMCID: PMC6341117.

Mann A, Moulédous L, Froment C, O'Neill PR, Dasgupta P, Günther T, Brunori G, Kieffer BL, Toll L, Bruchas MR, Zaveri NT, Schulz S. Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists. Sci Signal. 2019 Mar 26;12(574). pii: eaau8072. doi: 10.1126/scisignal.aau8072. PubMed PMID: 30914485; PubMed Central PMCID: PMC6934085.

Saaber F, Schütz D, Miess E, Abe P, Desikan S, Ashok Kumar P, Balk S, Huang K, Beaulieu JM, Schulz S, Stumm R. ACKR3 Regulation of Neuronal Migration Requires ACKR3 Phosphorylation, but Not β-Arrestin. Cell Rep. 2019 Feb 5;26(6):1473-1488.e9. doi: 10.1016/j.celrep.2019.01.049. PubMed PMID: 30726732.

Glück L, Loktev A, Moulédous L, Mollereau C, Law PY, Schulz S. Loss of morphine reward and dependence in mice lacking G protein-coupled receptor kinase 5. Biol Psychiatry. 2014 Nov 15;76(10):767-74. doi: 10.1016/j.biopsych.2014.01.021. Epub 2014 Feb 3. PubMed PMID: 24629717; PubMed Central PMCID: PMC4119866.

For further reading refer to: Kliewer A, Reinscheid RK, Schulz S. Emerging Paradigms of G Protein-Coupled Receptor Dephosphorylation. Trends Pharmacol Sci. 2017 Jul;38(7):621-636.... read more »
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For further reading refer to:

Kliewer A, Reinscheid RK, Schulz S. Emerging Paradigms of G Protein-Coupled Receptor Dephosphorylation. Trends Pharmacol Sci. 2017 Jul;38(7):621-636. doi:10.1016/j.tips.2017.04.002. Epub 2017 May 4. Review. PubMed PMID: 28478994.

Miess E, Gondin AB, Yousuf A, Steinborn R, Mösslein N, Yang Y, Göldner M, Ruland JG, Bünemann M, Krasel C, Christie MJ, Halls ML, Schulz S, Canals M. Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid μ-opioid receptor desensitization. Sci Signal. 2018 Jul 17;11(539). pii: eaas9609. doi: 10.1126/scisignal.aas9609. PubMed PMID: 30018083.

Kliewer A, Schmiedel F, Sianati S, Bailey A, Bateman JT, Levitt ES, Williams JT, Christie MJ, Schulz S. Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects. Nat Commun. 2019 Jan 21;10(1):367. doi: 10.1038/s41467-018-08162-1. PubMed PMID: 30664663; PubMed Central PMCID: PMC6341117.

Mann A, Moulédous L, Froment C, O'Neill PR, Dasgupta P, Günther T, Brunori G, Kieffer BL, Toll L, Bruchas MR, Zaveri NT, Schulz S. Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists. Sci Signal. 2019 Mar 26;12(574). pii: eaau8072. doi: 10.1126/scisignal.aau8072. PubMed PMID: 30914485; PubMed Central PMCID: PMC6934085.

Saaber F, Schütz D, Miess E, Abe P, Desikan S, Ashok Kumar P, Balk S, Huang K, Beaulieu JM, Schulz S, Stumm R. ACKR3 Regulation of Neuronal Migration Requires ACKR3 Phosphorylation, but Not β-Arrestin. Cell Rep. 2019 Feb 5;26(6):1473-1488.e9. doi: 10.1016/j.celrep.2019.01.049. PubMed PMID: 30726732.

Glück L, Loktev A, Moulédous L, Mollereau C, Law PY, Schulz S. Loss of morphine reward and dependence in mice lacking G protein-coupled receptor kinase 5. Biol Psychiatry. 2014 Nov 15;76(10):767-74. doi: 10.1016/j.biopsych.2014.01.021. Epub 2014 Feb 3. PubMed PMID: 24629717; PubMed Central PMCID: PMC4119866.

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