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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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pT442/pS443-GIPR (phospho-Gastric Inhibitory Polypeptide Receptor Antibody)
pT442/pS443-GIPR (phospho-Gastric Inhibitory...
Threonine442/Serine443 (T442/S443) is major phosphorylation site of human GIP receptor. The pT442/pS443-GIPR antibody detects phosphorylation in response to agonists. T442/S443 phosphorylation is likely to be involved in efficient ligand...
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Agonist-induced Serine433/Serine435 phosphorylation of GIPR
pS433/pS435-GIPR (phospho-Gastric Inhibitory...
Serine433/Serine435 (S433/S435) is major phosphorylation site of human GIP receptor. The pS433/pS435-GIPR antibody detects phosphorylation in response to agonists. S433/S435 phosphorylation is likely to be involved in efficient ligand...
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Agonist-induced Threoine339/Serine341 phosphorylation of GPR132
pT339/pS341-GPR132 (phospho-GPR132 Antibody)
Threonine339/Serine341 (T339/S341) is major phosphorylation site of human GPR132 receptor. The pT339/pS341-GPR132 antibody detects phosphorylation in response to agonists. T339/S341 phosphorylation is likely to be involved in efficient...
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Agonist-induced Threonine344/Serine349 phosphorylation of GPR132
pT344/pS349-GPR132 (phospho-GPR132 Antibody)
Threonine344/Serine349 (T344/S349) is major phosphorylation site of human GPR132 receptor. The pT344/pS349-GPR132 antibody detects phosphorylation in response to agonists. T344/S349 phosphorylation is likely to be involved in efficient...
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Agonist-induced Threonine358/Serine360 phosphorylation of GPR132
pT358/pS360-GPR132 (phospho-GPR132 Antibody)
Threonine358/Serine360 (T358/S360) is major phosphorylation site of human GPR132 receptor. The pT358/pS360-GPR132 antibody detects phosphorylation in response to agonists. T358/S360 phosphorylation is likely to be involved in efficient...
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Agonist-induced Serine221/Serine224 phosphorylation of GPR84
pS221/pS224-GPR84 (phospho-GPR84 Antibody)
Serine221/Serine224 (S221/S224) is major phosphorylation site of human GPR84 receptor. The pS221/pS224-GPR84 antibody detects phosphorylation in response to agonists. S221/S224 phosphorylation is likely to be involved in efficient ligand...
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Agonist-induced Threonine263/Threonine264 phosphorylation of GPR84
pT263/pT264-GPR84 (phospho-GPR84 Antibody)
Threonine263/Threonine264 (T263/T264) is major phosphorylation site of human GPR84 receptor. The pT263/pT264-GPR84 antibody detects phosphorylation in response to agonists. T263/T264 phosphorylation is likely to be involved in efficient...
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Agonist-induced Threonine347 phosphorylation of the FFA Receptor 4
pT347-FFA4 (phospho-FFA4 Antibody)
Threonine347 (T347) is major phosphorylation site of the FFA Receptor 4 (FFA4). The pT347-FFA4 antibody detects phosphorylation in response to agonists. T347 phosphorylation is likely to be involved in efficient ligand sequestration by...
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Agonist-induced Threonine349/Serine350 phosphorylation of the FFA Receptor 4
pT349/pS350-FFA4 (phospho-FFA4 Antibody)
Threonine349/Serine350 (T349/S350) is major phosphorylation site of the FFA Receptor 4 (FFA4). The pT349/pS350-FFA4 antibody detects phosphorylation in response to agonists. T349/S350 phosphorylation is likely to be involved in efficient...
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Agonist-induced Serine305/Serine306 phosphorylation of the FFA Receptor 3
pS305/pS306-FFA3 (phospho-FFA3 Antibody)
Serine305/Serine306 (S305/S306) is major phosphorylation site of the FFA Receptor 3 (FFA3). The pS305/pS306-FFA3 antibody detects phosphorylation in response to agonists. S305/S306 phosphorylation is likely to be involved in efficient...
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Agonist-induced Threonine328/Serine329 phosphorylation of the FFA Receptor 3
pT328/pS329-FFA3 (phospho-FFA3 Antibody)
Threonine328/Serine329 (T328/S329) is major phosphorylation site of the FFA Receptor 3 (FFA3). The pT328/pS329-FFA3 antibody detects phosphorylation in response to agonists. T328/S329 phosphorylation is likely to be involved in efficient...
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Agonist-induced Threonine306/Threonine310 phosphorylation of the FFA2 Receptor
pT306/pT310-FFA2 (phospho-FFA2 Antibody)
Threonine306/Threonine310 (T306/T310) is major phosphorylation site of the FFA 2 Receptor (FFA2). The pT306/pT310-FFA2 antibody detects phosphorylation in response to agonists. T306/T310 phosphorylation is likely to be involved in...
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Constitutive Serine296/Serine297 phosphorylation of the FFA Receptor 2
pS296/pS297-FFA2 (phospho-FFA2 Antibody)
Serine296/Serine297 (S296/S297) is major phosphorylation site of the FFA Receptor 2 (FFA2). The pS296/pS297-FFA2 antibody detects constitutive phosphorylation of FFA2.
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Agonist-induced Serine435/Serine436 phosphorylation of the Endothelin Receptor B
pS435/pS436-ETB (phospho-Endothelin Receptor B...
Serine435/Serine436 (S435/S436) is major phosphorylation site of the Endothelin Receptor B (ETB). The pS435/pS436-ETB antibody detects phosphorylation in response to agonists. S435/S436 phosphorylation is likely to be involved in...
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Agonist-induced Threonine382/Threonine386 phosphorylation of the Dopamine Receptor 5
pT382/pT386-D5 (phospho-Dopamine Receptor 5...
Threonine382/Threonine386 (T382/T386) is a major phosphorylation site of the D5 receptor. The pT382/pT386-D5 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. T382/T386...
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Agonist-induced Serine257/Threonine262 phosphorylation of the D3 Dopamine Receptor
pS257/pT262-D3 (phospho-Dopamine Receptor 3...
Serine257/Threonine262 (S257/T262) is a major phosphorylation site of the D3 dopamine receptor. The pS257/pT262-D3 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S262/T262...
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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.

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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