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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 Serine358/Threonine360/Serine361 phosphorylation of the CXC Chemokine Receptor 3
pS358/pT360/pS361-CXCR3 (phospho-CXC Chemokine...
Serine358/Threonine360/Serine361 (S358/T360/S361) are a major phosphorylation sites of the CXCR3 receptor. The pS358/pT360/pS361-CXCR3 detects phosphorylation in response to high- and low-efficacy agonists. S358/T360/S361 phosphorylation...
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Agonist-induced Serine501/Threonine503/Serine504 phosphorylation of the Parathyroid Hormone Receptor 1
pS501/pT503/pS504-PTH1 (phospho-Parathyroid...
Serine501/Threonine503/Serine504 (S501/T503/S504) is major phosphorylation site of the Parathyroid Hormone Receptor 1 (PTH1). The pS501pT503/pS504-PTH1 antibody detects phosphorylation in response to agonists. S501T503/S504...
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Agonist-induced Serine492/Serine493 phosphorylation of the Parathyroid Hormone Receptor 1
pS492/pS493-PTH1 (phospho-Parathyroid Hormone...
Serine492/Serine493 (S492/S493) is major phosphorylation site of the Parathyroid Hormone Receptor 1 (PTH1). The pS492/pS493-PTH1 antibody detects phosphorylation in response to agonists. S492/S493 phosphorylation is likely to be involved...
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Agonist-induced Threoine347/Serine349 phosphorylation of GPR183
pT347/pT349-GPR183 (phospho-GPR183 Antibody)
Threonine347/Threonine349 (T347/T349) is major phosphorylation site of human GPR183 receptor. The pT347/pT349-GPR183 antibody detects phosphorylation in response to agonists. T347/T349 phosphorylation is likely to be involved in...
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Agonist-induced Serine355 phosphorylation of GPR183
pS355-GPR183 (phospho-GPR183 Antibody)
Serine355 (S355) is major phosphorylation site of human GPR183 receptor. The pS355-GPR183 antibody detects phosphorylation in response to agonists. S355 phosphorylation is likely to be involved in efficient ligand sequestration by GPR183.
$ 375.00 *
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Agonist-induced Serine343 phosphorylation of GPR183
pS343-GPR183 (phospho-GPR183 Antibody)
Serine343 (S343) is major phosphorylation site of human GPR183 receptor. The pS343-GPR183 antibody detects phosphorylation in response to agonists. S343 phosphorylation is likely to be involved in efficient ligand sequestration by GPR183.
$ 375.00 *
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Agonist-induced Serine381/Serine382 phosphorylation of the Proteinase-Activated Receptor 4
pS381/pS382-PAR4 (phospho-Proteinase-Activated...
Serine381/Serine382 (S381/S382) is a major phosphorylation site of the Proteinase-Activated Receptor 4 (PAR4). The pS381/pS382-PAR4 antibody detects phosphorylation in response to agonists. S381/S382 phosphorylation is likely to be...
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Agonist-induced Serine374/Threonine379 phosphorylation of the Proteinase-Activated Receptor 4
pS374/pT379-PAR4 (phospho-Proteinase-Activated...
Serine374/Threonine379 (S374/T379) is a major phosphorylation site of the Proteinase-Activated Receptor 4 (PAR4). The pS374/pT379-PAR4 antibody detects phosphorylation in response to agonists. S374/T379 phosphorylation is likely to be...
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Agonist-induced Serine366/Serine369 phosphorylation of the Proteinase-Activated Receptor 4
pS366/pS369-PAR4 (phospho-Proteinase-Activated...
Serine366/Serine369 (S366/S369) is a major phosphorylation site of the Proteinase-Activated Receptor 4 (PAR4). The pS366/pS369-PAR4 antibody detects phosphorylation in response to agonists. S366/S369 phosphorylation is likely to be...
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Agonist-induced Serine422/Serine425 phosphorylation of the Calcitonin Recepto
pS422/pS425-CT (phospho-Calcitonin Receptor...
Serine422/Serine425 (S422/S425) is a major phosphorylation site of the Calcitonin receptor. The pS422/pS425-CT antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S422/S425...
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Agonist-induced Serine327/Serine328 phosphorylation of the MRGPRX2 Mas-related Receptor
pS327/pS328-MRGPRX2 (phospho-MRGPRX2...
Serine327/Serine328 (S327/S329) is a major phosphorylation site of the MRGPRX2 Mas-related receptor. The pS327/pS328-MRGPRX2 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation....
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Agonist-induced Serine339/Serine340 phosphorylation of the Chemokine Receptor CX3CR1
pS339/pS340-CX3CR1 (phospho-CX3CR1 Chemokine...
Serine339/Serine340 (S339/S340) is a major phosphorylation site of the CX3CR1 receptor. The pS339/pS340-CX3CR1 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S339/S340...
$ 375.00 *
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pS327/pS329-CX3CR1 (phospho-CX3CR1 Chemokine Receptor Antibody)
pS327/pS329-CX3CR1 (phospho-CX3CR1 Chemokine...
Serine327/Serine329 (S327/S329) is a major phosphorylation site of the CX3CR1 receptor. The pS327/pS329-CX3CR1 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S327/S329...
$ 375.00 *
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Agonist-induced Serine313 phosphorylation of the MRGPRX2 Mas-related Receptor
pS313-MRGPRX2 (phospho-MRGPRX2 Mas-related...
Serine313 (S313) is a major phosphorylation site of the MRGPRX2 Mas-related receptor. The pS313-MRGPRX2 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S313 phosphorylation is a...
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Agonist-induced Serine261/Serine262 phosphorylation of the β2-Adrenoceptor
pS261pS262-β2 (phospho-β2-Adrenoceptor Antibody)
Serine261/Serine262 (S261/S262) is a major phosphorylation site of the β2 adrenoceptor. The pS261/pS262-β2 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S261/S262...
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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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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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