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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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pS358/pT360/pS361-CXCR3 (phospho-CXC Chemokine Receptor 3 Antibody)
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.
$ 375.00 *
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Agonist-induced Serine412 phosphorylation of the β1-Adrenoceptor
pS412-β1 (phospho-β1-Adrenoceptor Antibody)
Serine412 (S412) is a major phosphorylation site of the β1 adrenoceptor. The pS412-β1 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S412 phosphorylation is primarily...
$ 375.00 *
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Agonist-induced Serine409/Serine410 phosphorylation of the Neurotensin Receptor 1
pS409/pS410-NTS1 (phospho-Neurotensin Receptor...
Serine409/Serine410 (S409/S410) is major phosphorylation site of the Neurotensin Receptor 1 (NTS1). The pS409/pS410-NTS1 antibody detects phosphorylation in response to agonists. S409/S410 phosphorylation is likely to be involved in...
$ 375.00 *
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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...
$ 375.00 *
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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...
$ 375.00 *
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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...
$ 375.00 *
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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....
$ 375.00 *
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Agonist-induced Serine343/Serine345 phosphorylation of the Apelin Receptor
pS343/pS345-APLNR (phospho-Apelin Receptor...
Serine343/Serine345 (S343/S345) is major phosphorylation site of the Apelin Receptor (APLNR). The pS343/pS345-APLNR antibody detects phosphorylation in response to agonists. S343/S345 phosphorylation is likely to be involved in efficient...
$ 375.00 *
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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...
$ 350.00 *
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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 Serine347/Serine348 phosphorylation of the Apelin Receptor
pS347/pS348-APLNR (phospho-Apelin Receptor...
Serine347/Serine348 (S347/S348) is major phosphorylation site of the Apelin Receptor (APLNR). The pS347/pS348-APLNR antibody detects phosphorylation in response to agonists. S347/S348 phosphorylation is likely to be involved in efficient...
$ 375.00 *
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Agonist-induced Threonine503/Serine504 phosphorylation of the Parathyroid Hormone Receptor 1
pT503/pS504-PTH1 (phospho-Parathyroid Hormone...
Threonine503/Serine504 (T503/S504) is major phosphorylation site of the Parathyroid Hormone Receptor 1 (PTH1). The pT503/pS504-PTH1 antibody detects phosphorylation in response to agonists. T503/S504 phosphorylation is likely to be...
$ 375.00 *
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pS493/pS495-PTH1 (phospho-Parathyroid Hormone Receptor 1 Antibody)
pS493/pS495-PTH1 (phospho-Parathyroid Hormone...
Serine493/Serine495 (S493/S495) is major phosphorylation site of the Parathyroid Hormone Receptor 1 (PTH1). The pS493/pS495-PTH1 antibody detects phosphorylation in response to agonists. S493/S495 phosphorylation is likely to be involved...
$ 375.00 *
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Agonist-induced Serine437/Serine438 phosphorylation of the PACAP Receptor 1
pS437/pS438-PAC1 (phospho-PACAP Receptor 1...
Serine437/Serine438 (S437/S438) is major phosphorylation site of the PACAP Receptor 1 (PAC1). The pS437/pS438-PAC1 antibody detects phosphorylation in response to agonists. S437/S438 phosphorylation is likely to be involved in efficient...
$ 375.00 *
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Agonist-induced Threonine444/Serine447 phosphorylation of the PACAP Receptor 1
pT444/pS447-PAC1 (phospho-PACAP Receptor 1...
Threonine444/Serine447 (T444/S447) is major phosphorylation site of the PACAP Receptor 1 (PAC1). The pT444/pS447-PAC1 antibody detects phosphorylation in response to agonists. T444/S447 phosphorylation is likely to be involved in...
$ 375.00 *
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Agonist-induced Serine450/Serine452 phosphorylation of the PACAP Receptor 1
pS450/pS452-PAC1 (phospho-PACAP Receptor 1...
Serine450/Serine452 (S450/S452) is major phosphorylation site of the PACAP Receptor 1 (PAC1). The pS450/pS452-PAC1 antibody detects phosphorylation in response to agonists. S450/S452 phosphorylation is likely to be involved in efficient...
$ 375.00 *
1 From 19

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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