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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 Serine319/Serine322 phosphorylation of the H2 Histamine Receptor
pS319/pS322-H2 (phospho-H2 Histamine Receptor...
Serine319/Ser322 are major phosphorylation site of the H2 histamine receptor. The pS319/pS322-H2 antibody detects phosphorylation in response to high-efficacy agonists. S319/S322 phosphorylation is a key regulator of H2 desensitization,...
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Agonist-induced Serine320/Threonine324 phosphorylation of the Leukotriene Receptor BLT2.
pS320/pT324-BLT2 (phospho-Leukotriene Receptor...
Serine320/Threonine324 (S320/T324) is a major phosphorylation site of the BLT2 receptor. The pS320/pT324-BLT2 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S320/T324...
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pT329/pT330-BLT2 (phospho-Leukotriene Receptor BLT2 Antibody)
pT329/pT330-BLT2 (phospho-Leukotriene Receptor...
Threonine329/Threonine330 (T329/T330) is a major phosphorylation site of the BLT2 receptor. The pT329/pT330-BLT2 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. T329/T330...
$ 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...
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Agonist-induced Serine351 phosphorylation of the Apelin Receptor
pS351-APLNR (phospho-Apelin Receptor Antibody)
Serine351 (S351) is major phosphorylation site of the Apelin Receptor (APLNR). The pS351-APLNR antibody detects phosphorylation in response to agonists. S351 phosphorylation is likely to be involved in efficient ligand sequestration by...
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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 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 Serine336/Serine337 phosphorylation of the Chemokine Receptor 5
pS336/pS337-CCR5 (phospho-Chemokine Receptor 5...
Serine336/Serine337 (S336/S337) is a major phosphorylation site of the CCR5 receptor. The pS336/pS337-CCR5 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S336/S337...
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Agonist-induced Threonine353 phosphorylation of the Chemokine Receptor 10
pT353-CCR10 (phospho-Chemokine Receptor 10...
Threonine353 (T353) is a major phosphorylation site of the CCR10 receptor. The pT353-CCR10 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. T353 phosphorylation is a key regulator...
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Agonist-induced Serine357 phosphorylation of the Chemokine Receptor 6
pS357-CCR6 (phospho-Chemokine Receptor 6 Antibody)
Serine357 (S357) is a major phosphorylation site of the CCR6 receptor. The pS357-CCR6 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S357 phosphorylation is a key regulator of...
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Agonist-induced Serine298 phosphorylation of the M1 Muscarinic Acetylcholine Receptor
pS298-M1 (phospho-M1 Muscarinic Acetylcholine...
Serine298 is a major phosphorylation site of the M1 muscarinic acetylcholine receptor. The pS298-M1 antibody detects phosphorylation in response to high-efficacy agonists.
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Agonist-induced Threonine271 phosphorylation of the M2 Muscarinic Acetycholine Receptor
pT271-M2 (phospho-M2 Muscarinic Acetylcholine...
Threonine271 is a major phosphorylation site of the M2 Muscarinic Acetylcholine Receptor. The pT271-M2 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T271 phosphorylation is a key...
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Agonist-induced Threonine311/Serine314 phosphorylation of the M4 Muscarinic Acetylcholine Receptor
pT311/pS314-M4 (phospho-M4 Muscarinic...
Threonine311/Serine314 is a major phosphorylation site of the M4 Muscarinic Acetylcholine Receptor. The pT311/pS314-M4 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T311/S314...
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Agonist-induced Serine346/Serine349/Threonine352 phosphorylation of the NPS Receptor
pS346/pS349/pT352-NPSR (phospho-NPS Receptor...
Serine346/Serine349/threonine352 (S346/S349/T352) is major phosphorylation site of the NPS Receptor (NPSR). The pS346/pS349/pT352-NPRS antibody detects phosphorylation in response to agonists. S346/S349/T352 phosphorylation is likely to...
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Agonist-induced Serine412/Serine413 phosphorylation of the Protease-Activated Receptor
pS412/pS413-PAR1 (phospho-Proteinase-Activated...
Serine412/Serine413 (S412/S413) is major phosphorylation site of the Proteinase-Activated Receptor 1 (PAR1). The pS412/pS413-PAR1 antibody detects phosphorylation in response to agonists. S412/S413 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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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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