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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 Serine286/Threonine287/Serine288 phosphorylation of the M2 Muscarinic Acetycholine Receptor
pS286/pT287/pS288-M2 (phospho-M2 Muscarinic...
Serine286/Threonine287/Serine288 is a major phosphorylation site of the M2 Muscarinic Acetylcholine Receptor. The pS286/pT287/pS288-M2 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation....
$ 375.00 *
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NEW
Agonist-induced Threonine307/Serine309 phosphorylation of the M2 Muscarinic Acetylcholine Receptor
pT307/pS309-M2 (phospho-M2 Muscarinic...
Threonine307/Serine309 is a major phosphorylation site of the M2 Muscarinic Acetylcholine Receptor. The pT307/pS309-M2 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T307/S309...
$ 375.00 *
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NEW
Agonist-induced Threonine310/Serine311 phosphorylation of the M2 Muscarinic Acetycholine Receptor
pT310/pS311-M2 (phospho-M2 Muscarinic...
Threonine310/Serine311 is a major phosphorylation site of the M2 Muscarinic Acetylcholine Receptor. The pT310/pS311-M2 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T310/S311...
$ 375.00 *
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NEW
Agonist-induced Serine315/Serine320 phosphorylation of the M2 Muscarinic Acetycholine Receptor
pS315/pS320-M2 (phospho-M2 Muscarinic...
Serine315/Serine320 is a major phosphorylation site of the M2 Muscarinic Acetylcholine Receptor. The pS315/pS320-M2 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. S315/S320...
$ 375.00 *
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NEW
Agonist-induced Serine332/Serine333/Serine334 phosphorylation of the M3 Muscarinic Acetycholine Receptor.
pS332/pS333/pS334-M3 (phospho-M3 Muscarinic...
Serine332/Serine333/Serine334 is a major phosphorylation site of the M3 Muscarinic Acetylcholine Receptor. The pS332/pS333/pS334-M3 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation....
$ 375.00 *
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NEW
Agonist-induced Serine359/Threonine361 phosphorylation of the M3 Muscarinic Acetylcholine Receptor
pS359/pT361-M3 (phospho-M3 Muscarinic...
Serine359/Threonine361 is a major phosphorylation site of the M3 Muscarinic Acetylcholine Receptor. The pS359/pT361-M3 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. S359/T361...
$ 375.00 *
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NEW
Agonist-induced Serine385/Serine386 phosphorylation of the M3 Muscarinic Acetylcholine Receptor
pS385/pS386-M3 (phospho-M3 Muscarinic...
Serine385/Serine386 is a major phosphorylation site of the M3 Muscarinic Acetylcholine Receptor. The pS385/pS386-M3 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. S385/S386...
$ 375.00 *
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NEW
Agonist-induced Serine296/Serine297 phosphorylation of the M4 Muscarinic Acetylcholine Receptor
pS296/pS297-M4 (phospho-M4 Muscarinic...
Serine296/Serine297 is a major phosphorylation site of the M4 Muscarinic Acetylcholine Receptor. The pS296/pS297-M4 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. S296/S297...
$ 375.00 *
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NEW
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...
$ 375.00 *
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NEW
Agonist-induced Threonine343/Serine347/Threonine348 phosphorylation of the 5-Hydroxytryptamine Receptor 4
pT343/pS347/pT348-5-HT4 (phospho-5-HT Receptor...
Threonine343/Serine347/Threonine348 is a major phosphorylation site of the 5-HT4 receptor. The pT343/pS347/pT348-5-HT4 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T343/S347/T348...
$ 375.00 *
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NEW
Agonist-induced Serine354/Threonine355 phosphorylation of the 5-Hydroxytryptamine Receptor 4
pS354/pT355-5-HT4 (phospho-5-HT Receptor 4...
Serine354/Threonine355 is a major phosphorylation site of the 5-HT4 receptor. The pS354/pT355-5-HT4 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. S354/T355 phosphorylation is a key...
$ 375.00 *
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NEW
Agonist-induced Serine350/Serine352 phosphorylation of the 5-Hydroxytryptamine Receptor 6
pS350/pS352-5-HT6 (phospho-5-HT Receptor 6...
Serine350/Serine352 is a major phosphorylation site of the 5-HT Receptor 6 (5-HT6). The pS350/pS352-5-HT6 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. S350/S352 phosphorylation is a...
$ 375.00 *
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NEW
Agonist-induced Threonine3545/Serine356 phosphorylation of the 5-Hydroxytryptamine Receptor 6
pT355/pS356-5-HT6 (phospho-5-HT Receptor 6...
Threonine355/Serine356 is a major phosphorylation site of the 5-HT6 receptor. The pT355/pS356-5-HT6 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T355/S356 phosphorylation is a key...
$ 375.00 *
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SAMPLE PACK
Agonist-induced Threonine324/Serine327 phosphorylation of the Complement C5a Receptor 1
C5a1 Sample Pack (phospho- and non-phospho-C5a1...
C51 Sample Pack consisting of all five available phospho- and two non-phospho-C5a1 Receptor Antibodies 7 x 20 µL trial size each. Specifically, this sample pack contains the following antibodies pT324/pS327-C5a1 (7TM0032A),...
$ 400.00 *
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SAMPLE PACK
Agonist-induced Serine355/Serine356 phosphorylation of the β2-Adrenoceptor
β2-Adrenoceptor Sample Pack (phospho- and...
β2-Adrenoceptor Antibody Sample Pack consisting of three phospho- and one non-phospho-β2-Adrenoceptor Antibodies 4 x 20 µL trial size each. Specifically, this sample pack contains the following antibodies pS355/pS356-β2 (7TM0029A),...
$ 300.00 *
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SAMPLE PACK
Agonist-induced Serine331/Threonine332 phosphorylation of the Angiotensin Receptor 1
AT1 Sample Pack (phospho- and...
AT1 Sample Pack consisting of all four available phospho- and non-phospho-AT1 Antibodies 4 x 20 µL trial size each. Specifically, this sample pack contains the following antibodies pS331/pT332-AT1 (7TM0034A), pS335/pT336-AT1 (7TM0034B),...
$ 300.00 *
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11 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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Premium Phosphosite-Specific 7TM Antibodies

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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