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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 Serine335/Serine337 phosphorylation of the Sphingosine 1-Phosphate Receptor 3
pS335/pS337-S1P3 (phospho-Sphingosine...
Serine335/Serine337 (S335/S337) is major phosphorylation site of the Sphingosine 1-Phosphate Receptor 3 (S1P3). The pS335/pS337-S1P3 antibody detects phosphorylation in response to agonists. S335/S337 phosphorylation is likely to be...
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Agonist-induced Threonine360 phosphorylation of the β2-Adrenoceptor
pT360-β2 (phospho-β2-Adrenoceptor Antibody)
Threonine360 (T360) is a major phosphorylation site of the β2 adrenoceptor. The pT360-β2 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. T360 phosphorylation is primarily...
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pT340-GAL1 (phospho-Galanin Receptor 1 Antibody)
pT340-GAL1 (phospho-Galanin Receptor 1 Antibody)
Threonine340 (T340) is a major phosphorylation site of the GAL1 receptor. The pT340-GAL1 antibody detects phosphorylation in response to high-efficacy agonists. T340 phosphorylation is a key regulator of GAL1 desensitization, β-arrestin...
$ 375.00 *
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Validation of the Galanin Receptor 1 in transfected HEK293 cells
GAL1 (non-phospho), Galanin Receptor 1 Antibody
The non-phospho-GAL1 receptor antibody is directed against the carboxyl-terminal tail of human GAL1. It can be used to detect total GAL1 receptors in Western blots independent of phosphorylation. The non-phospho-GAL1 antibody can also be...
$ 300.00 *
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Validation of the Tachykinin Receptor 1 in transfected HEK293 cells
NK1 (non-phospho), Tachykinin Receptor 1 Antibody
The NK1 antibody is directed against the distal end of the carboxyl-terminal tail of human Tachykinin Receptor 1 (also called Substance P Receptor). It detects selectively the canonical full-length NK1 Tachykinin Receptor. It can be used...
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pT344/pS347-NK1 (phospho-Tachykinin Receptor 1 Antibody)
pT344/pS347-NK1 (phospho-Tachykinin Receptor 1...
Threonine344/Serine347 (T344/S347) is a major phosphorylation site of the NK1 receptor. The pT344/pS347-NK1 antibody detects phosphorylation in response to high-efficacy agonists. T344/S347 phosphorylation is a key regulator of NK1...
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Agonist-induced Serine338/Threonine339 phosphorylation of NK1 Receptor
pS338/pT339-NK1 (phospho-Tachykinin Receptor 1...
Serine338/Threonine339 (S338/T339) is a major phosphorylation site of the NK1 receptor. The pS338/pT339-NK1 antibody detects phosphorylation in response to high-efficacy agonists. S338/T339 phosphorylation is a key regulator of NK1...
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pS337/pT341-SST3 (phospho-Somatostatin Receptor 3 Antibody)
pS337/pT341-SST3 (phospho-Somatostatin Receptor...
Serine337/Threonine341 (S337/T341) is a major phosphorylation site of the somatostatin receptor 3 (SST3). The pS337/pT341-SST3 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation....
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pT348-SST3 (phospho-Somatostatin Receptor 3 Antibody)
pT348-SST3 (phospho-Somatostatin Receptor 3...
Threonine348 (T348) is a major phosphorylation site of the somatostatin receptor 3 (SST3). The pT348-SST3 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. T348 phosphorylation...
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Validation of the Somatostatin Receptor 3 in transfected HEK293 cells.
SST3 (non-phospho), Somatostatin Receptor 3...
The non-phospho-SST3 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human SST3. In can be used to detect total SST3 receptors in Western blots independent of phosphorylation. The non-phospho-SST3...
$ 375.00 *
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Agonist-induced Serine361 phosphorylation of the Somatostatin Receptor 3
pS361-SST3 (phospho-Somatostatin Receptor 3...
Serine361 (T361) is a major phosphorylation site of the somatostatin receptor 3 (SST3). The pS361-SST3 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S361 phosphorylation is...
$ 375.00 *
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Agonist-induced Threonine333 phosphorylation of the Somatostatin Receptor 5.
pT333-SST5 (phospho-Somatostatin Receptor 5...
Threonine333 (T333) is a major phosphorylation site of the human somatostatin receptor 5 (SST5). The pT333-SST5 antibody detects phosphorylation in response to high-efficacy agonists such as pasireotide but not after activation of PKC....
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KO-Validated
Validation of the VIP Receptor 2 in transfected HEK293 cells
VPAC2 (non-phospho), VIP Receptor 2 Antibody
The VPAC2 antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human VIP receptor 2. It can be used to detect total VPAC2 receptors in Western blots independent of phosphorylation. The VPAC2...
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Agonist-induced Serine408/Serine409 phosphorylation of VPAC2 Receptor
pS408/pS409-VPAC2 (phospho-VIP Receptor 2...
Serine408/Serine409 (S408/S409) is a major phosphorylation site of the VPAC2 receptor. The pS408/pS409-VPAC2 antibody detects phosphorylation in response to high-efficacy agonists. S408/S409 phosphorylation is a key regulator of VPAC2...
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Agonist-induced Serine411/Serine415 phosphorylation of VPAC2 Receptor
pS411/pS415-VPAC2 (phospho-VIP Receptor 2...
Serine411/Serine415 (S411/S415) is a major phosphorylation site of the VPAC2 receptor. The pS411/pS415-VPAC2 antibody detects phosphorylation in response to high-efficacy agonists. S411/S415 phosphorylation is a key regulator of VPAC2...
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pS425/pS429-VPAC2 (phospho-VIP Receptor 2 Antibody)
pS425/pS429-VPAC2 (phospho-VIP Receptor 2...
Serine425/Serine429 (S425/S429) is a major phosphorylation site of the VPAC2 receptor. The pS425/pS429-VPAC2 antibody detects phosphorylation in response to high-efficacy agonists. S425/S429 phosphorylation is a key regulator of VPAC2...
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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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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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