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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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Immunohistochemical identification of DP1 Prostanoid receptor 1 in kidney
DP1 (IHC-grade), DP1 Prostanoid Receptor Antibody
The non-phospho-DP1 Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human DP1. It can be used to detect total DP1 receptors in Western blots independent of phosphorylation. The non-phospho-DP1...
£ 335.00 *
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Validation of the DP1 Prostanoid Receptor in transfected HEK293 cells
DP1 (non-phospho), DP1 Prostanoid Receptor...
The non-phospho-DP1 Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human DP1. It can be used to detect total DP1 receptors in Western blots independent of phosphorylation. The non-phospho-DP1...
£ 335.00 *
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Validation of the Dopamine Receptor 5 in transfected HEK293 cells
D5 (non-phospho), Dopamine Receptor 5 Antibody
The non-phospho-Dopamine Receptor 5 Antibody is directed against the distal end of the carboxyl-terminal tail of human D5. It can be used to detect total D5 receptors in Western blots independent of phosphorylation. The non-phospho-D5...
£ 335.00 *
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Immunohistochemical identification of CC Chemokine Receptor 10 in kidney
CCR10 (IHC-grade) Chemokine Receptor 10 Antibody
The non-phospho-CCR10 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CCR10. It can be used to detect total CCR10 receptors in Western blots independent of phosphorylation. The CCR10 antibody...
£ 335.00 *
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Validation of the CC Chemokine Receptor 10 in transfected HEK293 cells
CCR10 (non-phospho) Chemokine Receptor 10 Antibody
The non-phospho-CCR10 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CCR10. It can be used to detect total CCR10 receptors in Western blots independent of phosphorylation. The CCR10 antibody...
£ 335.00 *
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Immunohistochemical identification of CC Chemokine Receptor 6 in pancreas
CCR6 (IHC-grade) Chemokine Receptor 6 Antibody
The non-phospho-CCR6 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CCR6. It can be used to detect total CCR6 receptors in Western blots independent of phosphorylation. The CCR6 antibody can...
£ 335.00 *
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Validation of the CC Chemokine Receptor 6 in transfected HEK293 cells
CCR6 (non-phospho) Chemokine Receptor 6 Antibody
The non-phospho-CCR6 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CCR6. It can be used to detect total CCR6 receptors in Western blots independent of phosphorylation. The CCR6 antibody can...
£ 335.00 *
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Validation of the Calcium-sensing Receptor in transfected HEK293 cells
CaS (non-phospho), Calcium-sensing Receptor...
The non-phospho-CaS Calcium-sensing Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human CaS. It can be used to detect total CaS receptors in Western blots independent of phosphorylation. The...
£ 335.00 *
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Immunohistochemical identification of Calcium-sensing Receptor in pancreas
CaS (IHC-grade), Calcium-sensing Receptor Antibody
The non-phospho-CaS Calcium-sensing Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human CaS. It can be used to detect total CaS receptors in Western blots independent of phosphorylation. The...
£ 335.00 *
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Immunohistochemical varification of complement C3a Receptor antibody in human spleen
C3a (IHC-grade), Complement C3a Receptor Antibody
The non-phospho-C3a receptor antibody is directed against the distal end of the carboxyl-terminal tail of human C3a. It can be used to detect total C3a receptors in Western blots independent of phosphorylation. The non-phospho-C3a...
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Validation of the Complement C3a Receptor 1 in transfected HEK293 cells
C3a (non-phospho), Complement C3a Receptor...
The non-phospho-C3a receptor antibody is directed against the distal end of the carboxyl-terminal tail of human C3a. It can be used to detect total C3a receptors in Western blots independent of phosphorylation. The non-phospho-C3a...
£ 335.00 *
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Validation of the IP Prostacyclin Receptor in transfected HEK293 cells
IP (non-phospho), IP Prostacyclin Receptor...
The non-phospho-IP Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human IP. It can be used to detect total IP receptors in Western blots independent of phosphorylation. The non-phospho-IP antibody...
£ 335.00 *
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Validation of the TP Tromboxane Receptor in transfected HEK293 cells
TP (non-phospho), TP Thromboxane Receptor Antibody
The non-phospho-TP Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human TP. It can be used to detect total TP receptors in Western blots independent of phosphorylation. The non-phospho-TP antibody...
£ 335.00 *
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Validation of the Formylpeptide Receptor 1 in transfected HEK293 cells
FPR1 (non-phospho), Formylpeptide Receptor 1...
The non-phospho-FPR1 Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human FPR1. It can be used to detect total FPR1 receptors in Western blots independent of phosphorylation. The non-phospho-FPR1...
£ 335.00 *
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Validation of the Oxytocin Receptor in transfected HEK293 cells
OT (non-phospho), Oxytocin Receptor Antibody
The non-phospho-OT Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human OT. It can be used to detect total OT receptors in Western blots independent of phosphorylation. The non-phospho-OT antibody...
£ 335.00 *
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Validation of the P2RY Purinoceptor 8 in transfected HEK293 cells
P2RY8 (non-phospho), P2RY Purinoceptor 8 Antibody
The non-phospho-P2RY8 Receptor Antibody is directed against the distal end of the carboxyl-terminal tail of human P2RY8. It can be used to detect total P2RY8 receptors in Western blots independent of phosphorylation. The...
£ 335.00 *
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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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