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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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NEW
Agonist-induced Serine434/Serine437 phosphorylation of CRF1 Receptor
pS434/pS437-CRF1...
Serine434/Serine441 (S437/S441) is a major phosphorylation site of the CRF1 receptor. The pS434/pS437-CRF1 antibody detects phosphorylation in response to high-efficacy agonists. S434/S437 phosphorylation is a key regulator of CRF1...
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Validation of the Bombesin Receptor 3 in transfected HEK293 cells.
BB3 (non-phospho), Bombesin Receptor 3 Antibody
The BB3 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Bombesin Receptor 3. It can be used to detect BB3 in formalin-fixed, paraffin-embedded tissue sections by immunohistochemistry. It can be...
CHF400.00 *
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Citations
Validation of the Bombesin Receptor 2 in transfected HEK293 cells
BB2 (non-phospho), Bombesin Receptor 2 Antibody
The BB2/GRPR receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Bombesin Receptor 2 (previously called Gastrin-Releasing Peptide Receptor). It can be used to detect total BB2 receptors in Western...
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NEW
Agonist-induced Threonine340 phosphorylation of GAL1 Receptor.
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...
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NEW
Agonist-induced Threonine329/Serine331 phosphorylation of GAL2 Receptor
pT329/pS331-GAL2 (phospho-Galanin Receptor 2...
Threonine329/Serine331 (T329/S331) is a major phosphorylation site of the GAL2 receptor. The pT329/pS331-GAL2 antibody detects phosphorylation in response to high-efficacy agonists. T329/S331 phosphorylation is a key regulator of GAL2...
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NEW
Agonist-induced Serine331/Serine333 phosphorylation of GAL2 Receptor.
pS331/pS333-GAL2 (phospho-Galanin Receptor 2...
Serine331/Serine333 (S331/S333) is a major phosphorylation site of the GAL2 receptor. The pS331/pS333-GAL2 antibody detects phosphorylation in response to high-efficacy agonists. S331/S333 phosphorylation is a key regulator of GAL2...
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NEW
Agonist-induced Serine339/Serine340 phosphorylation of GAL2 Receptor
pS339/pS340-GAL2 (phospho-Galanin Receptor 2...
Serine339/Serine340 (S339/S340) is a major phosphorylation site of the GAL2 receptor. The pS339/pS340-GAL2 antibody detects phosphorylation in response to high-efficacy agonists. S339/S340 phosphorylation is a key regulator of GAL2...
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Rabbit Monoclonal
KO-Validated
NEW
Immunohistochemical identification of Somatostatin Receptor 2 in human neuroendocrine tumor tissue.
SST2 [UMB11] (RM-IHC-grade), Somatostatin...
The SST2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human Somatostatin Receptor 2. It detects selectively the canonical form of SST2 (also referred to as SST2A) and not the...
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Rabbit Monoclonal
KO-Validated
NEW
Western blot analysis of Somatostatin Receptor 2 in mouse brain in vivo.
SST2 [UMB11] (RM-non-phospho), Somatostatin...
The non-phospho-SST2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human SST2. It detects selectively the canonical form of SST2 (also referred to as SST2A) and not the putative...
CHF495.00 *
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Rabbit Monoclonal
KO-Validated
NEW
Immunohistochemical identification of CXC Chemokine Receptor 4 in human endometrial carcinoma.
CXCR4 [UMB22] (RM-IHC-grade), CXC Chemokine...
The CXCR4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human CXCR4. It can be used to detect CXCR4 receptors in Western blots in a phosphorylation-sensitive manner. After agonist...
CHF495.00 *
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Rabbit Monoclonal
KO-Validated
NEW
Validation of the CXC Chemokine Receptor 4 in transfected HEK293 cells.
CXCR4 [UMB22] (RM-non-phospho), CXC Chemokine...
The non-phospho-CXCR4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human CXCR4. It can be used to detect CXCR4 receptors in Western blots in a phosphorylation-sensitive manner....
CHF495.00 *
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Rabbit Monoclonal
KO-Validated
NEW
Immunohistochemical identification of Somatostatin Receptor 5 in human pancreatic islets
SST5 [UMB44] (RM-IHC-grade), Somatostatin...
The SST5 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 5. In can be used to detect total SST5 receptors in Western blots independent of phosphorylation. The SST5...
CHF495.00 *
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Rabbit Monoclonal
KO-Validated
NEW
Validation of the Somatostatin Receptor 5 in transfected HEK293 cells.
SST5 [UMB44] (RM-non-phospho), Somatostatin...
The non-phospho-SST5 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human SST5. In can be used to detect total SST5 receptors in Western blots independent of phosphorylation. The non-phospho-SST5...
CHF495.00 *
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Rabbit Monoclonal
KO-Validated
NEW
Immunohistochemical identification of µ-Opioid Receptor in caudate putamen.
MOP [UMB3] (RM-IHC-grade), µ-Opioid Receptor...
The µ-Opioid Receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human MOP. It detects selectively the canonical form of MOP and none of the putative splice variants. In can be used to...
CHF495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Immunohistochemical identification of Somatostatin Receptor 3 in human growth-hormone-producing pituitary adenoma tissue.
SST3 [UMB5] (RM-IHC-grade), Somatostatin...
The SST3 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 3. In can be used to detect total SST3 receptors in Western blots independent of phosphorylation. The SST3...
CHF495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Validation of the Somatostatin Receptor 3 in transfected HEK293 cells.
SST3 [UMB5] (RM-non-phospho), Somatostatin...
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...
CHF495.00 *
Details
29 From 42

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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