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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 Serine358/Serine360 phosphorylation of the GPR52 Receptor
pS358/pS360-GPR52 (phospho-GPR52 Antibody)
Serine358/Serine360 (S358/S360) is major phosphorylation site of the GPR52 Receptor (GPR52). The pS358/pS360-GPR52 antibody detects phosphorylation in response to agonists. S358/S360 phosphorylation is likely to be involved in efficient...
$ 375.00 *
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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...
$ 495.00 *
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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....
$ 495.00 *
Details
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...
$ 495.00 *
Details
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...
$ 495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Western blot analysis of Somatostatin Receptor 1 in membrane preparations from cells of AtT-20 and BON-1 cell lines.
SST1 [UMB7] (RM-non-phospho-Somatostatin...
The SST1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 1. It can be used to detect total SST1 receptors in Western blots independent of phosphorylation. The SST1...
$ 495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Immunohistochemical identification of Somatostatin Receptor 1 in human pituitary.
SST1 [UMB7] (RM-IHC-grade), Somatostatin...
The SST1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 1. It can be used to detect total SST1 receptors in Western blots independent of phosphorylation. The SST1...
$ 495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Immunohistochemical identification of Endotheline Receptor A in mouse heart.
ETA [UMB8] (RM-IHC-grade), Endothelin Receptor...
The ETA receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human endothelin receptor A. It can be used to detect ETA receptors in Western blots in a phosphorylation-sensitive manner...
$ 495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Indentification of the Endothelin Receptor A in mouse tissues.
ETA [UMB8] (RM-non-phospho-Endothelin Receptor...
The ETA receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human endothelin receptor A. It can be used to detect ETA receptors in Western blots in a phosphorylation-sensitive manner...
$ 495.00 *
Details
NEW
Validation of the S1P1 Receptor in transfected HEK293 cells
S1P1 (GP-non-phospho), Sphingosine 1-Phosphate...
The non-phospho-S1P1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P1. It also detects S1P1 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
$ 375.00 *
Details
NEW
Immunohistochemical identification of Threonine344/Serine347 phosphorylation of NK1 Receptor in striatum
pT344/pS347-NK1 (IHC-grade phospho-Tachykinin...
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...
$ 500.00 *
Details
NEW
Validation of the GPR52 Receptor in transfected HEK293 cells
GPR52 (non-phospho), G protein-coupled...
The non-phospho-GPR52 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR52. It can be used to detect total GPR52 receptors in Western blots independent of phosphorylation. The GPR52 antibody...
$ 375.00 *
Details
NEW
Immunohistochemical identification of S1P1 Receptor in human spleen
S1P1 (IHC-grade), Sphingosine 1-Phosphate...
The non-phospho-S1P1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P1. It also detects S1P1 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
$ 375.00 *
Details
Citations
KO-Validated
SST5 (IHC-grade), Somatostatin Receptor 5 Antibody
SST5 (IHC-grade), Somatostatin Receptor 5 Antibody
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...
$ 375.00 *
Details
Citations
KO-Validated
SST5 (non-phospho), Somatostatin Receptor 5 Antibody
SST5 (non-phospho), Somatostatin Receptor 5...
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...
$ 375.00 *
Details
Citations
SST3 (IHC-grade), Somatostatin Receptor 3 Antibody
SST3 (IHC-grade), Somatostatin Receptor 3 Antibody
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...
$ 375.00 *
Details
25 From 38

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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