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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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CX3CR1 (non-phospho), CX3C Chemokine Receptor 1 Antibody
CX3CR1 (non-phospho), CX3C Chemokine Receptor 1...
The non-phospho-CX3CR1 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human CX3CR1. It can be used to detect total CX3CR1 receptors in Western blots independent of phosphorylation.
375.00 € *
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CXCR3 (non-phospho), CXCR3 Chemokine Receptor Antibody
CXCR3 (non-phospho), CXCR3 Chemokine Receptor...
The non-phospho-CXCR3 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CXCR3. It can be used to detect total CXCR3 receptors in Western blots independent of phosphorylation.
375.00 € *
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KO-Validated
Immunohistochemical identification of µ-Opioid Receptor in Striatum
MOP (GP-IHC-grade), µ-Opioid Receptor Antibody,...
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...
375.00 € *
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KO-Validated
Validation of the µ-Opioid Receptor in transfected HEK293 cells
MOP (GP-non-phospho), µ-Opioid Receptor...
The non-phospho-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. It can be...
375.00 € *
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Immunohistochemical identification of Somatostatin Receptor 2 in human neuroendocrine tumor tissue
SST2 (GP-IHC-grade), Somatostatin Receptor 2...
The SST2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 2. It detects selectively the canonical form of SST2 (also referred to as SST2A) and not the putative splice...
375.00 € *
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KO-Validated
Western blot analysis of Somatostatin Receptor 2 in mouse tissues in vivo
SST2 (GP-non-phospho), Somatostatin Receptor 2...
The GP-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...
375.00 € *
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Immunohistochemical identification of Corticotropin-Releasing Factor Receptor 1 in anterior pituitary
CRF1 (IHC-grade), Corticotropin-Releasing...
The CRF1 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human CRF1. It can be used to detect total CRF1 receptors in Western blots independent of phosphorylation. The CRF1 antibody can also be used...
375.00 € *
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Citations
Validation of the Neurotensin Receptor 1 in transfected HEK293 cells
NTS1 (non-phospho), Neurotensin Receptor 1...
The NTS1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Neurotensin Receptor 1. It can be used to detect total NTS1 receptors in Western blots independent of phosphorylation. The NTS1 antibody...
375.00 € *
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Immunohistochemical identification of CC Chemokine Receptor 7 in human spleen
CCR7 (IHC-grade), CC Chemokine Receptor 7 Antibody
The CCR7 receptor antibody is directed against the distal end of the carboxyl-terminal tail human CCR7. It can be used to detect total CCR7 receptors in Western blots independent of phosphorylation. It can also be used to isolate and...
375.00 € *
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Validation of the CC Chemokine Receptor 7 in transfected HEK293 cells
CCR7 (non-phospho), CC Chemokine Receptor 7...
The CCR7 receptor antibody is directed against the distal end of the carboxyl-terminal tail human CCR7. It can be used to detect total CCR7 receptors in Western blots independent of phosphorylation. It can also be used to isolate and...
375.00 € *
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CXCR4 (GP-non-phospho), CXC Chemokine Receptor 4 Antibody, Guinea Pig
CXCR4 (GP-non-phospho), CXC Chemokine Receptor...
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. It...
375.00 € *
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Immunohistochemical identification of GPR35 Receptor in human colon
GPR35 (IHC-grade), GPR35 Receptor Antibody
The GPR35 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human GPR35. It can be used to detect total GPR35 receptors in Western blots independent of phosphorylation. The GPR35 antibody can also be...
375.00 € *
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NEW
Detection of non-phosphorylated human GPR35 Receptor
GPR35 (non-phospho), G Protein-coupled Receptor...
The non-phospho-GPR35 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human GPR35. It can be used to detect total GPR35 receptors in Western blots independent of phosphorylation. The...
375.00 € *
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Immunohistochemical identification of Growth Hormone-Releasing Hormone Receptor in breast carcinoma.
GHRHR (IHC-grade), GHRH Receptor Antibody
The GHRH receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Growth Hormone-Releasing Hormone Receptor. It detects the canonical form of GHRHR as well as the amino-terminal splice variant SV1. It...
375.00 € *
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Citations
Immunohistochemical identification of Endotheline Receptor A in mouse heart.
ETA (IHC-grade), Endothelin Receptor A Antibody
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...
375.00 € *
Details
Citations
Immunohistochemical identification of Somatostatin Receptor 1 in human pituitary.
SST1 (IHC-grade), Somatostatin Receptor 1 Antibody
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...
375.00 € *
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19 From 30

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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