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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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Validation of the FFA2 in transfected HEK293 cells
FFA2 (non-phospho-FFA2 Antibody)
The non-phospho-FFA2 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human FFA2. It can be used to detect total FFA2 receptors in Western blots independent of phosphorylation. The non-phospho-FFA2...
$ 375.00 *
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Immunohistochemical varification of 5-Hydroxytryptamine Receptor 6 antibody in Medial Septum
5-HT6 (IHC-grade), 5-HT Receptor 6 Antibody
The 5-HT6 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human 5-Hydroxytryptamine Receptor 6 (5-HT6). It can be used to detect total 5-HT6 receptors in Western blots independent of...
$ 375.00 *
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Immunohistochemical identification of Dopamine Receptor 1 in striatum
D1 (IHC-grade), Dopamine Receptor 1 Antibody
The D1 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human D1. It can be used to detect total D1 receptors in Western blots independent of phosphorylation. The D1 antibody can also be used to...
$ 375.00 *
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Validation of the S1P5 Receptor in transfected HEK293 cells.
S1P5 (non-phospho), Sphingosine 1-Phosphate...
The non-phospho-S1P5 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P5. It can be used to detect total S1P5 receptors in Western blots independent of phosphorylation. The S1P5 antibody can...
$ 375.00 *
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Agonist-induced Serine338/Threonine342 phosphorylation of MCH1 Receptor.
pS338/pT342-MCH1 (phospho-Melanin-Concentrating...
Serine338/Threonine342 (S338/T342) is a major phosphorylation site of the MCH1 receptor. The pS338/pT342-MCH1 antibody detects phosphorylation in response to high-efficacy agonists. S338/T342 phosphorylation is a key regulator of MCH1...
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Agonist-induced Threonine348/Serine350 phosphorylation of MCH1 Receptor
pT348/pS350-MCH1 (phospho-Melanin-Concentrating...
Threonine348/Serine350 (T348/S350) is a major phosphorylation site of the MCH1 receptor. The pT348/pS350-MCH1 antibody detects phosphorylation in response to high-efficacy agonists. T348/S350 phosphorylation is a key regulator of MCH1...
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Agonist-induced Threonine335/Serine338 phosphorylation of MCH2 Receptor
pT335/pS338-MCH2 (phospho-Melanin-Concentrating...
Threonine335/Serine338 (T335/S338) is a major phosphorylation site of the MCH2 receptor. The pT335/pS338-MCH2 antibody detects phosphorylation in response to high-efficacy agonists. T335/S338 phosphorylation is a key regulator of MCH2...
$ 375.00 *
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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...
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Agonist-induced Serine355/Serine360 phosphorylation of the Atypical Chemokine Receptor 3/CXC Chemokine Receptor 7
pS355/pS360-ACKR3 (phospho-Atypical Chemokine...
Serine355/Serine360 (S355/S360) is major phosphorylation site of the Atypical Chemokine Receptor 3 (ACKR3, previously called CXCR7). The pS355/pS360-ACKR3 antibody detects phosphorylation in response to agonists. S355/S360...
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Validation of the SUCNR1 Receptor in transfected HEK293 cells
SUCNR1/GPR91 (non-phospho), Succinate Receptor...
The non-phospho-SUCNR1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human SUCNR1. It can be used to detect total SUCNR1 receptors in Western blots independent of phosphorylation. The SUCNR1...
$ 375.00 *
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Validation of the EP2 Receptor in transfected HEK293 cells
EP2 (non-phospho), EP2 Prostanoid Receptor...
The non-phospho-EP2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human EP2. It can be used to detect total EP2 receptors in Western blots independent of phosphorylation.The EP2 antibody can also...
$ 375.00 *
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Validation of the EP4 Receptor in transfected HEK293 cells.
EP4 (non-phospho), EP4 Prostanoid Receptor...
The non-phospho-EP4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human EP4. It can be used to detect total EP4 receptors in Western blots independent of phosphorylation.
$ 375.00 *
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Indentification of EP4 Receptor in mouse tissues
EP4 (GP-non-phospho), EP4 Prostanoid Receptor...
The non-phospho-EP4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human EP4. It can be used to detect total EP4 receptors in Western blots independent of phosphorylation.
$ 375.00 *
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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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Immunohistochemical identification of Tachykinin Receptor 1 in pancreatic carcinoma
NK1 (IHC-grade), Tachykinin Receptor 1 Receptor...
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...
$ 375.00 *
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27 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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