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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 CC Chemokine Receptor 5 in transfected HEK293 cells
CCR5 (GP-non-phospho) Chemokine Receptor 5...
The non-phospho-CCR5 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CCR5. It can be used to detect total CCR5 receptors in Western blots independent of phosphorylation. The CCR5 antibody can...
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Validation of the Melatonin Receptor 1 in transfected HEK293 cells
MT1 (non-phospho) Melatonin Receptor 1 Antibody
The non-phospho MT1 receptor antibody is directed against the distal end of the carboxyl-terminal tail human MT1 receptor. It can be used to detect total MT1 receptors in Western blots independent of phosphorylation. It can also be used...
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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...
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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...
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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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Immunohistochemical identification of Secretin Receptor in human cortex
SCTR (IHC-grade), Secretin Receptor Antibody
The non-phospho SCTR receptor antibody is directed against the distal end of the carboxyl-terminal tail human SCTR receptor. It can be used to detect total SCTR receptors in Western blots independent of phosphorylation. It can also be...
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Validation of the Secretin Receptor in transfected HEK293 cells
SCTR (non-phospho) Secretin Receptor Antibody
The non-phospho SCTR receptor antibody is directed against the distal end of the carboxyl-terminal tail human SCTR receptor. It can be used to detect total SCTR receptors in Western blots independent of phosphorylation. It can also be...
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Validation of the Smoothened Receptor in transfected HEK293 cells
SMO (non-phospho) Smoothened Receptor Antibody
The non-phospho SMO receptor antibody is directed against the distal end of the carboxyl-terminal tail human SMO receptor. It can be used to detect total SMO receptors in Western blots independent of phosphorylation. It can also be used...
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Immunohistochemical identification of Smoothened Receptor in cilia
SMO (IHC-grade), Smoothened Receptor Antibody
The non-phospho SMO receptor antibody is directed against the distal end of the carboxyl-terminal tail human SMO receptor. It can be used to detect total SMO receptors in Western blots independent of phosphorylation. It can also be used...
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Isolation and enrichment of the Smoothened Receptor from tissue lysates
SMO (GP-non-phospho) Smoothened Receptor...
The non-phospho SMO receptor antibody is directed against the distal end of the carboxyl-terminal tail human SMO receptor. It can be used to detect total SMO receptors in Western blots independent of phosphorylation. It can also be used...
CHF400.00 *
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Immunohistochemical identification of Smoothened Receptor in heart
SMO (GP-IHC-grade), Smoothened Receptor...
The non-phospho SMO receptor antibody is directed against the distal end of the carboxyl-terminal tail human SMO receptor. It can be used to detect total SMO receptors in Western blots independent of phosphorylation. It can also be used...
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Agonist-induced Serine473/Serine475 phosphorylation of the β1-Adrenoceptor
pS473/pS475-β1 (phospho-β1-Adrenoceptor Antibody)
Serine473/Serine475 (S473/S475) is a major phosphorylation site of the β1 adrenoceptor. The pS473/pS475-β1 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S473/S475...
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Immunohistochemical identification of the Formylpeptide Receptor 2 in striatum
FPR2 (IHC-grade), Formylpeptide Receptor 2...
The FPR2 antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human FPR2. It can be used to detect total FPR2 receptors in Western blots independent of phosphorylation. The FPR2 antibody can also be...
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Agonist-induced Threonine314/Threonine315 phosphorylation of GPR55
pT314/pT315-GPR55 (phospho-GPR55 Antibody)
Threonine314/Threonine315 (T314/T315) is major phosphorylation site of human GPR55 receptor. The pT314/pT315-GPR55 antibody detects phosphorylation in response to agonists. T314/T315) phosphorylation is likely to be involved in efficient...
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Agonist-induced Serine354/Serine359 phosphorylation of the Relaxin Receptor 4
pS354/pS359-RXFP4 (phospho-Relaxin Receptor 4...
Serine354/Serine359 (S354/S359) is major phosphorylation site of the Relaxin Receptor 4 (RXFP4). The pS354/pS359-RXFP4 antibody detects phosphorylation in response to agonists. S354/S359 phosphorylation is likely to be involved in...
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Agonist-induced Threonine419/Threonine421/Threonine422 phosphorylation of the Relaxin Receptor 3
pT419/pT421/pT422-RXFP3 (phospho-Relaxin...
Threonine419/Threonine421/Threonine422 (T419/T421/T422) is major phosphorylation site of the Relaxin Receptor 3 (RXFP3). The pT419/pT421/pT422-RXFP3 antibody detects phosphorylation in response to agonists. T419/T421/T422 phosphorylation...
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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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