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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 GPR119 Receptor in transfected HEK293 cells
GPR119 (non-phospho), G protein-coupled...
The non-phospho-GPR119 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR119. It can be used to detect total GPR119 receptors in Western blots independent of phosphorylation. The GPR119...
375.00 € *
NEW
Validation of the Angiotensin Receptor 2 in transfected HEK293 cells
AT2 (non-phospho-Angiotensin Receptor 2 Antibody)
The non-phospho-AT2 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human Angiotensin Receptor 2 (AT2). It can be used to detect total AT2 receptors in Western blots independent of phosphorylation....
375.00 € *
NEW
Validation of the CCR8 Receptor in transfected HEK293 cells
CCR8 (non-phospho), CCR8 Chemokine Receptor...
The non-phospho-CCR8 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CCR8. It can be used to detect total CCR8 receptors in Western blots independent of phosphorylation. The non-phospho-CCR8...
375.00 € *
NEW
Validation of the Formylpeptide Receptor 2 in transfected HEK293 cells
FPR2 (non-phospho), Formylpeptide Receptor 2...
The FPR2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Formylpeptide Receptor 2. It can be used to detect total FPR2 receptors in Western blots independent of phosphorylation. The FPR2...
375.00 € *
NEW
Validation of the GPR183 Receptor in transfected HEK293 cells
GPR183 (non-phospho), Oxysterol Receptor Antibody
The non-phospho-GPR183 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR183. It also detects GPR183 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect...
375.00 € *
NEW
Validation of the G Protein-coupled Receptor 17 in transfected HEK293 cells
GPR17 (GP-non-phospho), G Protein-coupled...
The non-phospho-GPR17 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human GPR17. It can be used to detect total GPR17 receptors in Western blots independent of phosphorylation. The...
375.00 € *
NEW
GPR183 (GP-non-phospho), Oxysterol Receptor Antibody, Guinea Pig
GPR183 (GP-non-phospho), Oxysterol Receptor...
The non-phospho-GPR183 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR183. It also detects GPR183 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect...
375.00 € *
NEW
Validation of the GPR82 Receptor in transfected HEK293 cells
GPR82 (non-phospho), G protein-coupled...
The non-phospho-GPR82 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR82. It can be used to detect total GPR82 receptors in Western blots independent of phosphorylation. The GPR82 antibody...
375.00 € *
NEW
Validation of the G protein-coupled receptor 32 in transfected HEK293 cells
GPR32 (non-phospho), G protein-coupled Receptor...
The non-phospho-GPR32 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR32. It can be used to detect total GPR32 receptors in Western blots independent of phosphorylation. The GPR32 antibody...
375.00 € *
NEW
Validation of the GPR27 Receptor in transfected HEK293 cells
GPR27 (non-phospho), G protein-coupled...
The non-phospho-GPR27 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR27. It can be used to detect total GPR27 receptors in Western blots independent of phosphorylation. The GPR27 antibody...
375.00 € *
NEW
Validation of the G Protein-coupled Receptor 17 in transfected HEK293 cells
GPR17 (non-phospho), G Protein-coupled Receptor...
The non-phospho-GPR17 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human GPR17. It can be used to detect total GPR17 receptors in Western blots independent of phosphorylation. The...
375.00 € *
NEW
Validation of the GPR12 Receptor in transfected HEK293 cells
GPR12 (non-phospho), G protein-coupled Receptor...
The non-phospho-GPR12 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR12. It can be used to detect total GPR12 receptors in Western blots independent of phosphorylation. The GPR12 antibody...
375.00 € *
NEW
Validation of the GPR6 Receptor in transfected HEK293 cells.
GPR6 (non-phospho), G protein-coupled Receptor...
The non-phospho-GPR6 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR6. It can be used to detect total GPR6 receptors in Western blots independent of phosphorylation. The GPR6 antibody can...
375.00 € *
NEW
Validation of the MRGPRX2 Receptor in transfected HEK293 cells
MRGPRX2 (GP-non-phospho), MRGPRX2 Mas-related...
The non-phospho-MRGPRX2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human MRGPRX2. It can be used to detect total MRGPRX2 receptors in Western blots independent of phosphorylation. The MRGPRX2...
375.00 € *
NEW
Immunohistochemical identification of MRGPRX2 Receptor in Pancreas
MRGPRX2 (GP-IHC-grade), MRGPRX2 Mas-related...
The non-phospho-MRGPRX2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human MRGPRX2. It can be used to detect total MRGPRX2 receptors in Western blots independent of phosphorylation. The MRGPRX2...
375.00 € *
NEW
Immunohistochemical identification of MRGPRX2 Receptor in small intestine
MRGPRX2 (IHC-grade), MRGPRX2 Mas-related...
The non-phospho-MRGPRX2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human MRGPRX2. It can be used to detect total MRGPRX2 receptors in Western blots independent of phosphorylation. The MRGPRX2...
375.00 € *
17 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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