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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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Rabbit Monoclonal
NEW
Validation of the Corticotropin-Releasing Factor Receptor 1 in transfected HEK293 cells
CRF1 [UMB19]...
The non-phospho-CRF1 antibody is directed against the distal end 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...
CHF495.00 *
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NEW
Validation of the GPBA Receptor in transfected HEK293 cells.
GPBA (non-phospho), Bile Acid Receptor Antibody
The non-phospho-GPBA receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPBA. It can be used to detect total GPBA receptors in Western blots independent of phosphorylation. The GPBA antibody can...
CHF400.00 *
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Rabbit Monoclonal
NEW
Validation of the Calcitonin Receptor in transfected HEK293 cells
CT [UMB25] (RM-non-phospho-Calcitonin Receptor...
The non-phospho-CT antibody is directed against the distal end of the carboxyl-terminal tail of human CT. It can be used to detect total CT receptors in Western blots independent of phosphorylation. The CT antibody can also be used to...
CHF495.00 *
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NEW
Validation of the GPR149 Receptor in transfected HEK293 cells
GPR149 (non-phospho), G protein-coupled...
The non-phospho-GPR149 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR149. It can be used to detect total GPR149 receptors in Western blots independent of phosphorylation. The GPR149...
CHF400.00 *
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Rabbit Monoclonal
NEW
Immunohistochemical identification of Melanin-Concentrating Hormone Receptor 1 in neuronal cilia
MCH1 [UMB20]...
The non-phospho-MCH1 antibody is directed against the distal end of the carboxyl-terminal tail of human MCH1. It can be used to detect total MCH1 receptors in Western blots independent of phosphorylation. The MCH1 antibody can also be...
CHF495.00 *
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Rabbit Monoclonal
NEW
Validation of the Melanin-Concentrating Hormone Receptor 1 in transfected HEK293 cells.
MCH1 [UMB20]...
The non-phospho-MCH1 antibody is directed against the distal end of the carboxyl-terminal tail of human MCH1. It can be used to detect total MCH1 receptors in Western blots independent of phosphorylation. The MCH1 antibody can also be...
CHF495.00 *
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NEW
Validation of the Lysophosphatidic Acid Receptor 5 in transfected HEK293 cells.
LPA5 (non-phospho), Lysophosphatidic Acid...
The non-phospho-LPA5 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human LPA5. It can be used to detect total LPA5 receptors in Western blots independent of phosphorylation. The LPA5 antibody can...
CHF400.00 *
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NEW
Validation of the FFA3 in transfected HEK293 cells.
FFA3 (non-phospho-FFA3 Antibody)
The non-phospho-FFA3 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human FFA3. It can be used to detect total FFA3 receptors in Western blots independent of phosphorylation. The non-phospho-FFA3...
CHF400.00 *
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NEW
Validation of the mouse FFA3 in transfected HEK293 cells.
mFFA3 (non-phospho-Mouse FFA3 Antibody)
The non-phospho-FFA3 receptor antibody is directed against the distal part of the carboxyl-terminal tail of mouse FFA3. It can be used to detect total FFA3 receptors in Western blots independent of phosphorylation. The non-phospho-FFA3...
CHF400.00 *
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NEW
Validation of the mouse GPR62 Receptor in transfected HEK293 cells.
mGPR62 (non-phospho), Mouse G protein-coupled...
The non-phospho-mGPR62 receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse GPR62. It can be used to detect total GPR62 receptors in Western blots independent of phosphorylation. The GPR62 antibody...
CHF400.00 *
Details
NEW
Validation of the GPR162 Receptor in transfected HEK293 cells.
GPR162 (non-phospho), G protein-coupled...
The non-phospho-GPR162 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR162. It can be used to detect total GPR162 receptors in Western blots independent of phosphorylation. The GPR162...
CHF400.00 *
Details
NEW
Validation of the GPR153 Receptor in transfected HEK293 cells.
GPR153 (non-phospho), G protein-coupled...
The non-phospho-GPR153 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR153. It can be used to detect total GPR153 receptors in Western blots independent of phosphorylation. The GPR153...
CHF400.00 *
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Rabbit Monoclonal
NEW
Validation of the GABAB2 Receptor in transfected HEK293 cells.
GABAB2 [UMB24] (RM-non-phospho-GABAB Receptor 2...
The non-phospho-GABAB2 antibody is directed against the distal end of the carboxyl-terminal tail of human GABAB2 . It can be used to detect total GABAB2 receptors in Western blots independent of phosphorylation. The GABAB2 antibody can...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Validation of the Bombesin Receptor 2 in transfected HEK293 cells.
BB2 [UMB17] (RM-non-phospho-Bombesin Receptor 2...
The non-phospho-BB2 antibody is directed against the distal end of the carboxyl-terminal tail of human BB2. It can be used to detect total BB2 receptors in Western blots independent of phosphorylation. The BB2 antibody can also be used...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Validation of the Vasopressin Receptor 1A in transfected HEK293 cells
V1A [UMB21] (RM-non-phospho-Vasopressin...
The non-phospho-V1A antibody is directed against the distal end of the carboxyl-terminal tail of human V1A. It can be used to detect total V1A receptors in Western blots independent of phosphorylation. The V1A antibody can also be used...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Validation of the Vasopressin Receptor 2 in transfected HEK293 cells.
V2 [UMB16] (RM-non-phospho-Vasopressin Receptor...
The non-phospho-V2 antibody is directed against the distal end of the carboxyl-terminal tail of human V2. It can be used to detect total V2 receptors in Western blots independent of phosphorylation. The V2 antibody can also be used to...
CHF495.00 *
Details
26 From 42

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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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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