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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 Galanin Receptor 2 in transfected HEK293 cells
GAL2 [UMB15] (RM-non-phospho-Galanin Receptor 2...
The non-phospho-GAL2 antibody is directed against the distal end of the carboxyl-terminal tail of human GAL2. It can be used to detect total GAL2 receptors in Western blots independent of phosphorylation. The GAL2 antibody can also be...
CHF495.00 *
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Rabbit Monoclonal
NEW
Validation of the Galanin Receptor 1 in transfected HEK293 cells.
GAL1 [UMB14] (RM-non-phospho-Galanin Receptor 1...
The non-phospho-GAL1 antibody is directed against the distal end of the carboxyl-terminal tail of human GAL1. It can be used to detect total GAL1 receptors in Western blots independent of phosphorylation. The GAL1 antibody can also be...
CHF495.00 *
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Rabbit Monoclonal
NEW
Validation of the Bradykinin Receptor 2 in transfected HEK293 cells.
B2 [UMB12] (RM-non-phospho-Bradykinin Receptor...
The non-phospho-B2 Bradykinin Receptor antibody is directed against the distal end of the carboxyl-terminal tail of human B2. It can be used to detect total B2 receptors in Western blots independent of phosphorylation. The B2 antibody...
CHF495.00 *
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NEW
Validation of the OR51E1 Receptor in transfected HEK293 cells.
OR51E1 (non-phospho), OR51E1 Antibody
The non-phospho-OR51E1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human OR51E1. It can be used to detect total OR51E1 receptors in Western blots independent of phosphorylation. The OR51E1...
CHF400.00 *
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NEW
Validation of the CysLT1 Receptor in transfected HEK293 cells
CysLT1 (non-phospho), Leukotriene Receptor...
The non-phospho-CysLT1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CysLT1. It can be used to detect total CysLT1 receptors in Western blots independent of phosphorylation. The CysLT1...
CHF400.00 *
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Rabbit Monoclonal
NEW
Validation of the mGLUR4 Receptor in transfected HEK293 cells
mGLUR4 [UMB18] (RM-non-phospho-Metabotropic...
The non-phospho-mGLUR4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human mGLUR4. It can be used to detect total mGLUR4 receptors in Western blots independent of phosphorylation. The mGLUR4...
CHF495.00 *
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NEW
Validation of the mGLUR5 Receptor in transfected HEK293 cells
mGLUR5 (non-phospho), Metabotropic Glutamate...
The non-phospho-mGLUR5 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human mGLUR5. It can be used to detect total mGLUR5 receptors in Western blots independent of phosphorylation. The mGLUR5...
CHF400.00 *
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NEW
Validation of the ADGRD1/GPR133 Receptor in transfected HEK293 cells
ADGRD1/GPR133 (GP-non-phospho), Adhesion...
The non-phospho-ADGRD1/GPR133 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human ADGRD1/GPR133. It can be used to detect total ADGRD1/GPR133 receptors in Western blots independent of...
CHF400.00 *
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NEW
Validation of the ADGRD1/GPR133 Receptor in transfected HEK293 cells
ADGRD1/GPR133 (non-phospho), Adhesion Receptor...
The non-phospho-ADGRD1/GPR133 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human ADGRD1/GPR133. It can be used to detect total ADGRD1/GPR133 receptors in Western blots independent of...
CHF400.00 *
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NEW
Validation of the GPR156 Receptor in transfected HEK293 cells.
GPR156 (non-phospho), G protein-coupled...
The non-phospho-GPR156 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR156. It can be used to detect total GPR156 receptors in Western blots independent of phosphorylation. The GPR156...
CHF400.00 *
Details
NEW
Validation of the GPR152 Receptor in transfected HEK293 cells.
GPR152 (non-phospho), G protein-coupled...
The non-phospho-GPR152 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR152. It can be used to detect total GPR152 receptors in Western blots independent of phosphorylation. The GPR152...
CHF400.00 *
Details
NEW
Validation of the GPR151 Receptor in transfected HEK293 cells
GPR151 (non-phospho), G protein-coupled...
The non-phospho-GPR151 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR151. It can be used to detect total GPR151 receptors in Western blots independent of phosphorylation. The GPR151...
CHF400.00 *
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Citations
Validation of the Parathyroid Hormone Receptor 1 in transfected HEK293 cells
PTH1 (GP-non-phospho-Parathyroid Hormone...
The PTH1 antibody is directed against the distal end of the carboxyl-terminal tail of human Parathyroid Hormone Receptor 1. It can be used to detect total PTH1 receptors in Western blots independent of phosphorylation. The PTH1 antibody...
CHF400.00 *
Details
NEW
Validation of the GPR161 Receptor in transfected HEK293 cells
GPR161 (GP-non-phospho), G protein-coupled...
The non-phospho-GPR161 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR161. It can be used to detect total GPR161 receptors in Western blots independent of phosphorylation. The GPR161...
CHF400.00 *
Details
NEW
Validation of the Lysophosphatidic Acid Receptor 1 in transfected HEK293 cells.
LPA1 (GP-non-phospho), Lysophosphatidic Acid...
The non-phospho-LPA1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human LPA1. It can be used to detect total LPA1 receptors in Western blots independent of phosphorylation. The LPA1 antibody can...
CHF400.00 *
Details
NEW
Validation of the Lysophosphatidic Acid Receptor 4 in transfected HEK293 cells.
LPA4 (non-phospho), Lysophosphatidic Acid...
The non-phospho-LPA4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human LPA4. It can be used to detect total LPA4 receptors in Western blots independent of phosphorylation. The LPA4 antibody can...
CHF400.00 *
Details
27 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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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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