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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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NEW
Validation of the Atypical Chemokine Receptor 3/CXC Chemokine Receptor 7 in transfected HEK293 cells
ACKR3 (non-phos, N-Term), Atypical Chemokine...
The non-phospho-ACKR3 receptor antibody is directed against the amino-terminal tail of mouse, rat and human ACKR3/CXCR7. It can be used to detect total ACKR3 receptors in Western blots independent of phosphorylation. The...
CHF400.00 *
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SAMPLE PACK
Agonist-induced Serine355/Serine360 phosphorylation of the Atypical Chemokine Receptor 3/CXC Chemokine Receptor 7
ACKR3 Sample Pack (phospho- and...
ACKR3 Sample Pack consisting of all four available phospho- and non-phospho-Atypical Chemokine Receptor 3 Antibodies 4 x 20 µL trial size each. Specifically, this sample pack contains the following antibodies pS350/pT352-ACKR3...
CHF300.00 *
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Citations
Immunohistochemical identification of Bombesin Receptor 2/Gastrin-Relasing Peptide Receptor (BB2/GRPR) in human breast carcinoma.
BB2 (IHC-grade), Bombesin Receptor...
The BB2/GRPR receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Bombesin Receptor 2 (previously called Gastrin-Releasing Peptide Receptor). It can be used to detect total BB2 receptors in Western...
CHF400.00 *
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Citations
Immunohistochemical identification of Parathyroid Hormone Receptor 1 in human kidney.
PTH1 (IHC-grade), Parathyroid Hormone Receptor...
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 *
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Citations
Immunohistochemical identification of PACAP Receptor 1 in human neuroendocrine tumor
PAC1 (IHC-grade), PACAP Receptor 1 Antibody
The PAC1 antibody is directed against the distal end of the carboxyl-terminal tail of human PACAP Receptor 1. It can be used to detect total PAC1 receptors in Western blots independent of phosphorylation. The PAC1 antibody can also be...
CHF400.00 *
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Immunohistochemical identification of VIP Receptor 1 in small intestine.
VPAC1 (IHC-grade), VIP Receptor 1 Antibody
The VPAC1 antibody is directed against the distal end of the carboxyl-terminal tail of human VIP Receptor 1. It can be used to detect total VPAC1 receptors in Western blots independent of phosphorylation. The VPAC1 antibody can also be...
CHF400.00 *
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KO-Validated
Immunohistochemical identification of VIP Receptor 2 in small intestine.
VPAC2 (IHC-grade), VIP Receptor 2 Antibody
The VPAC2 antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human VIP receptor 2. It can be used to detect total VPAC2 receptors in Western blots independent of phosphorylation. The VPAC2...
CHF400.00 *
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Immunohistochemical identification of Cholecystokinin Receptor 1 in gastric mucosa.
CCK1 (IHC-grade), Cholecystokinin Receptor 1...
The CCK1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Cholecystokinin Receptor 1 (previously called CCKA). It can be used to detect total CCK1 receptors in Western blots independent of...
CHF400.00 *
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Citations
Immunohistochemical identification of PACAP Receptor 1 in mouse spinal cord dorsal horn.
mPAC1 (IHC-grade), PACAP Receptor 1 Antibody...
The mouse PAC1 antibody is directed against the distal end of the carboxyl-terminal tail of mouse and rat PACAP receptor 1. It can be used to detect total PAC1 receptors in Western blots independent of phosphorylation. The mouse PAC1...
CHF400.00 *
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NEW
KO-Validated
Immunohistochemical Identification of Agonist-induced Serine375 phosphorylation of the µ-Opioid Receptor in mouse spinal cord
pS375-MOP (IHC-grade phospho-µ-Opioid Receptor...
Serine375 (S375) is the primary phosphorylation site in a hierarchical phosphorylation cascade. The pS375-MOP antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S375...
CHF600.00 *
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NEW
KO-Validated
Immunohistochemical Identification of Agonist-induced Threonine376 phosphorylation of the µ-Opioid Receptor in mouse spinal cord
pT376-MOP (IHC-grade phospho-µ-Opioid Receptor...
Threonine376 (T376) is a major phosphorylation site of the µ-opioid receptor (MOP). The pT376-MOP antibody detects phosphorylation in response to high-efficacy agonists but to low-efficacy agonists or after PKC activation. T376...
CHF600.00 *
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NEW
KO-Validated
Immunohistochemical Identification of Agonist-induced Threonine379 phosphorylation of the µ-Opioid Receptor in mouse spinal cord
pT379-MOP (IHC-grade phospho-µ-Opioid Receptor...
Threonine379 (T379) is a major phosphorylation site of the µ-opioid receptor (MOP). The pT379-MOP antibody detects phosphorylation in response to high-efficacy agonists but to low-efficacy agonists or after PKC activation. T379...
CHF600.00 *
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Citations
KO-Validated
Immunohistochemical identification of Bradykinin Receptor 2 in pancreatic islets
B2 (IHC-grade), Bradykinin Receptor 2 Antibody
The B2 receptor antibody is directed against the distal part 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 can also be used to...
CHF400.00 *
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NEW
Immunohistochemical identification of FFA4 Receptor in human spleen
FFA4 (IHC-grade), FFA4 Receptor Antibody
The FFA4 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human FFA4. It can be used to detect total FFA4 receptors in Western blots independent of phosphorylation. The FFA4 antibody can also be used...
CHF400.00 *
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NEW
Immunohistochemical identification of APLN Receptor in human pancreas
APLNR (IHC-grade), Apelin Receptor Antibody
The non-phospho-APLNR antibody is directed against the distal end of the carboxyl-terminal tail of human apelin receptor. It also detects APLNR in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
CHF400.00 *
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NEW
Validation of the GPR15 Receptor in transfected HEK293 cells
GPR15 (non-phospho), G protein-coupled Receptor...
The non-phospho-GPR15 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR15. It can be used to detect total GPR15 receptors in Western blots independent of phosphorylation. The GPR15 antibody...
CHF400.00 *
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39 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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