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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 S1P1 Receptor in transfected HEK293 cells
S1P1 (GP-non-phospho), Sphingosine 1-Phosphate...
The non-phospho-S1P1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P1. It also detects S1P1 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
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NEW
Validation of the S1P1 Receptor in transfected HEK293 cells
S1P1 (non-phospho), Sphingosine 1-Phosphate...
The non-phospho-S1P1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P1. It also detects S1P1 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
CHF400.00 *
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NEW
Immunohistochemical identification of S1P1 Receptor in human spleen
S1P1 (IHC-grade), Sphingosine 1-Phosphate...
The non-phospho-S1P1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P1. It also detects S1P1 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
CHF400.00 *
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Validation of the Tachykinin Receptor 3 in transfected HEK293 cells
NK3 (non-phospho), Tachykinin Receptor 3 Antibody
The NK3 antibody is directed against the distal end of the carboxyl-terminal tail of human Tachykinin Receptor 3. It detects selectively the NK3 Tachykinin Receptor. It can be used to detect total NK3 receptors in Western blots...
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Validation of the Tachykinin Receptor 2 in transfected HEK293 cells
NK2 (non-phospho), Tachykinin Receptor 2 Antibody
The NK2 antibody is directed against the distal end of the carboxyl-terminal tail of human Tachykinin Receptor 2. It detects selectively the NK2 Tachykinin Receptor. It can be used to detect total NK2 receptors in Western blots...
CHF400.00 *
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Immunohistochemical identification of Tachykinin Receptor 2 in duodenum
NK2 (IHC-grade), Tachykinin Receptor 2 Antibody
The NK2 antibody is directed against the distal end of the carboxyl-terminal tail of human Tachykinin Receptor 2. It detects selectively the NK2 Tachykinin Receptor. It can be used to detect total NK2 receptors in Western blots...
CHF400.00 *
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Validation of the GPR139 Receptor in transfected HEK293 cells
GPR139 (non-phospho), G protein-coupled...
The non-phospho-GPR139 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR139. It can be used to detect total GPR139 receptors in Western blots independent of phosphorylation. The GPR139...
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Validation of the Neuropeptide FF Receptor 1 in transfected HEK293 cells
NPFF1 (non-phospho), Neuropeptide FF Receptor 1...
The NPFF1 antibody is directed against the distal end of the carboxyl-terminal tail of human NPFF1. It detects selectively the NPFF1. It can be used to detect total NPFF1 receptors in Western blots independent of phosphorylation. The...
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Validation of the S1P4 Receptor in transfected HEK293 cells
S1P4 (non-phospho), Sphingosine 1-Phosphate...
The non-phospho-S1P4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P4. It can be used to detect total S1P4 receptors in Western blots independent of phosphorylation. The S1P4 antibody can...
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Validation of the S1P2 Receptor in transfected HEK293 cells.
S1P2 (non-phospho), Sphingosine 1-Phosphate...
The non-phospho-S1P2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P2. It also detects S1P2 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
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Immunohistochemical varification of S1P2 Receptor antibody in human liver.
S1P2 (IHC-grade), Sphingosine 1-Phosphate...
The non-phospho-S1P2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human S1P2. It also detects S1P2 in cultured cells and tissue sections by immunohistochemistry. It can be used to detect total...
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Immunohistochemical identification of Glucagon-Like Peptide 1 Receptor in pancreas
GLP1 (IHC-grade), Glucagon-Like Peptide 1...
The GLP1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GLP1 Receptor. The GLP1 antibody can be used to isolate and enrich GLP1 receptors from cell and tissue lysates. It also detects GLP1 in...
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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...
CHF400.00 *
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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...
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Validation of the GPR146 Receptor in transfected HEK293 cells
GPR146 (non-phospho), G protein-coupled...
The non-phospho-GPR146 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR146. It can be used to detect total GPR146 receptors in Western blots independent of phosphorylation. The GPR146...
CHF400.00 *
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NEW
Validation of the GPR55 Receptor in transfected HEK293 cells
GPR55 (non-phospho), G protein-coupled...
The non-phospho-GPR55 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR55. It can be used to detect total GPR55 receptors in Western blots independent of phosphorylation. The GPR55 antibody...
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23 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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