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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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Agonist-induced Serine326 phosphorylation of the Cannabinoid Receptor 2
pS326-CB2 (phospho-Cannabinoid Receptor 2...
Serine326 (S326) is major phosphorylation site of the Cannabinoid Receptor 2 (CB2). The pS326-CB2 antibody detects phosphorylation in response to agonists. S326 phosphorylation is likely to be involved in efficient ligand sequestration...
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Agonist-induced Threonine338/Threonine340 phosphorylation of the Cannabinoid Receptor 2
pT338/pT340-CB2 (phospho-Cannabinoid Receptor 2...
Threonine338/Threonine340 (T338/T340) is major phosphorylation site of the Cannabinoid Receptor 2 (CB2). The pT338/pT340-CB2 antibody detects phosphorylation in response to agonists. T338/T340 phosphorylation is likely to be involved in...
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Agonist-induced Serine425 phosphorylation of the Cannabinoid Receptor 1
pS425-CB1 (phospho-Cannabinoid Receptor 1...
Serine425 (S425) is major phosphorylation site of the Cannabinoid Receptor 1 (CB1). The pS425-CB1 antibody detects phosphorylation in response to agonists. S425 phosphorylation is likely to be involved in efficient ligand sequestration...
$ 375.00 *
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Agonist-induced Serine429 phosphorylation of the Cannabinoid Receptor 1
pS429-CB1 (phospho-Cannabinoid Receptor 1...
Serine429 (S429) is major phosphorylation site of the Cannabinoid Receptor 1 (CB1). The pS429-CB1 antibody detects phosphorylation in response to agonists. S429 phosphorylation is likely to be involved in efficient ligand sequestration...
$ 375.00 *
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Agonist-induced Serine441 phosphorylation of the Cannabinoid Receptor 1
pS441-CB1 (phospho-Cannabinoid Receptor 1...
Serine441 (S441) is major phosphorylation site of the Cannabinoid Receptor 1 (CB1). The pS441-CB1 antibody detects phosphorylation in response to agonists. S441 phosphorylation is likely to be involved in efficient ligand sequestration...
$ 375.00 *
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pS335/pS336-CB2 (phospho-Cannabinoid Receptor 2 Antibody)
pS335/pS336-CB2 (phospho-Cannabinoid Receptor 2...
Serine335/Serine336 (S335/S336) is major phosphorylation site of the Cannabinoid Receptor 2 (CB2). The pS335/pS336-CB2 antibody detects phosphorylation in response to agonists. S335/S336 phosphorylation is likely to be involved in...
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Agonist-induced Serine422/Serine425 phosphorylation of the Calcitonin Recepto
pS422/pS425-CT (phospho-Calcitonin Receptor...
Serine422/Serine425 (S422/S425) is a major phosphorylation site of the Calcitonin receptor. The pS422/pS425-CT antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S422/S425...
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Agonist-induced Serine366/Threonine369 phosphorylation of the Bradykinin Receptor 2
pS366/pT369-B2 (phospho-Bradykinin Receptor 2...
Serine366/Threonine369 (S366/T369) is major phosphorylation site of the Bradykinin Receptor 2 (B2). The pS366/pT369-B2 antibody detects phosphorylation in response to agonists. S366/T369 phosphorylation is likely to be involved in...
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Agonist-induced Threonine372/Serine373 phosphorylation of the Bradykinin Receptor 2
pT372/pS373-B2 (phospho-Bradykinin Receptor 2...
Threonine372/Serine373 (T372/S373) is major phosphorylation site of the Bradykinin Receptor 2 (B2). The pT372/pS373-B2 antibody detects phosphorylation in response to agonists. T372/S373 phosphorylation is likely to be involved in...
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Agonist-induced Serine363/Threonine364 phosphorylation of the Bombesin Receptor 2
pS363/pT364-BB2 (phospho-Bombesin Receptor 2...
Serine363/Threonine364 (S363/T364) is major phosphorylation site of the Bombesin Receptor 2 (BB2). The pS363/pT364-BB2 antibody detects phosphorylation in response to agonists. S363/T364 phosphorylation is likely to be involved in...
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Agonist-induced Threonine359/Serine360 phosphorylation of the Bombesin Receptor 2
pT359/pS360-BB2 (phospho-Bombesin Receptor 2...
Threonine359/Serine360 (T359/S360) is major phosphorylation site of the Bombesin Receptor 2 (BB2). The pT359/pS360-BB2 antibody detects phosphorylation in response to agonists. T359/S360 phosphorylation is likely to be involved in...
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Agonist-induced Threonine360/Serine361 phosphorylation of the Bombesin Receptor 3
pT360/pS361-BB3 (phospho-Bombesin Receptor 3...
Threonine360/Serine361 (T360/S361) is major phosphorylation site of the Bombesin Receptor 3 (BB3). The pT360/pS361-BB3 antibody detects phosphorylation in response to agonists. T360/S361 phosphorylation is likely to be involved in...
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Agonist-induced Threonine363/Threonine364 phosphorylation of the Bombesin Receptor 3
pT363/pT364-BB3 (phospho-Bombesin Receptor 3...
Threonine363/Threonine360 (T363/T364) is major phosphorylation site of the Bombesin Receptor 3 (BB3). The pT363/pT364-BB3 antibody detects phosphorylation in response to agonists. T363/T364 phosphorylation is likely to be involved in...
$ 375.00 *
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Agonist-induced Threonine370 phosphorylation of the Bombesin Receptor 3
pT370-BB3 (phospho-Bombesin Receptor 3 Antibody)
Threonine370 (T370) is major phosphorylation site of the Bombesin Receptor 3 (BB3). The pT370-BB3 antibody detects phosphorylation in response to agonists. T370 phosphorylation is likely to be involved in efficient ligand sequestration...
$ 375.00 *
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Agonist-induced Serine347/Serine348 phosphorylation of the Apelin Receptor
pS347/pS348-APLNR (phospho-Apelin Receptor...
Serine347/Serine348 (S347/S348) is major phosphorylation site of the Apelin Receptor (APLNR). The pS347/pS348-APLNR antibody detects phosphorylation in response to agonists. S347/S348 phosphorylation is likely to be involved in efficient...
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Agonist-induced Serine331/Threonine332 phosphorylation of the Angiotensin Receptor 1
pS331/pT332-AT1 (phospho-Angiotensin Receptor 1...
Serine331/Threonine332 (S331/T332) is major phosphorylation site of the Angiotensin Receptor 1 (AT1). The pS331/pT332-AT1 antibody detects phosphorylation in response to agonists. S331/T332 phosphorylation is likely to be involved in...
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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.

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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