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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 Threonine442/Serine443 phosphorylation of GIPR.
pT442/pS443-GIPR (phospho-Gastric Inhibitory...
Threonine442/Serine443 (T442/S443) is major phosphorylation site of human GIP receptor. The pT442/pS443-GIPR antibody detects phosphorylation in response to agonists. T442/S443 phosphorylation is likely to be involved in efficient ligand...
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Agonist-induced Serine317/Threonine318 phosphorylation of the Dopamine Receptor 2.
pS317/pT318-D2 (phospho-Dopamine Receptor 2...
Serine317/threonine318 (S317/T318) is a major phosphorylation site of the D2 dopamine receptor. The pS317/pT318-D2 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S317/T318...
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Agonist-induced Serine372/Serine373 phosphorylation of the Dopamine Receptor 1
pS372/pS373-D1 (phospho-Dopamine Receptor 1...
Serine372/Serine373 (S372/S373) is a major phosphorylation site of the D1 receptor. The pS372/pS373-D1 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S372/S373...
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Agonist-induced Threonine354 phosphorylation of the Dopamine Receptor 1
pT354-D1 (phospho-Dopamine Receptor 1 Antibody)
Threonine354 (T354) is a major phosphorylation site of the D1 receptor. The pT354-D1 antibody detects phosphorylation in response to high-efficacy agonists but not after PKC activation. T354 phosphorylation is a key regulator of D1...
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Agonist-induced Serine327/Serine329 phosphorylation of the Chemokine Receptor CX3CR1
pS327/pS329-CX3CR1 (phospho-CX3CR1 Chemokine...
Serine327/Serine329 (S327/S329) is a major phosphorylation site of the CX3CR1 receptor. The pS327/pS329-CX3CR1 antibody detects phosphorylation in response to high- and low-efficacy agonists and after PKC activation. S327/S329...
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Agonist-induced Serine335/Serine336 phosphorylation of the Cannabinoid Receptor 2.
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 Threonine360/Serine364 phosphorylation of the β2 Adrenoceptor
pT360/pS364-β2 (phospho-β2-Adrenoceptor Antibody)
Threonine360/Serine364 (T360/S364) is a major phosphorylation site of the β2 adrenoceptor. The pT360/pS364-β2 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. T360/S364...
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Agonist-induced Serine355/Serine356 phosphorylation of the β2 Adrenoceptor
pS355/pS356-β2 (phospho-β2-Adrenoceptor Antibody)
Serine355/Serine356 (S355/S356) is a major phosphorylation site of the β2 adrenoceptor. The pS355/pS356-β2 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S355/S356...
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Validation of the Hydroxycarboxylic Acid Receptor 2 in transfected HEK293 cells
HCA2 (non-phospho) Hydroxycarboxylic Acid...
The non-phospho HCA2 receptor antibody is directed against the distal end of the carboxyl-terminal tail human HCA2 receptor. It can be used to detect total HCA2 receptors in Western blots independent of phosphorylation. It can also be...
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Validation of the Calcitonin Receptor-Like Receptor in transfected HEK293 cells
CALCR (GP-non-phospho) Calcitonin Receptor-Like...
The non-phospho-CALCR receptor antibody is directed against the distal end of the carboxyl-terminal tail of human CALCR. It can be used to detect total CALCR receptors in Western blots independent of phosphorylation. The CALCR antibody...
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Validation of the Dopamine Receptor 5 in transfected HEK293 cells
D5 (non-phospho), Dopamine Receptor 5 Antibody
The non-phospho-Dopamine Receptor 5 Antibody is directed against the distal end of the carboxyl-terminal tail of human D5. It can be used to detect total D5 receptors in Western blots independent of phosphorylation. The non-phospho-D5...
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Agonist-induced Threonine382/Threonine386 phosphorylation of the Dopamine Receptor 5
pT382/pT386-D5 (phospho-Dopamine Receptor 5...
Threonine382/Threonine386 (T382/T386) is a major phosphorylation site of the D5 receptor. The pT382/pT386-D5 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. T382/T386...
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Agonist-induced Serine257/Threonine262 phosphorylation of the D3 Dopamine Receptor
pS257/pT262-D3 (phospho-Dopamine Receptor 3...
Serine257/Threonine262 (S257/T262) is a major phosphorylation site of the D3 dopamine receptor. The pS257/pT262-D3 antibody detects phosphorylation in response to high- and low-efficacy agonists but not after PKC activation. S262/T262...
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Immunohistochemical identification of Dopamine Receptor 1 and Dopamine Receptor 2 in striatum
D2 (IHC-grade), Dopamine Receptor 2 Antibody
The D2 receptor antibody is directed against the third intracellular loop of mouse, rat and human D2 dopamine receptor. It detects both the long and short form of D2. It can be used to detect total D2 receptors in Western blots...
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Immunohistochemical identification of the Hydroxycarboxylic Acid Receptor 1 in pancreas
HCA1 (IHC-grade), Hydroxycarboxylic Acid...
The non-phospho HCA1 receptor antibody is directed against the distal end of the carboxyl-terminal tail human HCA1 receptor. It can be used to detect total HCA1 receptors in Western blots independent of phosphorylation. It can also be...
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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...
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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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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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