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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
KD-Validated
NEW
Western blot analysis of Somatostatin Receptor 1 in membrane preparations from cells of AtT-20 and BON-1 cell lines.
SST1 [UMB7] (RM-non-phospho-Somatostatin...
The SST1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 1. It can be used to detect total SST1 receptors in Western blots independent of phosphorylation. The SST1...
CHF495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Immunohistochemical identification of Somatostatin Receptor 1 in human pituitary.
SST1 [UMB7] (RM-IHC-grade), Somatostatin...
The SST1 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 1. It can be used to detect total SST1 receptors in Western blots independent of phosphorylation. The SST1...
CHF495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Immunohistochemical identification of Endotheline Receptor A in mouse heart.
ETA [UMB8] (RM-IHC-grade), Endothelin Receptor...
The ETA receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human endothelin receptor A. It can be used to detect ETA receptors in Western blots in a phosphorylation-sensitive manner...
CHF495.00 *
Details
Rabbit Monoclonal
KD-Validated
NEW
Indentification of the Endothelin Receptor A in mouse tissues.
ETA [UMB8] (RM-non-phospho-Endothelin Receptor...
The ETA receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human endothelin receptor A. It can be used to detect ETA receptors in Western blots in a phosphorylation-sensitive manner...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Validation of the Somatostatin Receptor 4 in transfected HEK293 cells
SST4 [UMB9] (RM-non-phospho), Somatostatin...
The non-phospho-SST4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human SST4. In can be used to detect total SST4 receptors in Western blots independent of phosphorylation. The non-phospho-SST4...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Immunohistochemical identification of Somatostatin Receptor 4 in parathyroid adenoma
SST4 [UMB9] (RM-IHC-grade), Somatostatin...
The SST4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human Somatostatin Receptor 4. In can be used to detect total SST4 receptors in Western blots independent of phosphorylation. The SST4...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Validation of the Dopamine Receptor 1 in transfected HEK293 cells
D1 [UMB10] (RM-non-phospho), Dopamine Receptor...
The non-phospho-D1 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human D1. It can be used to detect total D1 receptors in Western blots independent of phosphorylation. The non-phospho-D1 antibody...
CHF495.00 *
Details
Rabbit Monoclonal
NEW
Immunohistochemical identification of Dopamine Receptor 1 in striatum
D1 [UMB10] (RM-IHC-grade), Dopamine Receptor 1...
The non-phospho-D1 receptor antibody is directed against the distal part of the carboxyl-terminal tail of human D1. It can be used to detect total D1 receptors in Western blots independent of phosphorylation. The non-phospho-D1 antibody...
CHF495.00 *
Details
Rabbit Monoclonal
KO-Validated
NEW
Validation of the µ-Opioid Receptor in transfected HEK293 cells
MOP [UMB3] (RM-non-phospho), µ-Opioid Receptor...
The non-phospho-µ-opioid receptor antibody is directed against the distal end of the carboxyl-terminal tail of mouse, rat and human MOP. It detects selectively the canonical form of MOP and none of the putative splice variants. It can be...
CHF495.00 *
Details
NEW
Validation of the GPR97/ADGR3G Receptor in transfected HEK293 cells
ADGRG3/GPR97 (non-phospho), Adhesion Receptor...
The non-phospho-ADGRG3/GPR97 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human ADGRG3/GPR97. It can be used to detect total ADGRG3/GPR97 receptors in Western blots independent of phosphorylation....
CHF400.00 *
Details
Citations
Validation of the Parathyroid Hormone Receptor 1 in transfected HEK293 cells
PTH1 (non-phospho-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 *
Details
NEW
Validation of the GPR161 Receptor in transfected HEK293 cells
GPR161 (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 Bradykinin Receptor 2 in transfected HEK293 cells
B2 (non-phospho-Bradykinin Receptor 2 Antibody)
The non-phospho-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 non-phospho-B2 antibody...
CHF400.00 *
Details
NEW
Validation of the BLT2 Receptor in transfected HEK293 cells.
BLT2 (non-phospho), Leukotriene Receptor BLT2...
The non-phospho-BLT2 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human BLT2. It can be used to detect total BLT2 receptors in Western blots independent of phosphorylation. The BLT2 antibody can...
CHF400.00 *
Details
NEW
Agonist-induced Serine300/Serine303 phosphorylation of GPR35 Receptor.
pS300/pS303-hGPR35 (phospho-human GPR35 Antibody)
Serine300/Serine303 (S300/S303) is a major phosphorylation site of the human GPR35 receptor. The pS300/pS303-hGPR35 antibody detects phosphorylation in response to high-efficacy agonists. S300/S303 phosphorylation is a key regulator of...
CHF400.00 *
Details
Citations
NEW
Agonist-induced Serine298/Serine301 phosphorylation of mouse GPR35 Receptor
pS298/pS301-mGPR35 (phospho-mouse GPR35 Antibody)
Serine298/Serine301 (S298/S301) is a major phosphorylation site of the mouse GPR35 receptor. The pS298/pS301-mGPR35 antibody detects phosphorylation in response to high-efficacy agonists. S298/S301 phosphorylation is a key regulator of...
CHF400.00 *
Details
30 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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