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Most Recent References

Walker MF, Zhang J, Steiner W, Ku PI, Zhu JF, Michaelson Z, Yen YC, Long AB, Casey MJ, Poddar A, Nelson IB, Arveseth CD, Nagel F, Clough R, LaPotin S, Kwan KM, Schulz S, Stewart RA, Tesmer JJG, Caspary T, Subramanian R, Ge X, Myers BR. A Ciliary SMOOTHENED-GRK2-PKA Signaling Pathway Initiates Hedgehog Signal Transduction. bioRxiv [Preprint]. 2023 May 11:2023.05.10.540226. doi:
10.1101/2023.05.10.540226. PMID: 37214942; PMCID: PMC10197709.

Fritzwanker S, Nagel F, Kliewer A, Stammer V, Schulz S. In situ visualization of opioid and cannabinoid drug effects using phosphosite-specific GPCR antibodies. Commun Biol. 2023 Apr 15;6(1):419. doi: 10.1038/s42003-023-04786-2. PMID: 37061609; PMCID: PMC10105690.

Kaufmann J, Blum NK, Nagel F, Schuler A, Drube J, Degenhart C, Engel J,Eickhoff JE, Dasgupta P, Fritzwanker S, Guastadisegni M, Schulte C, Miess-Tanneberg E, Maric HM, Spetea M, Kliewer A, Baumann M, Klebl B, Reinscheid RK,Hoffmann C, Schulz S. A bead-based GPCR phosphorylation immunoassay for high-throughput ligand profiling and GRK inhibitor screening. Commun Biol. 2022 Nov 9;5(1):1206. doi: 10.1038/s42003-022-04135-9. PMID: 36352263; PMCID: PMC9646841.

Drube J, Haider RS, Matthees ESF, Reichel M, Zeiner J, Fritzwanker S, Ziegler C, Barz S, Klement L, Filor J, Weitzel V, Kliewer A, Miess-Tanneberg E, Kostenis E, Schulz S, Hoffmann C. GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation. Nat Commun. 2022 Jan 27;13(1):540. doi: 10.1038/s41467-022-28152-8. PMID: 35087057; PMCID: PMC8795447.

Benkel T, Zimmermann M, Zeiner J, Bravo S, Merten N, Lim VJY, Matthees ESF, Drube J, Miess-Tanneberg E, Malan D, Szpakowska M, Monteleone S, Grimes J, Koszegi Z, Lanoiselée Y, O'Brien S, Pavlaki N, Dobberstein N, Inoue A, Nikolaev V, Calebiro D, Chevigné A, Sasse P, Schulz S, Hoffmann C, Kolb P, Waldhoer M, Simon K, Gomeza J, Kostenis E. How Carvedilol activates β2-adrenoceptors. Nat Commun. 2022 Nov 19;13(1):7109. doi: 10.1038/s41467-022-34765-w. PMID: 36402762; PMCID: PMC9675828.

Marsango S, Ward RJ, Jenkins L, Butcher AJ, Al Mahmud Z, Dwomoh L, Nagel F, Schulz S, Tikhonova IG, Tobin AB, Milligan G. Selective phosphorylation of threonine residues defines GPR84-arrestin interactions of biased ligands. J Biol Chem. 2022 May;298(5):101932. doi: 10.1016/j.jbc.2022.101932. Epub 2022 Apr 12. PMID: 35427647; PMCID: PMC9118924.

Divorty N, Jenkins L, Ganguly A, Butcher AJ, Hudson BD, Schulz S, Tobin AB, Nicklin SA, Milligan G. Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor. J Biol Chem. 2022 Mar;298(3):101655. doi: 10.1016/j.jbc.2022.101655. Epub 2022 Jan 29. PMID: 35101446; PMCID: PMC8892012.

Recent References using 7TM Antibodies

Fritzwanker S, Moulédous L, Mollereau C, Froment C, Burlet-Schiltz O, Effah F, Bailey A, Spetea M, Reinscheid RK, Schulz S, Kliewer A. HA-MOP knockin mice express the canonical µ-opioid receptor but lack detectable splice variants. Commun Biol. 2021 Sep 14;4(1):1070. doi: 10.1038/s42003-021-02580-6. PMID: 34522000.

Fritzwanker S, Schulz S, Kliewer A. SR-17018 Stimulates Atypical µ-Opioid Receptor Phosphorylation and Dephosphorylation. Molecules. 2021 Jul 27;26(15):4509. doi: 10.3390/molecules26154509. PMID: 34361663; PMCID: PMC8348759.

Mann A, Keen AC, Mark H, Dasgupta P, Javitch JA, Canals M, Schulz S, Robert Lane J. New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D2 receptor regulation and signaling. Sci Rep. 2021 Apr 15;11(1):8288. doi: 10.1038/s41598-021-87417-2. PMID: 33859231; PMCID: PMC8050214.

Mann A, Liebetrau S, Klima M, Dasgupta P, Massotte D, Schulz S. Agonist-induced phosphorylation bar code and differential post-activation signaling of the delta opioid receptor revealed by phosphosite-specific antibodies. Sci Rep. 2020 May 22;10(1):8585. doi: 10.1038/s41598-020-65589-7. PMID: 32444688

Gillis A, Gondin AB, Kliewer A, Sanchez J, Lim HD, Alamein C, Manandhar P,Santiago M, Fritzwanker S, Schmiedel F, Katte TA, Reekie T, Grimsey NL, Kassiou M, Kellam B, Krasel C, Halls ML, Connor M, Lane JR, Schulz S, Christie MJ, Canals M. Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists. Sci Signal. 2020 Mar 31;13(625). pii: eaaz3140. doi: 10.1126/scisignal.aaz3140. PubMed PMID: 32234959.

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.

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.

References showing the physiological relevance of GPCR phosphorylation for receptor desensitization, tolerance and addiction

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.

Yousuf A, Miess E, Sianati S, Du YP, Schulz S, Christie MJ. Role of Phosphorylation Sites in Desensitization of µ-Opioid Receptor. Mol Pharmacol. 2015 Oct;88(4):825-35. doi: 10.1124/mol.115.098244. Epub 2015 May 12. PubMed PMID: 25969388.

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.

Bowman SL, Soohoo AL, Shiwarski DJ, Schulz S, Pradhan AA, Puthenveedu MA. Cell-autonomous regulation of Mu-opioid receptor recycling by substance P. Cell Rep. 2015 Mar 24;10(11):1925-36. PubMed PMID: 25801029; PubMed Central PMCID: PMC4494997.

Grecksch G, Just S, Pierstorff C, Imhof AK, Glück L, Doll C, Lupp A, Becker A, Koch T, Stumm R, Höllt V, Schulz S. Analgesic tolerance to high-efficacy agonists but not to morphine is diminished in phosphorylation-deficient S375A μ-opioid receptor knock-in mice. J Neurosci. 2011 Sep 28;31(39):13890-6. doi: 10.1523/JNEUROSCI.2304-11.2011. PubMed PMID: 21957251; PubMed Central PMCID: PMC6633166.

References showing the physiological relevance of phosphorylation for receptor-mediated ligand sequestration

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.

Sánchez-Alcañiz JA, Haege S, Mueller W, Pla R, Mackay F, Schulz S, López-Bendito G, Stumm R, Marín O. Cxcr7 controls neuronal migration by regulating chemokine responsiveness. Neuron. 2011 Jan 13;69(1):77-90. doi: 10.1016/j.neuron.2010.12.006. PubMed PMID: 21220100.

Nakai A, Fujimoto J, Miyata H, Stumm R, Narazaki M, Schulz S, Baba Y, Kumanogoh A, Suzuki K. The COMMD3/8 complex determines GRK6 specificity for chemoattractant receptors. J Exp Med. 2019 Jul 1;216(7):1630-1647. doi: 10.1084/jem.20181494. Epub 2019 May 14. PubMed PMID: 31088898; PubMed Central PMCID: PMC6605747.

References showing hierarchical phosphorylation patterns of GPCRs: The Phosphorylation Bar Code

Just S, Illing S, Trester-Zedlitz M, Lau EK, Kotowski SJ, Miess E, Mann A, Doll C, Trinidad JC, Burlingame AL, von Zastrow M, Schulz S. Differentiation of opioid drug effects by hierarchical multi-site phosphorylation. Mol Pharmacol. 2013 Mar;83(3):633-9. doi: 10.1124/mol.112.082875. Epub 2012 Dec 13. PubMed PMID: 23239825; PubMed Central PMCID: PMC3583494.

Doll C, Konietzko J, Pöll F, Koch T, Höllt V, Schulz S. Agonist-selective patterns of µ-opioid receptor phosphorylation revealed by phosphosite-specific antibodies. Br J Pharmacol. 2011 Sep;164(2):298-307. doi: 10.1111/j.1476-5381.2011.01382.x. PubMed PMID: 21449911; PubMed Central PMCID: PMC3174411.

Pöll F, Lehmann D, Illing S, Ginj M, Jacobs S, Lupp A, Stumm R, Schulz S. Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation. Mol Endocrinol. 2010 Feb;24(2):436-46. doi: 10.1210/me.2009-0315. Epub 2010 Jan 5. PubMed PMID: 20051480; PubMed Central PMCID: PMC5428126.

Lehmann A, Kliewer A, Schütz D, Nagel F, Stumm R, Schulz S. Carboxyl-terminal multi-site phosphorylation regulates internalization and desensitization of the human sst2 somatostatin receptor. Mol Cell Endocrinol. 2014 Apr 25;387(1-2):44-51. doi: 10.1016/j.mce.2014.02.009. Epub 2014 Feb 22. PubMed PMID: 24565897.

Chiu YT, Chen C, Yu D, Schulz S, Liu-Chen LY. Agonist-Dependent and -Independent κ Opioid Receptor Phosphorylation: Distinct Phosphorylation Patterns and Different Cellular Outcomes. Mol Pharmacol. 2017 Nov;92(5):588-600. doi: 10.1124/mol.117.108555. Epub 2017 Sep 11. Erratum in: Mol Pharmacol. 2018 Aug;94(2):895. PubMed PMID: 28893975; PubMed Central PMCID: PMC5635518.

Lehmann A, Kliewer A, Günther T, Nagel F, Schulz S. Identification of Phosphorylation Sites Regulating sst3 Somatostatin Receptor Trafficking. Mol Endocrinol. 2016 Jun;30(6):645-59. doi: 10.1210/me.2015-1244. Epub 2016 Apr 21. PubMed PMID: 27101376; PubMed Central PMCID: PMC5414643.

Kliewer A, Mann A, Petrich A, Pöll F, Schulz S. A transplantable phosphorylation probe for direct assessment of G protein-coupled receptor activation. PLoS One. 2012;7(6):e39458. doi: 10.1371/journal.pone.0039458. Epub 2012 Jun 26. PubMed PMID: 22745760; PubMed Central PMCID: PMC3383726.

References showing the identification of GPCR kinases and phosphates using Premium Phosphorylation Site-Specific 7TM Antibodies

Pöll F, Doll C, Schulz S. Rapid dephosphorylation of G protein-coupled receptors by protein phosphatase 1β is required for termination of β-arrestin-dependent signaling. J Biol Chem. 2011 Sep 23;286(38):32931-6. doi:10.1074/jbc.M111.224899. Epub 2011 Jul 27. PubMed PMID: 21795688; PubMed Central PMCID: PMC3190940.

Doll C, Pöll F, Peuker K, Loktev A, Glück L, Schulz S. Deciphering µ-opioid receptor phosphorylation and dephosphorylation in HEK293 cells. Br J Pharmacol. 2012 Nov;167(6):1259-70. doi: 10.1111/j.1476-5381.2012.02080.x. PubMed PMID: 22725608; PubMed Central PMCID: PMC3504992.

Lehmann A, Kliewer A, Märtens JC, Nagel F, Schulz S. Carboxyl-terminal receptor domains control the differential dephosphorylation of somatostatin receptors by protein phosphatase 1 isoforms. PLoS One. 2014 Mar 17;9(3):e91526. doi: 10.1371/journal.pone.0091526. eCollection 2014. PubMed PMID: 24637622; PubMed Central PMCID: PMC3956607.

Lehmann A, Kliewer A, Günther T, Nagel F, Schulz S. Identification of Phosphorylation Sites Regulating sst3 Somatostatin Receptor Trafficking. Mol Endocrinol. 2016 Jun;30(6):645-59. doi: 10.1210/me.2015-1244. Epub 2016 Apr 21. PubMed PMID: 27101376; PubMed Central PMCID: PMC5414643.

Nakai A, Fujimoto J, Miyata H, Stumm R, Narazaki M, Schulz S, Baba Y, Kumanogoh A, Suzuki K. The COMMD3/8 complex determines GRK6 specificity for chemoattractant receptors. J Exp Med. 2019 Jul 1;216(7):1630-1647. doi: 10.1084/jem.20181494. Epub 2019 May 14. PubMed PMID: 31088898; PubMed Central PMCID: PMC6605747.

Luo J, Busillo JM, Stumm R, Benovic JL. G Protein-Coupled Receptor Kinase 3 and Protein Kinase C Phosphorylate the Distal C-Terminal Tail of the Chemokine Receptor CXCR4 and Mediate Recruitment of β-Arrestin. Mol Pharmacol. 2017 Jun;91(6):554-566. doi: 10.1124/mol.116.106468. Epub 2017 Mar 22. PubMed PMID: 28331048; PubMed Central PMCID: PMC5438129.

Mueller W, Schütz D, Nagel F, Schulz S, Stumm R. Hierarchical organization of multi-site phosphorylation at the CXCR4 C terminus. PLoS One. 2013 May 29;8(5):e64975. doi: 10.1371/journal.pone.0064975. Print 2013. PubMed PMID: 23734232; PubMed Central PMCID: PMC3666969.

References showing the diagnostic and predictive value of Premium IHC-Grade 7TM Antibodies

Asnacios A, Courbon F, Rochaix P, Bauvin E, Cances-Lauwers V, Susini C, Schulz S, Boneu A, Guimbaud R, Buscail L. Indium-111-pentetreotide scintigraphy and somatostatin receptor subtype 2 expression: new prognostic factors for malignant well-differentiated endocrine tumors. J Clin Oncol. 2008 Feb 20;26(6):963-70. doi: 10.1200/JCO.2007.12.7431. PubMed PMID: 18281671.

Lee M, Lupp A, Mendoza N, Martin N, Beschorner R, Honegger J, Schlegel J, Shively T, Pulz E, Schulz S, Roncaroli F, Pellegata NS. SSTR3 is a putative target for the medical treatment of gonadotroph adenomas of the pituitary. Endocr Relat Cancer. 2015 Feb;22(1):111-9. doi: 10.1530/ERC-14-0472. Epub 2014 Dec 16. PubMed PMID: 25515731.

Kaemmerer D, Specht E, Sänger J, Wirtz RM, Sayeg M, Schulz S, Lupp A. Somatostatin receptors in bronchopulmonary neuroendocrine neoplasms: new diagnostic, prognostic, and therapeutic markers. J Clin Endocrinol Metab. 2015 Mar;100(3):831-40. doi: 10.1210/jc.2014-2699. Epub 2014 Dec 12. PubMed PMID: 25494861.

Casar-Borota O, Heck A, Schulz S, Nesland JM, Ramm-Pettersen J, Lekva T, Alafuzoff I, Bollerslev J. Expression of SSTR2a, but not of SSTRs 1, 3, or 5 in somatotroph adenomas assessed by monoclonal antibodies was reduced by octreotide and correlated with the acute and long-term effects of octreotide. J Clin Endocrinol Metab. 2013 Nov;98(11):E1730-9. doi: 10.1210/jc.2013-2145. Epub 2013 Oct 3. PubMed PMID: 24092823.

van der Pas R, Feelders RA, Gatto F, de Bruin C, Pereira AM, van Koetsveld PM, Sprij-Mooij DM, Waaijers AM, Dogan F, Schulz S, Kros JM, Lamberts SW, Hofland LJ. Preoperative normalization of cortisol levels in Cushing's disease after medical treatment: consequences for somatostatin and dopamine receptor subtype expression and in vitro response to somatostatin analogs and dopamine agonists. J Clin Endocrinol Metab. 2013 Dec;98(12):E1880-90. doi: 10.1210/jc.2013-1987. Epub 2013 Sep 30. PubMed PMID: 24081741.

Chahal HS, Trivellin G, Leontiou CA, Alband N, Fowkes RC, Tahir A, Igreja SC, Chapple JP, Jordan S, Lupp A, Schulz S, Ansorge O, Karavitaki N, Carlsen E, Wass JA, Grossman AB, Korbonits M. Somatostatin analogs modulate AIP in somatotroph adenomas: the role of the ZAC1 pathway. J Clin Endocrinol Metab. 2012 Aug;97(8):E1411-20. doi: 10.1210/jc.2012-1111. Epub 2012 Jun 1. PubMed PMID: 22659247.

Plöckinger U, Albrecht S, Mawrin C, Saeger W, Buchfelder M, Petersenn S, Schulz S. Selective loss of somatostatin receptor 2 in octreotide-resistant growth hormone-secreting adenomas. J Clin Endocrinol Metab. 2008 Apr;93(4):1203-10. doi: 10.1210/jc.2007-1986. Epub 2008 Jan 15. PubMed PMID: 18198230.

Mundschenk J, Unger N, Schulz S, Höllt V, Schulz S, Steinke R, Lehnert H. Somatostatin receptor subtypes in human pheochromocytoma: subcellular expression pattern and functional relevance for octreotide scintigraphy. J Clin Endocrinol Metab. 2003 Nov;88(11):5150-7. PubMed PMID: 14602742.

Schulz S, Pauli SU, Schulz S, Händel M, Dietzmann K, Firsching R, Höllt V. Immunohistochemical determination of five somatostatin receptors in meningioma reveals frequent overexpression of somatostatin receptor subtype sst2A. Clin Cancer Res. 2000 May;6(5):1865-74. PubMed PMID: 10815909.

References showing the generation and characterization of Premium IHC-Grade 7TM Antibodies

Schulz S, Schreff M, Schmidt H, Händel M, Przewlocki R, Höllt V. Immunocytochemical localization of somatostatin receptor sst2A in the rat spinal cord and dorsal root ganglia. Eur J Neurosci. 1998 Dec;10(12):3700-8. PubMed PMID: 9875349.

Händel M, Schulz S, Stanarius A, Schreff M, Erdtmann-Vourliotis M, Schmidt H, Wolf G, Höllt V. Selective targeting of somatostatin receptor 3 to neuronal cilia. Neuroscience. 1999 Mar;89(3):909-26. PubMed PMID: 10199624.

Schulz S, Pauli SU, Schulz S, Händel M, Dietzmann K, Firsching R, Höllt V. Immunohistochemical determination of five somatostatin receptors in meningioma reveals frequent overexpression of somatostatin receptor subtype sst2A. Clin Cancer Res. 2000 May;6(5):1865-74. PubMed PMID: 10815909.

Lupp A, Nagel F, Doll C, Röcken C, Evert M, Mawrin C, Saeger W, Schulz S. Reassessment of sst3 somatostatin receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-5. Neuroendocrinology. 2012;96(4):301-10. doi: 10.1159/000337659. Epub 2012 May 4. PubMed PMID: 22414742.

Lupp A, Hunder A, Petrich A, Nagel F, Doll C, Schulz S. Reassessment of sst(5) somatostatin receptor expression in normal and neoplastic human tissues using the novel rabbit monoclonal antibody UMB-4. Neuroendocrinology. 2011;94(3):255-64. doi: 10.1159/000329876. Epub 2011 Sep 27. PubMed PMID: 21952553.

Fischer T, Doll C, Jacobs S, Kolodziej A, Stumm R, Schulz S. Reassessment of sst2 somatostatin receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-1. J Clin Endocrinol Metab. 2008 Nov;93(11):4519-24. doi: 10.1210/jc.2008-1063. Epub 2008 Aug 12. PubMed PMID: 18697876.

Fischer T, Nagel F, Jacobs S, Stumm R, Schulz S. Reassessment of CXCR4 chemokine receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-2. PLoS One. 2008;3(12):e4069. doi: 10.1371/journal.pone.0004069. Epub 2008 Dec 31. PubMed PMID: 19116653; PubMed Central PMCID: PMC2605258.

Most Recent References Walker MF, Zhang J, Steiner W, Ku PI, Zhu JF, Michaelson Z, Yen YC, Long AB, Casey MJ, Poddar A, Nelson IB, Arveseth CD, Nagel F, Clough R, LaPotin S, Kwan KM, Schulz S,... read more »
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7TM Antibodies References

Most Recent References

Walker MF, Zhang J, Steiner W, Ku PI, Zhu JF, Michaelson Z, Yen YC, Long AB, Casey MJ, Poddar A, Nelson IB, Arveseth CD, Nagel F, Clough R, LaPotin S, Kwan KM, Schulz S, Stewart RA, Tesmer JJG, Caspary T, Subramanian R, Ge X, Myers BR. A Ciliary SMOOTHENED-GRK2-PKA Signaling Pathway Initiates Hedgehog Signal Transduction. bioRxiv [Preprint]. 2023 May 11:2023.05.10.540226. doi:
10.1101/2023.05.10.540226. PMID: 37214942; PMCID: PMC10197709.

Fritzwanker S, Nagel F, Kliewer A, Stammer V, Schulz S. In situ visualization of opioid and cannabinoid drug effects using phosphosite-specific GPCR antibodies. Commun Biol. 2023 Apr 15;6(1):419. doi: 10.1038/s42003-023-04786-2. PMID: 37061609; PMCID: PMC10105690.

Kaufmann J, Blum NK, Nagel F, Schuler A, Drube J, Degenhart C, Engel J,Eickhoff JE, Dasgupta P, Fritzwanker S, Guastadisegni M, Schulte C, Miess-Tanneberg E, Maric HM, Spetea M, Kliewer A, Baumann M, Klebl B, Reinscheid RK,Hoffmann C, Schulz S. A bead-based GPCR phosphorylation immunoassay for high-throughput ligand profiling and GRK inhibitor screening. Commun Biol. 2022 Nov 9;5(1):1206. doi: 10.1038/s42003-022-04135-9. PMID: 36352263; PMCID: PMC9646841.

Drube J, Haider RS, Matthees ESF, Reichel M, Zeiner J, Fritzwanker S, Ziegler C, Barz S, Klement L, Filor J, Weitzel V, Kliewer A, Miess-Tanneberg E, Kostenis E, Schulz S, Hoffmann C. GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation. Nat Commun. 2022 Jan 27;13(1):540. doi: 10.1038/s41467-022-28152-8. PMID: 35087057; PMCID: PMC8795447.

Benkel T, Zimmermann M, Zeiner J, Bravo S, Merten N, Lim VJY, Matthees ESF, Drube J, Miess-Tanneberg E, Malan D, Szpakowska M, Monteleone S, Grimes J, Koszegi Z, Lanoiselée Y, O'Brien S, Pavlaki N, Dobberstein N, Inoue A, Nikolaev V, Calebiro D, Chevigné A, Sasse P, Schulz S, Hoffmann C, Kolb P, Waldhoer M, Simon K, Gomeza J, Kostenis E. How Carvedilol activates β2-adrenoceptors. Nat Commun. 2022 Nov 19;13(1):7109. doi: 10.1038/s41467-022-34765-w. PMID: 36402762; PMCID: PMC9675828.

Marsango S, Ward RJ, Jenkins L, Butcher AJ, Al Mahmud Z, Dwomoh L, Nagel F, Schulz S, Tikhonova IG, Tobin AB, Milligan G. Selective phosphorylation of threonine residues defines GPR84-arrestin interactions of biased ligands. J Biol Chem. 2022 May;298(5):101932. doi: 10.1016/j.jbc.2022.101932. Epub 2022 Apr 12. PMID: 35427647; PMCID: PMC9118924.

Divorty N, Jenkins L, Ganguly A, Butcher AJ, Hudson BD, Schulz S, Tobin AB, Nicklin SA, Milligan G. Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor. J Biol Chem. 2022 Mar;298(3):101655. doi: 10.1016/j.jbc.2022.101655. Epub 2022 Jan 29. PMID: 35101446; PMCID: PMC8892012.

Recent References using 7TM Antibodies

Fritzwanker S, Moulédous L, Mollereau C, Froment C, Burlet-Schiltz O, Effah F, Bailey A, Spetea M, Reinscheid RK, Schulz S, Kliewer A. HA-MOP knockin mice express the canonical µ-opioid receptor but lack detectable splice variants. Commun Biol. 2021 Sep 14;4(1):1070. doi: 10.1038/s42003-021-02580-6. PMID: 34522000.

Fritzwanker S, Schulz S, Kliewer A. SR-17018 Stimulates Atypical µ-Opioid Receptor Phosphorylation and Dephosphorylation. Molecules. 2021 Jul 27;26(15):4509. doi: 10.3390/molecules26154509. PMID: 34361663; PMCID: PMC8348759.

Mann A, Keen AC, Mark H, Dasgupta P, Javitch JA, Canals M, Schulz S, Robert Lane J. New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D2 receptor regulation and signaling. Sci Rep. 2021 Apr 15;11(1):8288. doi: 10.1038/s41598-021-87417-2. PMID: 33859231; PMCID: PMC8050214.

Mann A, Liebetrau S, Klima M, Dasgupta P, Massotte D, Schulz S. Agonist-induced phosphorylation bar code and differential post-activation signaling of the delta opioid receptor revealed by phosphosite-specific antibodies. Sci Rep. 2020 May 22;10(1):8585. doi: 10.1038/s41598-020-65589-7. PMID: 32444688

Gillis A, Gondin AB, Kliewer A, Sanchez J, Lim HD, Alamein C, Manandhar P,Santiago M, Fritzwanker S, Schmiedel F, Katte TA, Reekie T, Grimsey NL, Kassiou M, Kellam B, Krasel C, Halls ML, Connor M, Lane JR, Schulz S, Christie MJ, Canals M. Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists. Sci Signal. 2020 Mar 31;13(625). pii: eaaz3140. doi: 10.1126/scisignal.aaz3140. PubMed PMID: 32234959.

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.

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.

References showing the physiological relevance of GPCR phosphorylation for receptor desensitization, tolerance and addiction

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.

Yousuf A, Miess E, Sianati S, Du YP, Schulz S, Christie MJ. Role of Phosphorylation Sites in Desensitization of µ-Opioid Receptor. Mol Pharmacol. 2015 Oct;88(4):825-35. doi: 10.1124/mol.115.098244. Epub 2015 May 12. PubMed PMID: 25969388.

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.

Bowman SL, Soohoo AL, Shiwarski DJ, Schulz S, Pradhan AA, Puthenveedu MA. Cell-autonomous regulation of Mu-opioid receptor recycling by substance P. Cell Rep. 2015 Mar 24;10(11):1925-36. PubMed PMID: 25801029; PubMed Central PMCID: PMC4494997.

Grecksch G, Just S, Pierstorff C, Imhof AK, Glück L, Doll C, Lupp A, Becker A, Koch T, Stumm R, Höllt V, Schulz S. Analgesic tolerance to high-efficacy agonists but not to morphine is diminished in phosphorylation-deficient S375A μ-opioid receptor knock-in mice. J Neurosci. 2011 Sep 28;31(39):13890-6. doi: 10.1523/JNEUROSCI.2304-11.2011. PubMed PMID: 21957251; PubMed Central PMCID: PMC6633166.

References showing the physiological relevance of phosphorylation for receptor-mediated ligand sequestration

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.

Sánchez-Alcañiz JA, Haege S, Mueller W, Pla R, Mackay F, Schulz S, López-Bendito G, Stumm R, Marín O. Cxcr7 controls neuronal migration by regulating chemokine responsiveness. Neuron. 2011 Jan 13;69(1):77-90. doi: 10.1016/j.neuron.2010.12.006. PubMed PMID: 21220100.

Nakai A, Fujimoto J, Miyata H, Stumm R, Narazaki M, Schulz S, Baba Y, Kumanogoh A, Suzuki K. The COMMD3/8 complex determines GRK6 specificity for chemoattractant receptors. J Exp Med. 2019 Jul 1;216(7):1630-1647. doi: 10.1084/jem.20181494. Epub 2019 May 14. PubMed PMID: 31088898; PubMed Central PMCID: PMC6605747.

References showing hierarchical phosphorylation patterns of GPCRs: The Phosphorylation Bar Code

Just S, Illing S, Trester-Zedlitz M, Lau EK, Kotowski SJ, Miess E, Mann A, Doll C, Trinidad JC, Burlingame AL, von Zastrow M, Schulz S. Differentiation of opioid drug effects by hierarchical multi-site phosphorylation. Mol Pharmacol. 2013 Mar;83(3):633-9. doi: 10.1124/mol.112.082875. Epub 2012 Dec 13. PubMed PMID: 23239825; PubMed Central PMCID: PMC3583494.

Doll C, Konietzko J, Pöll F, Koch T, Höllt V, Schulz S. Agonist-selective patterns of µ-opioid receptor phosphorylation revealed by phosphosite-specific antibodies. Br J Pharmacol. 2011 Sep;164(2):298-307. doi: 10.1111/j.1476-5381.2011.01382.x. PubMed PMID: 21449911; PubMed Central PMCID: PMC3174411.

Pöll F, Lehmann D, Illing S, Ginj M, Jacobs S, Lupp A, Stumm R, Schulz S. Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation. Mol Endocrinol. 2010 Feb;24(2):436-46. doi: 10.1210/me.2009-0315. Epub 2010 Jan 5. PubMed PMID: 20051480; PubMed Central PMCID: PMC5428126.

Lehmann A, Kliewer A, Schütz D, Nagel F, Stumm R, Schulz S. Carboxyl-terminal multi-site phosphorylation regulates internalization and desensitization of the human sst2 somatostatin receptor. Mol Cell Endocrinol. 2014 Apr 25;387(1-2):44-51. doi: 10.1016/j.mce.2014.02.009. Epub 2014 Feb 22. PubMed PMID: 24565897.

Chiu YT, Chen C, Yu D, Schulz S, Liu-Chen LY. Agonist-Dependent and -Independent κ Opioid Receptor Phosphorylation: Distinct Phosphorylation Patterns and Different Cellular Outcomes. Mol Pharmacol. 2017 Nov;92(5):588-600. doi: 10.1124/mol.117.108555. Epub 2017 Sep 11. Erratum in: Mol Pharmacol. 2018 Aug;94(2):895. PubMed PMID: 28893975; PubMed Central PMCID: PMC5635518.

Lehmann A, Kliewer A, Günther T, Nagel F, Schulz S. Identification of Phosphorylation Sites Regulating sst3 Somatostatin Receptor Trafficking. Mol Endocrinol. 2016 Jun;30(6):645-59. doi: 10.1210/me.2015-1244. Epub 2016 Apr 21. PubMed PMID: 27101376; PubMed Central PMCID: PMC5414643.

Kliewer A, Mann A, Petrich A, Pöll F, Schulz S. A transplantable phosphorylation probe for direct assessment of G protein-coupled receptor activation. PLoS One. 2012;7(6):e39458. doi: 10.1371/journal.pone.0039458. Epub 2012 Jun 26. PubMed PMID: 22745760; PubMed Central PMCID: PMC3383726.

References showing the identification of GPCR kinases and phosphates using Premium Phosphorylation Site-Specific 7TM Antibodies

Pöll F, Doll C, Schulz S. Rapid dephosphorylation of G protein-coupled receptors by protein phosphatase 1β is required for termination of β-arrestin-dependent signaling. J Biol Chem. 2011 Sep 23;286(38):32931-6. doi:10.1074/jbc.M111.224899. Epub 2011 Jul 27. PubMed PMID: 21795688; PubMed Central PMCID: PMC3190940.

Doll C, Pöll F, Peuker K, Loktev A, Glück L, Schulz S. Deciphering µ-opioid receptor phosphorylation and dephosphorylation in HEK293 cells. Br J Pharmacol. 2012 Nov;167(6):1259-70. doi: 10.1111/j.1476-5381.2012.02080.x. PubMed PMID: 22725608; PubMed Central PMCID: PMC3504992.

Lehmann A, Kliewer A, Märtens JC, Nagel F, Schulz S. Carboxyl-terminal receptor domains control the differential dephosphorylation of somatostatin receptors by protein phosphatase 1 isoforms. PLoS One. 2014 Mar 17;9(3):e91526. doi: 10.1371/journal.pone.0091526. eCollection 2014. PubMed PMID: 24637622; PubMed Central PMCID: PMC3956607.

Lehmann A, Kliewer A, Günther T, Nagel F, Schulz S. Identification of Phosphorylation Sites Regulating sst3 Somatostatin Receptor Trafficking. Mol Endocrinol. 2016 Jun;30(6):645-59. doi: 10.1210/me.2015-1244. Epub 2016 Apr 21. PubMed PMID: 27101376; PubMed Central PMCID: PMC5414643.

Nakai A, Fujimoto J, Miyata H, Stumm R, Narazaki M, Schulz S, Baba Y, Kumanogoh A, Suzuki K. The COMMD3/8 complex determines GRK6 specificity for chemoattractant receptors. J Exp Med. 2019 Jul 1;216(7):1630-1647. doi: 10.1084/jem.20181494. Epub 2019 May 14. PubMed PMID: 31088898; PubMed Central PMCID: PMC6605747.

Luo J, Busillo JM, Stumm R, Benovic JL. G Protein-Coupled Receptor Kinase 3 and Protein Kinase C Phosphorylate the Distal C-Terminal Tail of the Chemokine Receptor CXCR4 and Mediate Recruitment of β-Arrestin. Mol Pharmacol. 2017 Jun;91(6):554-566. doi: 10.1124/mol.116.106468. Epub 2017 Mar 22. PubMed PMID: 28331048; PubMed Central PMCID: PMC5438129.

Mueller W, Schütz D, Nagel F, Schulz S, Stumm R. Hierarchical organization of multi-site phosphorylation at the CXCR4 C terminus. PLoS One. 2013 May 29;8(5):e64975. doi: 10.1371/journal.pone.0064975. Print 2013. PubMed PMID: 23734232; PubMed Central PMCID: PMC3666969.

References showing the diagnostic and predictive value of Premium IHC-Grade 7TM Antibodies

Asnacios A, Courbon F, Rochaix P, Bauvin E, Cances-Lauwers V, Susini C, Schulz S, Boneu A, Guimbaud R, Buscail L. Indium-111-pentetreotide scintigraphy and somatostatin receptor subtype 2 expression: new prognostic factors for malignant well-differentiated endocrine tumors. J Clin Oncol. 2008 Feb 20;26(6):963-70. doi: 10.1200/JCO.2007.12.7431. PubMed PMID: 18281671.

Lee M, Lupp A, Mendoza N, Martin N, Beschorner R, Honegger J, Schlegel J, Shively T, Pulz E, Schulz S, Roncaroli F, Pellegata NS. SSTR3 is a putative target for the medical treatment of gonadotroph adenomas of the pituitary. Endocr Relat Cancer. 2015 Feb;22(1):111-9. doi: 10.1530/ERC-14-0472. Epub 2014 Dec 16. PubMed PMID: 25515731.

Kaemmerer D, Specht E, Sänger J, Wirtz RM, Sayeg M, Schulz S, Lupp A. Somatostatin receptors in bronchopulmonary neuroendocrine neoplasms: new diagnostic, prognostic, and therapeutic markers. J Clin Endocrinol Metab. 2015 Mar;100(3):831-40. doi: 10.1210/jc.2014-2699. Epub 2014 Dec 12. PubMed PMID: 25494861.

Casar-Borota O, Heck A, Schulz S, Nesland JM, Ramm-Pettersen J, Lekva T, Alafuzoff I, Bollerslev J. Expression of SSTR2a, but not of SSTRs 1, 3, or 5 in somatotroph adenomas assessed by monoclonal antibodies was reduced by octreotide and correlated with the acute and long-term effects of octreotide. J Clin Endocrinol Metab. 2013 Nov;98(11):E1730-9. doi: 10.1210/jc.2013-2145. Epub 2013 Oct 3. PubMed PMID: 24092823.

van der Pas R, Feelders RA, Gatto F, de Bruin C, Pereira AM, van Koetsveld PM, Sprij-Mooij DM, Waaijers AM, Dogan F, Schulz S, Kros JM, Lamberts SW, Hofland LJ. Preoperative normalization of cortisol levels in Cushing's disease after medical treatment: consequences for somatostatin and dopamine receptor subtype expression and in vitro response to somatostatin analogs and dopamine agonists. J Clin Endocrinol Metab. 2013 Dec;98(12):E1880-90. doi: 10.1210/jc.2013-1987. Epub 2013 Sep 30. PubMed PMID: 24081741.

Chahal HS, Trivellin G, Leontiou CA, Alband N, Fowkes RC, Tahir A, Igreja SC, Chapple JP, Jordan S, Lupp A, Schulz S, Ansorge O, Karavitaki N, Carlsen E, Wass JA, Grossman AB, Korbonits M. Somatostatin analogs modulate AIP in somatotroph adenomas: the role of the ZAC1 pathway. J Clin Endocrinol Metab. 2012 Aug;97(8):E1411-20. doi: 10.1210/jc.2012-1111. Epub 2012 Jun 1. PubMed PMID: 22659247.

Plöckinger U, Albrecht S, Mawrin C, Saeger W, Buchfelder M, Petersenn S, Schulz S. Selective loss of somatostatin receptor 2 in octreotide-resistant growth hormone-secreting adenomas. J Clin Endocrinol Metab. 2008 Apr;93(4):1203-10. doi: 10.1210/jc.2007-1986. Epub 2008 Jan 15. PubMed PMID: 18198230.

Mundschenk J, Unger N, Schulz S, Höllt V, Schulz S, Steinke R, Lehnert H. Somatostatin receptor subtypes in human pheochromocytoma: subcellular expression pattern and functional relevance for octreotide scintigraphy. J Clin Endocrinol Metab. 2003 Nov;88(11):5150-7. PubMed PMID: 14602742.

Schulz S, Pauli SU, Schulz S, Händel M, Dietzmann K, Firsching R, Höllt V. Immunohistochemical determination of five somatostatin receptors in meningioma reveals frequent overexpression of somatostatin receptor subtype sst2A. Clin Cancer Res. 2000 May;6(5):1865-74. PubMed PMID: 10815909.

References showing the generation and characterization of Premium IHC-Grade 7TM Antibodies

Schulz S, Schreff M, Schmidt H, Händel M, Przewlocki R, Höllt V. Immunocytochemical localization of somatostatin receptor sst2A in the rat spinal cord and dorsal root ganglia. Eur J Neurosci. 1998 Dec;10(12):3700-8. PubMed PMID: 9875349.

Händel M, Schulz S, Stanarius A, Schreff M, Erdtmann-Vourliotis M, Schmidt H, Wolf G, Höllt V. Selective targeting of somatostatin receptor 3 to neuronal cilia. Neuroscience. 1999 Mar;89(3):909-26. PubMed PMID: 10199624.

Schulz S, Pauli SU, Schulz S, Händel M, Dietzmann K, Firsching R, Höllt V. Immunohistochemical determination of five somatostatin receptors in meningioma reveals frequent overexpression of somatostatin receptor subtype sst2A. Clin Cancer Res. 2000 May;6(5):1865-74. PubMed PMID: 10815909.

Lupp A, Nagel F, Doll C, Röcken C, Evert M, Mawrin C, Saeger W, Schulz S. Reassessment of sst3 somatostatin receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-5. Neuroendocrinology. 2012;96(4):301-10. doi: 10.1159/000337659. Epub 2012 May 4. PubMed PMID: 22414742.

Lupp A, Hunder A, Petrich A, Nagel F, Doll C, Schulz S. Reassessment of sst(5) somatostatin receptor expression in normal and neoplastic human tissues using the novel rabbit monoclonal antibody UMB-4. Neuroendocrinology. 2011;94(3):255-64. doi: 10.1159/000329876. Epub 2011 Sep 27. PubMed PMID: 21952553.

Fischer T, Doll C, Jacobs S, Kolodziej A, Stumm R, Schulz S. Reassessment of sst2 somatostatin receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-1. J Clin Endocrinol Metab. 2008 Nov;93(11):4519-24. doi: 10.1210/jc.2008-1063. Epub 2008 Aug 12. PubMed PMID: 18697876.

Fischer T, Nagel F, Jacobs S, Stumm R, Schulz S. Reassessment of CXCR4 chemokine receptor expression in human normal and neoplastic tissues using the novel rabbit monoclonal antibody UMB-2. PLoS One. 2008;3(12):e4069. doi: 10.1371/journal.pone.0004069. Epub 2008 Dec 31. PubMed PMID: 19116653; PubMed Central PMCID: PMC2605258.

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