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2001 6
2002 6
2003 7
2004 5
2005 7
2006 8
2007 5
2008 5
2009 8
2010 7
2011 9
2012 6
2013 9
2014 13
2015 7
2016 12
2017 13
2018 15
2019 9
2020 11
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2024 8

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Page 1
A molecular mechanism to diversify Ca2+ signaling downstream of Gs protein-coupled receptors.
Brands J, Bravo S, Jürgenliemke L, Grätz L, Schihada H, Frechen F, Alenfelder J, Pfeil C, Ohse PG, Hiratsuka S, Kawakami K, Schmacke LC, Heycke N, Inoue A, König G, Pfeifer A, Wachten D, Schulte G, Steinmetzer T, Watts VJ, Gomeza J, Simon K, Kostenis E. Brands J, et al. Among authors: kostenis e. Nat Commun. 2024 Sep 3;15(1):7684. doi: 10.1038/s41467-024-51991-6. Nat Commun. 2024. PMID: 39227390 Free PMC article.
Reply to: How carvedilol does not activate β2-adrenoceptors.
Kostenis E, Gomeza J, Miess-Tanneberg E, Blum NK, Benkel T, Chevigné A, Hoffmann C, Kolb P, Nikolaev V, Waldhoer M, Szpakowska M, Inoue A, Schulz S. Kostenis E, et al. Nat Commun. 2023 Nov 30;14(1):7867. doi: 10.1038/s41467-023-42849-4. Nat Commun. 2023. PMID: 38036502 Free PMC article. No abstract available.
Glucose-stimulated insulin secretion depends on FFA1 and Gq in neonatal mouse islets.
Lorza-Gil E, Kaiser G, Carlein C, Hoffmann MDA, König GM, Haug S, Prates Roma L, Rexen Ulven E, Ulven T, Kostenis E, Birkenfeld AL, Häring HU, Ullrich S, Gerst F. Lorza-Gil E, et al. Among authors: kostenis e. Diabetologia. 2023 Aug;66(8):1501-1515. doi: 10.1007/s00125-023-05932-5. Epub 2023 May 23. Diabetologia. 2023. PMID: 37217659 Free PMC article.
Giving ERK a jERK from the endosome.
Kostenis E, Bravo S, Gomeza J. Kostenis E, et al. Trends Pharmacol Sci. 2023 Mar;44(3):131-133. doi: 10.1016/j.tips.2022.12.004. Epub 2023 Jan 3. Trends Pharmacol Sci. 2023. PMID: 36604224
Author Correction: Selective optogenetic control of Gq signaling using human Neuropsin.
Wagdi A, Malan D, Sathyanarayanan U, Beauchamp JS, Vogt M, Zipf D, Beiert T, Mansuroglu B, Dusend V, Meininghaus M, Schneider L, Kalthof B, Wiegert JS, König GM, Kostenis E, Patejdl R, Sasse P, Bruegmann T. Wagdi A, et al. Among authors: kostenis e. Nat Commun. 2023 Jan 4;14(1):58. doi: 10.1038/s41467-022-35612-8. Nat Commun. 2023. PMID: 36599836 Free PMC article. No abstract available.
How Carvedilol activates β2-adrenoceptors.
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. Benkel T, et al. Among authors: kostenis e. Nat Commun. 2022 Nov 19;13(1):7109. doi: 10.1038/s41467-022-34765-w. Nat Commun. 2022. PMID: 36402762 Free PMC article.
Humanized zebrafish as a tractable tool for in vivo evaluation of pro-myelinating drugs.
Häberlein F, Mingardo E, Merten N, Schulze Köhling NK, Reinoß P, Simon K, Japp A, Nagarajan B, Schrage R, Pegurier C, Gillard M, Monk KR, Odermatt B, Kostenis E, Gomeza J. Häberlein F, et al. Among authors: kostenis e. Cell Chem Biol. 2022 Oct 20;29(10):1541-1555.e7. doi: 10.1016/j.chembiol.2022.08.007. Epub 2022 Sep 19. Cell Chem Biol. 2022. PMID: 36126653 Free article.
Induced antibodies directed to the angiotensin receptor type 1 provoke skin and lung inflammation, dermal fibrosis and act species overarching.
Yue X, Yin J, Wang X, Heidecke H, Hackel AM, Dong X, Kasper B, Wen L, Zhang L, Schulze-Forster K, Junker J, Grasshoff H, Müller A, Wallukat G, Schimke I, Zeiner J, Deckstein LM, Mertens N, Kerstein-Staehle A, Hundt JE, Kostenis E, Yu X, Riemekasten G, Petersen F. Yue X, et al. Among authors: kostenis e. Ann Rheum Dis. 2022 Aug 11;81(9):1281-1289. doi: 10.1136/annrheumdis-2021-222088. Ann Rheum Dis. 2022. PMID: 35595388 Free PMC article.
Selective optogenetic control of Gq signaling using human Neuropsin.
Wagdi A, Malan D, Sathyanarayanan U, Beauchamp JS, Vogt M, Zipf D, Beiert T, Mansuroglu B, Dusend V, Meininghaus M, Schneider L, Kalthof B, Wiegert JS, König GM, Kostenis E, Patejdl R, Sasse P, Bruegmann T. Wagdi A, et al. Among authors: kostenis e. Nat Commun. 2022 Apr 1;13(1):1765. doi: 10.1038/s41467-022-29265-w. Nat Commun. 2022. PMID: 35365606 Free PMC article.
Community guidelines for GPCR ligand bias: IUPHAR review 32.
Kolb P, Kenakin T, Alexander SPH, Bermudez M, Bohn LM, Breinholt CS, Bouvier M, Hill SJ, Kostenis E, Martemyanov KA, Neubig RR, Onaran HO, Rajagopal S, Roth BL, Selent J, Shukla AK, Sommer ME, Gloriam DE. Kolb P, et al. Among authors: kostenis e. Br J Pharmacol. 2022 Jul;179(14):3651-3674. doi: 10.1111/bph.15811. Epub 2022 Mar 27. Br J Pharmacol. 2022. PMID: 35106752 Free PMC article. Review.
Gq signaling in α cells is critical for maintaining euglycemia.
Liu L, Dattaroy D, Simpson KF, Barella LF, Cui Y, Xiong Y, Jin J, König GM, Kostenis E, Roman JC, Kaestner KH, Doliba NM, Wess J. Liu L, et al. Among authors: kostenis e. JCI Insight. 2021 Dec 22;6(24):e152852. doi: 10.1172/jci.insight.152852. JCI Insight. 2021. PMID: 34752420 Free PMC article.
Unraveling binding mechanism and kinetics of macrocyclic Gαq protein inhibitors.
Voss JH, Nagel J, Rafehi M, Guixà-González R, Malfacini D, Patt J, Kehraus S, Inoue A, König GM, Kostenis E, Deupi X, Namasivayam V, Müller CE. Voss JH, et al. Among authors: kostenis e. Pharmacol Res. 2021 Nov;173:105880. doi: 10.1016/j.phrs.2021.105880. Epub 2021 Sep 17. Pharmacol Res. 2021. PMID: 34506902
An experimental strategy to probe Gq contribution to signal transduction in living cells.
Patt J, Alenfelder J, Pfeil EM, Voss JH, Merten N, Eryilmaz F, Heycke N, Rick U, Inoue A, Kehraus S, Deupi X, Müller CE, König GM, Crüsemann M, Kostenis E. Patt J, et al. Among authors: kostenis e. J Biol Chem. 2021 Jan-Jun;296:100472. doi: 10.1016/j.jbc.2021.100472. Epub 2021 Feb 25. J Biol Chem. 2021. PMID: 33639168 Free PMC article.
Thioesterase-mediated side chain transesterification generates potent Gq signaling inhibitor FR900359.
Hermes C, Richarz R, Wirtz DA, Patt J, Hanke W, Kehraus S, Voß JH, Küppers J, Ohbayashi T, Namasivayam V, Alenfelder J, Inoue A, Mergaert P, Gütschow M, Müller CE, Kostenis E, König GM, Crüsemann M. Hermes C, et al. Among authors: kostenis e. Nat Commun. 2021 Jan 8;12(1):144. doi: 10.1038/s41467-020-20418-3. Nat Commun. 2021. PMID: 33420046 Free PMC article.
Heterotrimeric G Protein Subunit Gαq Is a Master Switch for Gβγ-Mediated Calcium Mobilization by Gi-Coupled GPCRs.
Pfeil EM, Brands J, Merten N, Vögtle T, Vescovo M, Rick U, Albrecht IM, Heycke N, Kawakami K, Ono Y, Ngako Kadji FM, Hiratsuka S, Aoki J, Häberlein F, Matthey M, Garg J, Hennen S, Jobin ML, Seier K, Calebiro D, Pfeifer A, Heinemann A, Wenzel D, König GM, Nieswandt B, Fleischmann BK, Inoue A, Simon K, Kostenis E. Pfeil EM, et al. Among authors: kostenis e. Mol Cell. 2020 Dec 17;80(6):940-954.e6. doi: 10.1016/j.molcel.2020.10.027. Epub 2020 Nov 16. Mol Cell. 2020. PMID: 33202251 Free article.
Ligand-Specific Allosteric Coupling Controls G-Protein-Coupled Receptor Signaling.
Holze J, Bermudez M, Pfeil EM, Kauk M, Bödefeld T, Irmen M, Matera C, Dallanoce C, De Amici M, Holzgrabe U, König GM, Tränkle C, Wolber G, Schrage R, Mohr K, Hoffmann C, Kostenis E, Bock A. Holze J, et al. Among authors: kostenis e. ACS Pharmacol Transl Sci. 2020 Sep 2;3(5):859-867. doi: 10.1021/acsptsci.0c00069. eCollection 2020 Oct 9. ACS Pharmacol Transl Sci. 2020. PMID: 33073186 Free PMC article.
Gq/11-dependent regulation of endosomal cAMP generation by parathyroid hormone class B GPCR.
White AD, Jean-Alphonse FG, Fang F, Peña KA, Liu S, König GM, Inoue A, Aslanoglou D, Gellman SH, Kostenis E, Xiao K, Vilardaga JP. White AD, et al. Among authors: kostenis e. Proc Natl Acad Sci U S A. 2020 Mar 31;117(13):7455-7460. doi: 10.1073/pnas.1918158117. Epub 2020 Mar 17. Proc Natl Acad Sci U S A. 2020. PMID: 32184323 Free PMC article.
BIM-46174 fragments as potential ligands of G proteins.
Küppers J, Benkel T, Annala S, Schnakenburg G, Kostenis E, Gütschow M. Küppers J, et al. Among authors: kostenis e. Medchemcomm. 2019 Aug 21;10(10):1838-1843. doi: 10.1039/c9md00269c. eCollection 2019 Oct 1. Medchemcomm. 2019. PMID: 32180917 Free PMC article.
Heterotrimeric Gq proteins as therapeutic targets?
Kostenis E, Pfeil EM, Annala S. Kostenis E, et al. J Biol Chem. 2020 Apr 17;295(16):5206-5215. doi: 10.1074/jbc.REV119.007061. Epub 2020 Mar 2. J Biol Chem. 2020. PMID: 32122969 Free PMC article. Review.
Impaired endothelium-mediated cerebrovascular reactivity promotes anxiety and respiration disorders in mice.
Wenzel J, Hansen CE, Bettoni C, Vogt MA, Lembrich B, Natsagdorj R, Huber G, Brands J, Schmidt K, Assmann JC, Stölting I, Saar K, Sedlacik J, Fiehler J, Ludewig P, Wegmann M, Feller N, Richter M, Müller-Fielitz H, Walther T, König GM, Kostenis E, Raasch W, Hübner N, Gass P, Offermanns S, de Wit C, Wagner CA, Schwaninger M. Wenzel J, et al. Among authors: kostenis e. Proc Natl Acad Sci U S A. 2020 Jan 21;117(3):1753-1761. doi: 10.1073/pnas.1907467117. Epub 2020 Jan 2. Proc Natl Acad Sci U S A. 2020. PMID: 31896584 Free PMC article.
Direct targeting of Gαq and Gα11 oncoproteins in cancer cells.
Annala S, Feng X, Shridhar N, Eryilmaz F, Patt J, Yang J, Pfeil EM, Cervantes-Villagrana RD, Inoue A, Häberlein F, Slodczyk T, Reher R, Kehraus S, Monteleone S, Schrage R, Heycke N, Rick U, Engel S, Pfeifer A, Kolb P, König G, Bünemann M, Tüting T, Vázquez-Prado J, Gutkind JS, Gaffal E, Kostenis E. Annala S, et al. Among authors: kostenis e. Sci Signal. 2019 Mar 19;12(573):eaau5948. doi: 10.1126/scisignal.aau5948. Sci Signal. 2019. PMID: 30890659
A Platform of Synthetic Lethal Gene Interaction Networks Reveals that the GNAQ Uveal Melanoma Oncogene Controls the Hippo Pathway through FAK.
Feng X, Arang N, Rigiracciolo DC, Lee JS, Yeerna H, Wang Z, Lubrano S, Kishore A, Pachter JA, König GM, Maggiolini M, Kostenis E, Schlaepfer DD, Tamayo P, Chen Q, Ruppin E, Gutkind JS. Feng X, et al. Among authors: kostenis e. Cancer Cell. 2019 Mar 18;35(3):457-472.e5. doi: 10.1016/j.ccell.2019.01.009. Epub 2019 Feb 14. Cancer Cell. 2019. PMID: 30773340 Free PMC article.
Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity.
Malfacini D, Patt J, Annala S, Harpsøe K, Eryilmaz F, Reher R, Crüsemann M, Hanke W, Zhang H, Tietze D, Gloriam DE, Bräuner-Osborne H, Strømgaard K, König GM, Inoue A, Gomeza J, Kostenis E. Malfacini D, et al. Among authors: kostenis e. J Biol Chem. 2019 Apr 12;294(15):5747-5758. doi: 10.1074/jbc.RA118.007250. Epub 2019 Feb 11. J Biol Chem. 2019. PMID: 30745359 Free PMC article.
Label-Free Whole Cell Biosensing for High-Throughput Discovery of Activators and Inhibitors Targeting G Protein-Activated Inwardly Rectifying Potassium Channels.
Krebs KM, Pfeil EM, Simon K, Grundmann M, Häberlein F, Bautista-Aguilera OM, Gütschow M, Weaver CD, Fleischmann BK, Kostenis E. Krebs KM, et al. Among authors: kostenis e. ACS Omega. 2018 Nov 30;3(11):14814-14823. doi: 10.1021/acsomega.8b02254. Epub 2018 Nov 5. ACS Omega. 2018. PMID: 30555990 Free PMC article.
Gβγ signaling to the chemotactic effector P-REX1 and mammalian cell migration is directly regulated by Gαq and Gα13 proteins.
Cervantes-Villagrana RD, Adame-García SR, García-Jiménez I, Color-Aparicio VM, Beltrán-Navarro YM, König GM, Kostenis E, Reyes-Cruz G, Gutkind JS, Vázquez-Prado J. Cervantes-Villagrana RD, et al. Among authors: kostenis e. J Biol Chem. 2019 Jan 11;294(2):531-546. doi: 10.1074/jbc.RA118.006254. Epub 2018 Nov 16. J Biol Chem. 2019. PMID: 30446620 Free PMC article.
NOP receptor pharmacological profile - A dynamic mass redistribution study.
Malfacini D, Simon K, Trapella C, Guerrini R, Zaveri NT, Kostenis E, Calo' G. Malfacini D, et al. Among authors: kostenis e. PLoS One. 2018 Aug 30;13(8):e0203021. doi: 10.1371/journal.pone.0203021. eCollection 2018. PLoS One. 2018. PMID: 30161182 Free PMC article.
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
Baqi Y, Pillaiyar T, Abdelrahman A, Kaufmann O, Alshaibani S, Rafehi M, Ghasimi S, Akkari R, Ritter K, Simon K, Spinrath A, Kostenis E, Zhao Q, Köse M, Namasivayam V, Müller CE. Baqi Y, et al. Among authors: kostenis e. J Med Chem. 2018 Sep 27;61(18):8136-8154. doi: 10.1021/acs.jmedchem.7b01768. Epub 2018 Sep 5. J Med Chem. 2018. PMID: 30048589
Arrestins as rheostats of GPCR signalling.
Gutkind JS, Kostenis E. Gutkind JS, et al. Among authors: kostenis e. Nat Rev Mol Cell Biol. 2018 Oct;19(10):615-616. doi: 10.1038/s41580-018-0041-y. Nat Rev Mol Cell Biol. 2018. PMID: 30026541 No abstract available.
Deciphering Specificity Determinants for FR900359-Derived Gq α Inhibitors Based on Computational and Structure-Activity Studies.
Reher R, Kühl T, Annala S, Benkel T, Kaufmann D, Nubbemeyer B, Odhiambo JP, Heimer P, Bäuml CA, Kehraus S, Crüsemann M, Kostenis E, Tietze D, König GM, Imhof D. Reher R, et al. Among authors: kostenis e. ChemMedChem. 2018 Aug 20;13(16):1634-1643. doi: 10.1002/cmdc.201800304. Epub 2018 Jul 3. ChemMedChem. 2018. PMID: 29873888
Repurposing HAMI3379 to Block GPR17 and Promote Rodent and Human Oligodendrocyte Differentiation.
Merten N, Fischer J, Simon K, Zhang L, Schröder R, Peters L, Letombe AG, Hennen S, Schrage R, Bödefeld T, Vermeiren C, Gillard M, Mohr K, Lu QR, Brüstle O, Gomeza J, Kostenis E. Merten N, et al. Among authors: kostenis e. Cell Chem Biol. 2018 Jun 21;25(6):775-786.e5. doi: 10.1016/j.chembiol.2018.03.012. Epub 2018 Apr 26. Cell Chem Biol. 2018. PMID: 29706593 Free PMC article.
Lack of beta-arrestin signaling in the absence of active G proteins.
Grundmann M, Merten N, Malfacini D, Inoue A, Preis P, Simon K, Rüttiger N, Ziegler N, Benkel T, Schmitt NK, Ishida S, Müller I, Reher R, Kawakami K, Inoue A, Rick U, Kühl T, Imhof D, Aoki J, König GM, Hoffmann C, Gomeza J, Wess J, Kostenis E. Grundmann M, et al. Among authors: kostenis e. Nat Commun. 2018 Jan 23;9(1):341. doi: 10.1038/s41467-017-02661-3. Nat Commun. 2018. PMID: 29362459 Free PMC article.
Heterologous Expression, Biosynthetic Studies, and Ecological Function of the Selective Gq-Signaling Inhibitor FR900359.
Crüsemann M, Reher R, Schamari I, Brachmann AO, Ohbayashi T, Kuschak M, Malfacini D, Seidinger A, Pinto-Carbó M, Richarz R, Reuter T, Kehraus S, Hallab A, Attwood M, Schiöth HB, Mergaert P, Kikuchi Y, Schäberle TF, Kostenis E, Wenzel D, Müller CE, Piel J, Carlier A, Eberl L, König GM. Crüsemann M, et al. Among authors: kostenis e. Angew Chem Int Ed Engl. 2018 Jan 15;57(3):836-840. doi: 10.1002/anie.201707996. Epub 2017 Dec 20. Angew Chem Int Ed Engl. 2018. PMID: 29194875
Temporal Bias: Time-Encoded Dynamic GPCR Signaling.
Grundmann M, Kostenis E. Grundmann M, et al. Among authors: kostenis e. Trends Pharmacol Sci. 2017 Dec;38(12):1110-1124. doi: 10.1016/j.tips.2017.09.004. Epub 2017 Oct 23. Trends Pharmacol Sci. 2017. PMID: 29074251 Review.
The neuropeptide neuromedin U stimulates innate lymphoid cells and type 2 inflammation.
Klose CSN, Mahlakõiv T, Moeller JB, Rankin LC, Flamar AL, Kabata H, Monticelli LA, Moriyama S, Putzel GG, Rakhilin N, Shen X, Kostenis E, König GM, Senda T, Carpenter D, Farber DL, Artis D. Klose CSN, et al. Among authors: kostenis e. Nature. 2017 Sep 14;549(7671):282-286. doi: 10.1038/nature23676. Epub 2017 Sep 6. Nature. 2017. PMID: 28869965 Free PMC article.
A New Molecular Mechanism To Engineer Protean Agonism at a G Protein-Coupled Receptor.
De Min A, Matera C, Bock A, Holze J, Kloeckner J, Muth M, Traenkle C, De Amici M, Kenakin T, Holzgrabe U, Dallanoce C, Kostenis E, Mohr K, Schrage R. De Min A, et al. Among authors: kostenis e. Mol Pharmacol. 2017 Apr;91(4):348-356. doi: 10.1124/mol.116.107276. Epub 2017 Feb 6. Mol Pharmacol. 2017. PMID: 28167741
Engineered Context-Sensitive Agonism: Tissue-Selective Drug Signaling through a G Protein-Coupled Receptor.
Seemann WK, Wenzel D, Schrage R, Etscheid J, Bödefeld T, Bartol A, Warnken M, Sasse P, Klöckner J, Holzgrabe U, DeAmici M, Schlicker E, Racké K, Kostenis E, Meyer R, Fleischmann BK, Mohr K. Seemann WK, et al. Among authors: kostenis e. J Pharmacol Exp Ther. 2017 Feb;360(2):289-299. doi: 10.1124/jpet.116.237149. Epub 2016 Nov 15. J Pharmacol Exp Ther. 2017. PMID: 28082514
Functional selectivity and dualsteric/bitopic GPCR targeting.
Schrage R, Kostenis E. Schrage R, et al. Among authors: kostenis e. Curr Opin Pharmacol. 2017 Feb;32:85-90. doi: 10.1016/j.coph.2016.12.001. Epub 2016 Dec 24. Curr Opin Pharmacol. 2017. PMID: 28027487 Review.
WNT Stimulation Dissociates a Frizzled 4 Inactive-State Complex with Gα12/13.
Arthofer E, Hot B, Petersen J, Strakova K, Jäger S, Grundmann M, Kostenis E, Gutkind JS, Schulte G. Arthofer E, et al. Among authors: kostenis e. Mol Pharmacol. 2016 Oct;90(4):447-59. doi: 10.1124/mol.116.104919. Epub 2016 Jul 25. Mol Pharmacol. 2016. PMID: 27458145 Free PMC article.
A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias.
Bolognini D, Moss CE, Nilsson K, Petersson AU, Donnelly I, Sergeev E, König GM, Kostenis E, Kurowska-Stolarska M, Miller A, Dekker N, Tobin AB, Milligan G. Bolognini D, et al. Among authors: kostenis e. J Biol Chem. 2016 Sep 2;291(36):18915-31. doi: 10.1074/jbc.M116.736157. Epub 2016 Jul 5. J Biol Chem. 2016. PMID: 27385588 Free PMC article.
The Adhesion G Protein-Coupled Receptor GPR56/ADGRG1 Is an Inhibitory Receptor on Human NK Cells.
Chang GW, Hsiao CC, Peng YM, Vieira Braga FA, Kragten NA, Remmerswaal EB, van de Garde MD, Straussberg R, König GM, Kostenis E, Knäuper V, Meyaard L, van Lier RA, van Gisbergen KP, Lin HH, Hamann J. Chang GW, et al. Among authors: kostenis e. Cell Rep. 2016 May 24;15(8):1757-70. doi: 10.1016/j.celrep.2016.04.053. Epub 2016 May 12. Cell Rep. 2016. PMID: 27184850 Free article.
Mapping physiological G protein-coupled receptor signaling pathways reveals a role for receptor phosphorylation in airway contraction.
Bradley SJ, Wiegman CH, Iglesias MM, Kong KC, Butcher AJ, Plouffe B, Goupil E, Bourgognon JM, Macedo-Hatch T, LeGouill C, Russell K, Laporte SA, König GM, Kostenis E, Bouvier M, Chung KF, Amrani Y, Tobin AB. Bradley SJ, et al. Among authors: kostenis e. Proc Natl Acad Sci U S A. 2016 Apr 19;113(16):4524-9. doi: 10.1073/pnas.1521706113. Epub 2016 Apr 8. Proc Natl Acad Sci U S A. 2016. PMID: 27071102 Free PMC article.
The Gq signalling pathway inhibits brown and beige adipose tissue.
Klepac K, Kilić A, Gnad T, Brown LM, Herrmann B, Wilderman A, Balkow A, Glöde A, Simon K, Lidell ME, Betz MJ, Enerbäck S, Wess J, Freichel M, Blüher M, König G, Kostenis E, Insel PA, Pfeifer A. Klepac K, et al. Among authors: kostenis e. Nat Commun. 2016 Mar 9;7:10895. doi: 10.1038/ncomms10895. Nat Commun. 2016. PMID: 26955961 Free PMC article.
Holistic Methods for the Analysis of cNMP Effects.
Grundmann M, Kostenis E. Grundmann M, et al. Among authors: kostenis e. Handb Exp Pharmacol. 2017;238:339-357. doi: 10.1007/164_2015_42. Handb Exp Pharmacol. 2017. PMID: 26721676 Review.
The experimental power of FR900359 to study Gq-regulated biological processes.
Schrage R, Schmitz AL, Gaffal E, Annala S, Kehraus S, Wenzel D, Büllesbach KM, Bald T, Inoue A, Shinjo Y, Galandrin S, Shridhar N, Hesse M, Grundmann M, Merten N, Charpentier TH, Martz M, Butcher AJ, Slodczyk T, Armando S, Effern M, Namkung Y, Jenkins L, Horn V, Stößel A, Dargatz H, Tietze D, Imhof D, Galés C, Drewke C, Müller CE, Hölzel M, Milligan G, Tobin AB, Gomeza J, Dohlman HG, Sondek J, Harden TK, Bouvier M, Laporte SA, Aoki J, Fleischmann BK, Mohr K, König GM, Tüting T, Kostenis E. Schrage R, et al. Among authors: kostenis e. Nat Commun. 2015 Dec 14;6:10156. doi: 10.1038/ncomms10156. Nat Commun. 2015. PMID: 26658454 Free PMC article.
N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
Blöcher R, Lamers C, Wittmann SK, Merk D, Hartmann M, Weizel L, Diehl O, Brüggerhoff A, Boß M, Kaiser A, Schader T, Göbel T, Grundmann M, Angioni C, Heering J, Geisslinger G, Wurglics M, Kostenis E, Brüne B, Steinhilber D, Schubert-Zsilavecz M, Kahnt AS, Proschak E. Blöcher R, et al. Among authors: kostenis e. J Med Chem. 2016 Jan 14;59(1):61-81. doi: 10.1021/acs.jmedchem.5b01239. Epub 2015 Dec 25. J Med Chem. 2016. PMID: 26595749
Superagonism at G protein-coupled receptors and beyond.
Schrage R, De Min A, Hochheiser K, Kostenis E, Mohr K. Schrage R, et al. Among authors: kostenis e. Br J Pharmacol. 2016 Oct;173(20):3018-27. doi: 10.1111/bph.13278. Epub 2015 Oct 24. Br J Pharmacol. 2016. PMID: 26276510 Free PMC article. Review.
Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases.
Christiansen E, Watterson KR, Stocker CJ, Sokol E, Jenkins L, Simon K, Grundmann M, Petersen RK, Wargent ET, Hudson BD, Kostenis E, Ejsing CS, Cawthorne MA, Milligan G, Ulven T. Christiansen E, et al. Among authors: kostenis e. Br J Nutr. 2015 Jun 14;113(11):1677-88. doi: 10.1017/S000711451500118X. Epub 2015 Apr 28. Br J Nutr. 2015. PMID: 25916176 Free article.
Mice Lacking Free Fatty Acid Receptor 1 (GPR40/FFAR1) are Protected Against Conjugated Linoleic Acid-Induced Fatty Liver but Develop Inflammation and Insulin Resistance in the Brain.
Sartorius T, Drescher A, Panse M, Lastovicka P, Peter A, Weigert C, Kostenis E, Ullrich S, Häring HU. Sartorius T, et al. Among authors: kostenis e. Cell Physiol Biochem. 2015;35(6):2272-84. doi: 10.1159/000374031. Epub 2015 Apr 13. Cell Physiol Biochem. 2015. PMID: 25895678 Free article.
Label-free biosensor assays in GPCR screening.
Grundmann M, Kostenis E. Grundmann M, et al. Among authors: kostenis e. Methods Mol Biol. 2015;1272:199-213. doi: 10.1007/978-1-4939-2336-6_14. Methods Mol Biol. 2015. PMID: 25563186
cNMP-AMs mimic and dissect bacterial nucleotidyl cyclase toxin effects.
Beckert U, Grundmann M, Wolter S, Schwede F, Rehmann H, Kaever V, Kostenis E, Seifert R. Beckert U, et al. Among authors: kostenis e. Biochem Biophys Res Commun. 2014 Sep 5;451(4):497-502. doi: 10.1016/j.bbrc.2014.07.134. Epub 2014 Aug 7. Biochem Biophys Res Commun. 2014. PMID: 25108158
Heteromerization of GPR55 and cannabinoid CB2 receptors modulates signalling.
Balenga NA, Martínez-Pinilla E, Kargl J, Schröder R, Peinhaupt M, Platzer W, Bálint Z, Zamarbide M, Dopeso-Reyes IG, Ricobaraza A, Pérez-Ortiz JM, Kostenis E, Waldhoer M, Heinemann A, Franco R. Balenga NA, et al. Among authors: kostenis e. Br J Pharmacol. 2014 Dec;171(23):5387-406. doi: 10.1111/bph.12850. Epub 2014 Sep 5. Br J Pharmacol. 2014. PMID: 25048571 Free PMC article.
A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformation.
Schmitz AL, Schrage R, Gaffal E, Charpentier TH, Wiest J, Hiltensperger G, Morschel J, Hennen S, Häußler D, Horn V, Wenzel D, Grundmann M, Büllesbach KM, Schröder R, Brewitz HH, Schmidt J, Gomeza J, Galés C, Fleischmann BK, Tüting T, Imhof D, Tietze D, Gütschow M, Holzgrabe U, Sondek J, Harden TK, Mohr K, Kostenis E. Schmitz AL, et al. Among authors: kostenis e. Chem Biol. 2014 Jul 17;21(7):890-902. doi: 10.1016/j.chembiol.2014.06.003. Chem Biol. 2014. PMID: 25036778 Free PMC article.
Allostery: A GPCR's back door.
Mohr K, Kostenis E. Mohr K, et al. Among authors: kostenis e. Nat Chem Biol. 2014 Aug;10(8):609-10. doi: 10.1038/nchembio.1583. Nat Chem Biol. 2014. PMID: 25036308 No abstract available.
Dynamic ligand binding dictates partial agonism at a G protein-coupled receptor.
Bock A, Chirinda B, Krebs F, Messerer R, Bätz J, Muth M, Dallanoce C, Klingenthal D, Tränkle C, Hoffmann C, De Amici M, Holzgrabe U, Kostenis E, Mohr K. Bock A, et al. Among authors: kostenis e. Nat Chem Biol. 2014 Jan;10(1):18-20. doi: 10.1038/nchembio.1384. Epub 2013 Nov 10. Nat Chem Biol. 2014. PMID: 24212135
Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist.
Hennen S, Wang H, Peters L, Merten N, Simon K, Spinrath A, Blättermann S, Akkari R, Schrage R, Schröder R, Schulz D, Vermeiren C, Zimmermann K, Kehraus S, Drewke C, Pfeifer A, König GM, Mohr K, Gillard M, Müller CE, Lu QR, Gomeza J, Kostenis E. Hennen S, et al. Among authors: kostenis e. Sci Signal. 2013 Oct 22;6(298):ra93. doi: 10.1126/scisignal.2004350. Sci Signal. 2013. PMID: 24150254 Free PMC article.
Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
Christiansen E, Hansen SV, Urban C, Hudson BD, Wargent ET, Grundmann M, Jenkins L, Zaibi M, Stocker CJ, Ullrich S, Kostenis E, Kassack MU, Milligan G, Cawthorne MA, Ulven T. Christiansen E, et al. Among authors: kostenis e. ACS Med Chem Lett. 2013 May 9;4(5):441-445. doi: 10.1021/ml4000673. Epub 2013 Apr 8. ACS Med Chem Lett. 2013. PMID: 23687558 Free PMC article.
Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability.
Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schmidt J, Hansen SV, Hudson BD, Zaibi M, Markussen SB, Hagesaether E, Milligan G, Cawthorne MA, Kostenis E, Kassack MU, Ulven T. Christiansen E, et al. Among authors: kostenis e. J Med Chem. 2013 Feb 14;56(3):982-92. doi: 10.1021/jm301470a. Epub 2013 Jan 22. J Med Chem. 2013. PMID: 23294321
Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor.
Schrage R, Seemann WK, Klöckner J, Dallanoce C, Racké K, Kostenis E, De Amici M, Holzgrabe U, Mohr K. Schrage R, et al. Among authors: kostenis e. Br J Pharmacol. 2013 May;169(2):357-70. doi: 10.1111/bph.12003. Br J Pharmacol. 2013. PMID: 23062057 Free PMC article.
The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling.
Bock A, Merten N, Schrage R, Dallanoce C, Bätz J, Klöckner J, Schmitz J, Matera C, Simon K, Kebig A, Peters L, Müller A, Schrobang-Ley J, Tränkle C, Hoffmann C, De Amici M, Holzgrabe U, Kostenis E, Mohr K. Bock A, et al. Among authors: kostenis e. Nat Commun. 2012;3:1044. doi: 10.1038/ncomms2028. Nat Commun. 2012. PMID: 22948826 Free PMC article.
A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer.
Blättermann S, Peters L, Ottersbach PA, Bock A, Konya V, Weaver CD, Gonzalez A, Schröder R, Tyagi R, Luschnig P, Gäb J, Hennen S, Ulven T, Pardo L, Mohr K, Gütschow M, Heinemann A, Kostenis E. Blättermann S, et al. Among authors: kostenis e. Nat Chem Biol. 2012 Jul;8(7):631-8. doi: 10.1038/nchembio.962. Epub 2012 May 27. Nat Chem Biol. 2012. PMID: 22634634
Signaling pathways: Purinosomes under GPCR control.
Mohr K, Kostenis E. Mohr K, et al. Among authors: kostenis e. Nat Chem Biol. 2011 Nov 15;7(12):860-1. doi: 10.1038/nchembio.716. Nat Chem Biol. 2011. PMID: 22086285 No abstract available.
GPR55 regulates cannabinoid 2 receptor-mediated responses in human neutrophils.
Balenga NA, Aflaki E, Kargl J, Platzer W, Schröder R, Blättermann S, Kostenis E, Brown AJ, Heinemann A, Waldhoer M. Balenga NA, et al. Among authors: kostenis e. Cell Res. 2011 Oct;21(10):1452-69. doi: 10.1038/cr.2011.60. Epub 2011 Apr 5. Cell Res. 2011. PMID: 21467997 Free PMC article.
Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3.
Schmidt J, Smith NJ, Christiansen E, Tikhonova IG, Grundmann M, Hudson BD, Ward RJ, Drewke C, Milligan G, Kostenis E, Ulven T. Schmidt J, et al. Among authors: kostenis e. J Biol Chem. 2011 Mar 25;286(12):10628-40. doi: 10.1074/jbc.M110.210872. Epub 2011 Jan 10. J Biol Chem. 2011. PMID: 21220428 Free PMC article.
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.
Christiansen E, Due-Hansen ME, Urban C, Merten N, Pfleiderer M, Karlsen KK, Rasmussen SS, Steensgaard M, Hamacher A, Schmidt J, Drewke C, Petersen RK, Kristiansen K, Ullrich S, Kostenis E, Kassack MU, Ulven T. Christiansen E, et al. Among authors: kostenis e. ACS Med Chem Lett. 2010 Jul 2;1(7):345-9. doi: 10.1021/ml100106c. eCollection 2010 Oct 14. ACS Med Chem Lett. 2010. PMID: 24900217 Free PMC article.
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements.
Schröder R, Janssen N, Schmidt J, Kebig A, Merten N, Hennen S, Müller A, Blättermann S, Mohr-Andrä M, Zahn S, Wenzel J, Smith NJ, Gomeza J, Drewke C, Milligan G, Mohr K, Kostenis E. Schröder R, et al. Among authors: kostenis e. Nat Biotechnol. 2010 Sep;28(9):943-9. doi: 10.1038/nbt.1671. Epub 2010 Aug 15. Nat Biotechnol. 2010. PMID: 20711173 Free article.
GPR55 ligands promote receptor coupling to multiple signalling pathways.
Henstridge CM, Balenga NA, Schröder R, Kargl JK, Platzer W, Martini L, Arthur S, Penman J, Whistler JL, Kostenis E, Waldhoer M, Irving AJ. Henstridge CM, et al. Among authors: kostenis e. Br J Pharmacol. 2010 Jun;160(3):604-14. doi: 10.1111/j.1476-5381.2009.00625.x. Epub 2010 Feb 5. Br J Pharmacol. 2010. PMID: 20136841 Free PMC article.
Rational design of dualsteric GPCR ligands: quests and promise.
Mohr K, Tränkle C, Kostenis E, Barocelli E, De Amici M, Holzgrabe U. Mohr K, et al. Among authors: kostenis e. Br J Pharmacol. 2010 Mar;159(5):997-1008. doi: 10.1111/j.1476-5381.2009.00601.x. Epub 2010 Feb 5. Br J Pharmacol. 2010. PMID: 20136835 Free PMC article. Review.
The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai and downstream signaling cascade activation.
Schröder R, Merten N, Mathiesen JM, Martini L, Kruljac-Letunic A, Krop F, Blaukat A, Fang Y, Tran E, Ulven T, Drewke C, Whistler J, Pardo L, Gomeza J, Kostenis E. Schröder R, et al. Among authors: kostenis e. J Biol Chem. 2009 Jan 9;284(2):1324-36. doi: 10.1074/jbc.M806867200. Epub 2008 Nov 14. J Biol Chem. 2009. PMID: 19010788 Free article.
Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity.
Antony J, Kellershohn K, Mohr-Andrä M, Kebig A, Prilla S, Muth M, Heller E, Disingrini T, Dallanoce C, Bertoni S, Schrobang J, Tränkle C, Kostenis E, Christopoulos A, Höltje HD, Barocelli E, De Amici M, Holzgrabe U, Mohr K. Antony J, et al. Among authors: kostenis e. FASEB J. 2009 Feb;23(2):442-50. doi: 10.1096/fj.08-114751. Epub 2008 Oct 8. FASEB J. 2009. PMID: 18842964
The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking.
Schratl P, Royer JF, Kostenis E, Ulven T, Sturm EM, Waldhoer M, Hoefler G, Schuligoi R, Lippe IT, Peskar BA, Heinemann A. Schratl P, et al. Among authors: kostenis e. J Immunol. 2007 Oct 1;179(7):4792-9. doi: 10.4049/jimmunol.179.7.4792. J Immunol. 2007. PMID: 17878378
Heterotrimeric G-proteins: a short history.
Milligan G, Kostenis E. Milligan G, et al. Among authors: kostenis e. Br J Pharmacol. 2006 Jan;147 Suppl 1(Suppl 1):S46-55. doi: 10.1038/sj.bjp.0706405. Br J Pharmacol. 2006. PMID: 16402120 Free PMC article. Review.
A highly conserved glycine within linker I and the extreme C terminus of G protein alpha subunits interact cooperatively in switching G protein-coupled receptor-to-effector specificity.
Kostenis E, Martini L, Ellis J, Waldhoer M, Heydorn A, Rosenkilde MM, Norregaard PK, Jorgensen R, Whistler JL, Milligan G. Kostenis E, et al. J Pharmacol Exp Ther. 2005 Apr;313(1):78-87. doi: 10.1124/jpet.104.080424. Epub 2004 Dec 22. J Pharmacol Exp Ther. 2005. PMID: 15615862
Urotensin II causes fatal circulatory collapse in anesthesized monkeys in vivo: a "vasoconstrictor" with a unique hemodynamic profile.
Zhu YZ, Wang ZJ, Zhu YC, Zhang L, Oakley RM, Chung CW, Lim KW, Lee HS, Ozoux ML, Linz W, Böhm M, Kostenis E. Zhu YZ, et al. Among authors: kostenis e. Am J Physiol Heart Circ Physiol. 2004 Mar;286(3):H830-6. doi: 10.1152/ajpheart.00406.2003. Epub 2003 Nov 13. Am J Physiol Heart Circ Physiol. 2004. PMID: 14615276 Free article.
Modulation of myocardial contractility by lysophosphatidic acid (LPA).
Cremers B, Flesch M, Kostenis E, Maack C, Niedernberg A, Stoff A, Südkamp M, Wendler O, Böhm M. Cremers B, et al. Among authors: kostenis e. J Mol Cell Cardiol. 2003 Jan;35(1):71-80. doi: 10.1016/s0022-2828(02)00279-1. J Mol Cell Cardiol. 2003. PMID: 12623301
A new ligand for the urotensin II receptor.
Camarda V, Guerrini R, Kostenis E, Rizzi A, Calò G, Hattenberger A, Zucchini M, Salvadori S, Regoli D. Camarda V, et al. Among authors: kostenis e. Br J Pharmacol. 2002 Oct;137(3):311-4. doi: 10.1038/sj.bjp.0704895. Br J Pharmacol. 2002. PMID: 12237249 Free PMC article.
Single amino acid substitutions and deletions that alter the G protein coupling properties of the V2 vasopressin receptor identified in yeast by receptor random mutagenesis.
Erlenbach I, Kostenis E, Schmidt C, Serradeil-Le Gal C, Raufaste D, Dumont ME, Pausch MH, Wess J. Erlenbach I, et al. Among authors: kostenis e. J Biol Chem. 2001 Aug 3;276(31):29382-92. doi: 10.1074/jbc.M103203200. Epub 2001 May 25. J Biol Chem. 2001. PMID: 11375990 Free article.
Molecular aspects of vasopressin receptor function.
Schöneberg T, Kostenis E, Liu J, Gudermann T, Wess J. Schöneberg T, et al. Among authors: kostenis e. Adv Exp Med Biol. 1998;449:347-58. doi: 10.1007/978-1-4615-4871-3_44. Adv Exp Med Biol. 1998. PMID: 10026824
[Omeprazole].
Kostenis E, Mohr K. Kostenis E, et al. Dtsch Med Wochenschr. 1994 Aug 26;119(34-35):1173-4. doi: 10.1055/s-0029-1235090. Dtsch Med Wochenschr. 1994. PMID: 8076506 German. No abstract available.