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Items: 1 to 50 of 147

1.

FZD5 is a Gαq-coupled receptor that exhibits the functional hallmarks of prototypical GPCRs.

Wright SC, Cañizal MCA, Benkel T, Simon K, Le Gouill C, Matricon P, Namkung Y, Lukasheva V, König GM, Laporte SA, Carlsson J, Kostenis E, Bouvier M, Schulte G, Hoffmann C.

Sci Signal. 2018 Dec 4;11(559). pii: eaar5536. doi: 10.1126/scisignal.aar5536.

PMID:
30514810
2.

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-Jimenez I, Color-Aparicio VM, Beltran-Navarro YM, König GM, Kostenis E, Reyes-Cruz G, Gutkind JS, Vázquez-Prado J.

J Biol Chem. 2018 Nov 16. pii: jbc.RA118.006254. doi: 10.1074/jbc.RA118.006254. [Epub ahead of print]

3.

Pro-Angiogenic Effects of Latent Heparanase and Thrombin Receptor-Mediated Pathways-Do They Share a Common Ground in Melanoma Cells?

Hoß SG, Grundmann M, Benkel T, Gockel L, Schwarz S, Kostenis E, Schlesinger M, Ilan N, Vlodavsky I, Bendas G.

Thromb Haemost. 2018 Oct;118(10):1803-1814. doi: 10.1055/s-0038-1669922. Epub 2018 Sep 20.

PMID:
30235481
4.

RXFP1 Receptor Activation by Relaxin-2 Induces Vascular Relaxation in Mice via a Gαi2-Protein/PI3Kß/γ/Nitric Oxide-Coupled Pathway.

Lian X, Beer-Hammer S, König GM, Kostenis E, Nürnberg B, Gollasch M.

Front Physiol. 2018 Sep 4;9:1234. doi: 10.3389/fphys.2018.01234. eCollection 2018.

5.

NOP receptor pharmacological profile - A dynamic mass redistribution study.

Malfacini D, Simon K, Trapella C, Guerrini R, Zaveri NT, Kostenis E, Calo' G.

PLoS One. 2018 Aug 30;13(8):e0203021. doi: 10.1371/journal.pone.0203021. eCollection 2018.

6.

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.

J Med Chem. 2018 Sep 27;61(18):8136-8154. doi: 10.1021/acs.jmedchem.7b01768. Epub 2018 Sep 5.

PMID:
30048589
7.

Arrestins as rheostats of GPCR signalling.

Gutkind JS, Kostenis E.

Nat Rev Mol Cell Biol. 2018 Oct;19(10):615-616. doi: 10.1038/s41580-018-0041-y. No abstract available.

PMID:
30026541
8.

Applying Molecular Networking for the Detection of Natural Sources and Analogues of the Selective Gq Protein Inhibitor FR900359.

Reher R, Kuschak M, Heycke N, Annala S, Kehraus S, Dai HF, Müller CE, Kostenis E, König GM, Crüsemann M.

J Nat Prod. 2018 Jul 27;81(7):1628-1635. doi: 10.1021/acs.jnatprod.8b00222. Epub 2018 Jun 26.

PMID:
29943987
9.

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.

ChemMedChem. 2018 Aug 20;13(16):1634-1643. doi: 10.1002/cmdc.201800304. Epub 2018 Jul 3.

PMID:
29873888
10.

5-HT2A receptor-dependent phosphorylation of mGlu2 receptor at Serine 843 promotes mGlu2 receptor-operated Gi/o signaling.

Murat S, Bigot M, Chapron J, König GM, Kostenis E, Battaglia G, Nicoletti F, Bourinet E, Bockaert J, Marin P, Vandermoere F.

Mol Psychiatry. 2018 Jun 1. doi: 10.1038/s41380-018-0069-6. [Epub ahead of print]

PMID:
29858599
11.

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.

Cell Chem Biol. 2018 Jun 21;25(6):775-786.e5. doi: 10.1016/j.chembiol.2018.03.012. Epub 2018 Apr 26.

PMID:
29706593
12.

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.

Nat Commun. 2018 Jan 23;9(1):341. doi: 10.1038/s41467-017-02661-3.

13.

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.

Angew Chem Int Ed Engl. 2018 Jan 15;57(3):836-840. doi: 10.1002/anie.201707996. Epub 2017 Dec 20.

PMID:
29194875
14.

Bruton's tyrosine kinase and RAC1 promote cell survival in MLL-rearranged acute myeloid leukemia.

Nimmagadda SC, Frey S, Edelmann B, Hellmich C, Zaitseva L, König GM, Kostenis E, Bowles KM, Fischer T.

Leukemia. 2018 Mar;32(3):846-849. doi: 10.1038/leu.2017.324. Epub 2017 Nov 7. No abstract available.

15.

Temporal Bias: Time-Encoded Dynamic GPCR Signaling.

Grundmann M, Kostenis E.

Trends Pharmacol Sci. 2017 Dec;38(12):1110-1124. doi: 10.1016/j.tips.2017.09.004. Epub 2017 Oct 23. Review.

PMID:
29074251
16.

Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma.

Matthey M, Roberts R, Seidinger A, Simon A, Schröder R, Kuschak M, Annala S, König GM, Müller CE, Hall IP, Kostenis E, Fleischmann BK, Wenzel D.

Sci Transl Med. 2017 Sep 13;9(407). pii: eaag2288. doi: 10.1126/scitranslmed.aag2288.

PMID:
28904224
17.

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.

Nature. 2017 Sep 14;549(7671):282-286. doi: 10.1038/nature23676. Epub 2017 Sep 6.

18.

Reactivation of Gαi-coupled formyl peptide receptors is inhibited by Gαq-selective inhibitors when induced by signals generated by the platelet-activating factor receptor.

Holdfeldt A, Dahlstrand Rudin A, Gabl M, Rajabkhani Z, König GM, Kostenis E, Dahlgren C, Forsman H.

J Leukoc Biol. 2017 Sep;102(3):871-880. doi: 10.1189/jlb.2A0317-086RR. Epub 2017 Jul 31.

PMID:
28760822
19.

Prostaglandin E2 glyceryl ester is an endogenous agonist of the nucleotide receptor P2Y6.

Brüser A, Zimmermann A, Crews BC, Sliwoski G, Meiler J, König GM, Kostenis E, Lede V, Marnett LJ, Schöneberg T.

Sci Rep. 2017 May 24;7(1):2380. doi: 10.1038/s41598-017-02414-8.

20.

The molecular mechanism by which saturated lysophosphatidylcholine attenuates the metastatic capacity of melanoma cells.

Ross T, Jakubzig B, Grundmann M, Massing U, Kostenis E, Schlesinger M, Bendas G.

FEBS Open Bio. 2016 Nov 24;6(12):1297-1309. doi: 10.1002/2211-5463.12152. eCollection 2016 Dec.

21.

The Orphan Receptor GPR17 Is Unresponsive to Uracil Nucleotides and Cysteinyl Leukotrienes.

Simon K, Merten N, Schröder R, Hennen S, Preis P, Schmitt NK, Peters L, Schrage R, Vermeiren C, Gillard M, Mohr K, Gomeza J, Kostenis E.

Mol Pharmacol. 2017 May;91(5):518-532. doi: 10.1124/mol.116.107904. Epub 2017 Mar 2. Erratum in: Mol Pharmacol. 2017 Jul;92 (1):100.

22.

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.

Mol Pharmacol. 2017 Apr;91(4):348-356. doi: 10.1124/mol.116.107276. Epub 2017 Feb 6.

23.

FZD10-Gα13 signalling axis points to a role of FZD10 in CNS angiogenesis.

Hot B, Valnohova J, Arthofer E, Simon K, Shin J, Uhlén M, Kostenis E, Mulder J, Schulte G.

Cell Signal. 2017 Apr;32:93-103. doi: 10.1016/j.cellsig.2017.01.023. Epub 2017 Jan 24.

PMID:
28126591
24.

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.

J Pharmacol Exp Ther. 2017 Feb;360(2):289-299. doi: 10.1124/jpet.116.237149. Epub 2016 Nov 15.

25.

Functional selectivity and dualsteric/bitopic GPCR targeting.

Schrage R, Kostenis E.

Curr Opin Pharmacol. 2017 Feb;32:85-90. doi: 10.1016/j.coph.2016.12.001. Epub 2016 Dec 24. Review.

PMID:
28027487
26.

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.

Mol Pharmacol. 2016 Oct;90(4):447-59. doi: 10.1124/mol.116.104919. Epub 2016 Jul 25.

27.

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.

J Biol Chem. 2016 Sep 2;291(36):18915-31. doi: 10.1074/jbc.M116.736157. Epub 2016 Jul 5.

28.

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.

Cell Rep. 2016 May 24;15(8):1757-70. doi: 10.1016/j.celrep.2016.04.053. Epub 2016 May 12.

29.

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.

Proc Natl Acad Sci U S A. 2016 Apr 19;113(16):4524-9. doi: 10.1073/pnas.1521706113. Epub 2016 Apr 8.

30.

A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor.

Grundmann M, Tikhonova IG, Hudson BD, Smith NJ, Mohr K, Ulven T, Milligan G, Kenakin T, Kostenis E.

Cell Chem Biol. 2016 Mar 17;23(3):392-403. doi: 10.1016/j.chembiol.2016.02.014.

31.

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.

Nat Commun. 2016 Mar 9;7:10895. doi: 10.1038/ncomms10895.

32.

Holistic Methods for the Analysis of cNMP Effects.

Grundmann M, Kostenis E.

Handb Exp Pharmacol. 2017;238:339-357. doi: 10.1007/164_2015_42. Review.

PMID:
26721676
33.

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.

Nat Commun. 2015 Dec 14;6:10156. doi: 10.1038/ncomms10156.

34.

The Orphan G Protein-coupled Receptor GPR17 Negatively Regulates Oligodendrocyte Differentiation via Gαi/o and Its Downstream Effector Molecules.

Simon K, Hennen S, Merten N, Blättermann S, Gillard M, Kostenis E, Gomeza J.

J Biol Chem. 2016 Jan 8;291(2):705-18. doi: 10.1074/jbc.M115.683953. Epub 2015 Nov 30.

35.

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.

J Med Chem. 2016 Jan 14;59(1):61-81. doi: 10.1021/acs.jmedchem.5b01239. Epub 2015 Dec 25.

PMID:
26595749
36.

Superagonism at G protein-coupled receptors and beyond.

Schrage R, De Min A, Hochheiser K, Kostenis E, Mohr K.

Br J Pharmacol. 2016 Oct;173(20):3018-27. doi: 10.1111/bph.13278. Epub 2015 Oct 24. Review.

37.

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.

Br J Nutr. 2015 Jun 14;113(11):1677-88. doi: 10.1017/S000711451500118X. Epub 2015 Apr 28.

PMID:
25916176
38.

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.

Cell Physiol Biochem. 2015;35(6):2272-84. doi: 10.1159/000374031. Epub 2015 Apr 13.

39.

Label-free biosensor assays in GPCR screening.

Grundmann M, Kostenis E.

Methods Mol Biol. 2015;1272:199-213. doi: 10.1007/978-1-4939-2336-6_14.

PMID:
25563186
40.

Pilot the pulse: controlling the multiplicity of receptor dynamics.

Bock A, Kostenis E, Tränkle C, Lohse MJ, Mohr K.

Trends Pharmacol Sci. 2014 Dec;35(12):630-8. doi: 10.1016/j.tips.2014.10.002. Epub 2014 Oct 31.

PMID:
25455830
41.

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.

Biochem Biophys Res Commun. 2014 Sep 5;451(4):497-502. doi: 10.1016/j.bbrc.2014.07.134. Epub 2014 Aug 7.

PMID:
25108158
42.

Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.

Schmitz J, van der Mey D, Bermudez M, Klöckner J, Schrage R, Kostenis E, Tränkle C, Wolber G, Mohr K, Holzgrabe U.

J Med Chem. 2014 Aug 14;57(15):6739-50. doi: 10.1021/jm500790x. Epub 2014 Aug 4.

PMID:
25051097
43.

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.

Br J Pharmacol. 2014 Dec;171(23):5387-406. doi: 10.1111/bph.12850. Epub 2014 Sep 5.

44.

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.

Chem Biol. 2014 Jul 17;21(7):890-902. doi: 10.1016/j.chembiol.2014.06.003.

45.

Allostery: A GPCR's back door.

Mohr K, Kostenis E.

Nat Chem Biol. 2014 Aug;10(8):609-10. doi: 10.1038/nchembio.1583. No abstract available.

PMID:
25036308
46.

Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.

Köse M, Ritter K, Thiemke K, Gillard M, Kostenis E, Müller CE.

ACS Med Chem Lett. 2014 Jan 16;5(4):326-30. doi: 10.1021/ml400399f. eCollection 2014 Apr 10.

47.

New insight into active muscarinic receptors with the novel radioagonist [³H]iperoxo.

Schrage R, Holze J, Klöckner J, Balkow A, Klause AS, Schmitz AL, De Amici M, Kostenis E, Tränkle C, Holzgrabe U, Mohr K.

Biochem Pharmacol. 2014 Aug 1;90(3):307-19. doi: 10.1016/j.bcp.2014.05.012. Epub 2014 May 23.

PMID:
24863257
48.

A biased non-Gαi OXE-R antagonist demonstrates that Gαi protein subunit is not directly involved in neutrophil, eosinophil, and monocyte activation by 5-oxo-ETE.

Konya V, Blättermann S, Jandl K, Platzer W, Ottersbach PA, Marsche G, Gütschow M, Kostenis E, Heinemann A.

J Immunol. 2014 May 15;192(10):4774-82. doi: 10.4049/jimmunol.1302013. Epub 2014 Apr 14.

49.

β-arrestin 2 inhibits proinflammatory chemokine production and attenuates contact allergic inflammation in the skin.

Gaffal E, Jakobs M, Glodde N, Schröder R, Kostenis E, Tüting T.

J Invest Dermatol. 2014 Aug;134(8):2131-2137. doi: 10.1038/jid.2014.117. Epub 2014 Feb 27.

50.

Detection of free fatty acid receptor 1 expression: the critical role of negative and positive controls.

Teutsch CA, Panse M, Grundmann M, Kaiser G, Kostenis E, Häring HU, Ullrich S.

Diabetologia. 2014 Apr;57(4):776-80. doi: 10.1007/s00125-014-3161-8. Epub 2014 Jan 26.

PMID:
24463963

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