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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: simon k. Nat Commun. 2012;3:1044. doi: 10.1038/ncomms2028. Nat Commun. 2012. PMID: 22948826 Free PMC article.
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: simon k. Sci Signal. 2013 Oct 22;6(298):ra93. doi: 10.1126/scisignal.2004350. Sci Signal. 2013. PMID: 24150254 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: simon k. Nat Commun. 2016 Mar 9;7:10895. doi: 10.1038/ncomms10895. Nat Commun. 2016. PMID: 26955961 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: simon k. Nat Commun. 2018 Jan 23;9(1):341. doi: 10.1038/s41467-017-02661-3. Nat Commun. 2018. PMID: 29362459 Free PMC article.
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: simon k. 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.
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: simon k. 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
1,342 results