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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: schrage r. 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.
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: schrage r. Sci Signal. 2013 Oct 22;6(298):ra93. doi: 10.1126/scisignal.2004350. Sci Signal. 2013. PMID: 24150254 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: schrage r. 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.
Superagonism at G protein-coupled receptors and beyond.
Schrage R, De Min A, Hochheiser K, Kostenis E, Mohr K. Schrage R, et al. 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.
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: schrage r. 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.
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: schrage r. Nat Commun. 2012;3:1044. doi: 10.1038/ncomms2028. Nat Commun. 2012. PMID: 22948826 Free PMC article.
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: schrage r. 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
45 results