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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. Nat Chem Biol. 2014 Jan;10(1):18-20. doi: 10.1038/nchembio.1384. Epub 2013 Nov 10. Nat Chem Biol. 2014. PMID: 24212135
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: bock a. Nat Chem Biol. 2012 Jul;8(7):631-8. doi: 10.1038/nchembio.962. Epub 2012 May 27. Nat Chem Biol. 2012. PMID: 22634634
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: bock a. Mol Pharmacol. 2017 Apr;91(4):348-356. doi: 10.1124/mol.116.107276. Epub 2017 Feb 6. Mol Pharmacol. 2017. PMID: 28167741
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: bock a. 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.
698 results