Bock A - Search Results

1

Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.

Chen X, Klöckner J, Holze J, Zimmermann C, Seemann WK, Schrage R, Bock A, Mohr K, Tränkle C, Holzgrabe U, Decker M. Chen X, et al. Among authors: bock a. J Med Chem. 2015 Jan 22;58(2):560-76. doi: 10.1021/jm500860w. Epub 2014 Dec 19. J Med Chem. 2015. PMID: 25478907

2

Dualsteric GPCR targeting and functional selectivity: the paradigmatic M(2) muscarinic acetylcholine receptor.

Bock A, Mohr K. Bock A, et al. Drug Discov Today Technol. 2013 Summer;10(2):e245-52. doi: 10.1016/j.ddtec.2012.12.003. Drug Discov Today Technol. 2013. PMID: 24050275 Review.

3

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

4

Pilot the pulse: controlling the multiplicity of receptor dynamics.

Bock A, Kostenis E, Tränkle C, Lohse MJ, Mohr K. Bock A, et al. Trends Pharmacol Sci. 2014 Dec;35(12):630-8. doi: 10.1016/j.tips.2014.10.002. Epub 2014 Oct 31. Trends Pharmacol Sci. 2014. PMID: 25455830

5

Ligand Binding Ensembles Determine Graded Agonist Efficacies at a G Protein-coupled Receptor.

Bock A, Bermudez M, Krebs F, Matera C, Chirinda B, Sydow D, Dallanoce C, Holzgrabe U, De Amici M, Lohse MJ, Wolber G, Mohr K. Bock A, et al. J Biol Chem. 2016 Jul 29;291(31):16375-89. doi: 10.1074/jbc.M116.735431. Epub 2016 Jun 13. J Biol Chem. 2016. PMID: 27298318 Free PMC article.

6

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

7

Ligand-Specific Restriction of Extracellular Conformational Dynamics Constrains Signaling of the M₂ Muscarinic Receptor.

Bermudez M, Bock A, Krebs F, Holzgrabe U, Mohr K, Lohse MJ, Wolber G. Bermudez M, et al. Among authors: bock a. ACS Chem Biol. 2017 Jul 21;12(7):1743-1748. doi: 10.1021/acschembio.7b00275. Epub 2017 Jun 12. ACS Chem Biol. 2017. PMID: 28585805

8

Allosteric modulators targeting CNS muscarinic receptors.

Bock A, Schrage R, Mohr K. Bock A, et al. Neuropharmacology. 2018 Jul 1;136(Pt C):427-437. doi: 10.1016/j.neuropharm.2017.09.024. Epub 2017 Sep 18. Neuropharmacology. 2018. PMID: 28935216 Review.

9

Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M₁ and M₂.

Messerer R, Dallanoce C, Matera C, Wehle S, Flammini L, Chirinda B, Bock A, Irmen M, Tränkle C, Barocelli E, Decker M, Sotriffer C, De Amici M, Holzgrabe U. Messerer R, et al. Among authors: bock a. Medchemcomm. 2017 Apr 27;8(6):1346-1359. doi: 10.1039/c7md00149e. eCollection 2017 Jun 1. Medchemcomm. 2017. PMID: 30108847 Free PMC article.

10

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.

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