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Macrocyclic Gq Protein Inhibitors FR900359 and/or YM-254890-Fit for Translation?
Schlegel JG, Tahoun M, Seidinger A, Voss JH, Kuschak M, Kehraus S, Schneider M, Matthey M, Fleischmann BK, König GM, Wenzel D, Müller CE. Schlegel JG, et al. Among authors: voss jh. ACS Pharmacol Transl Sci. 2021 Feb 19;4(2):888-897. doi: 10.1021/acsptsci.1c00021. eCollection 2021 Apr 9. ACS Pharmacol Transl Sci. 2021. PMID: 33860209 Free PMC article.
Cell-permeable high-affinity tracers for Gq proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors.
Kuschak M, Namasivayam V, Rafehi M, Voss JH, Garg J, Schlegel JG, Abdelrahman A, Kehraus S, Reher R, Küppers J, Sylvester K, Hinz S, Matthey M, Wenzel D, Fleischmann BK, Pfeifer A, Inoue A, Gütschow M, König GM, Müller CE. Kuschak M, et al. Among authors: voss jh. Br J Pharmacol. 2020 Apr;177(8):1898-1916. doi: 10.1111/bph.14960. Epub 2020 Feb 11. Br J Pharmacol. 2020. PMID: 31881095 Free PMC article.
Thioesterase-mediated side chain transesterification generates potent Gq signaling inhibitor FR900359.
Hermes C, Richarz R, Wirtz DA, Patt J, Hanke W, Kehraus S, Voß JH, Küppers J, Ohbayashi T, Namasivayam V, Alenfelder J, Inoue A, Mergaert P, Gütschow M, Müller CE, Kostenis E, König GM, Crüsemann M. Hermes C, et al. Among authors: voss jh. Nat Commun. 2021 Jan 8;12(1):144. doi: 10.1038/s41467-020-20418-3. Nat Commun. 2021. PMID: 33420046 Free PMC article.
An experimental strategy to probe Gq contribution to signal transduction in living cells.
Patt J, Alenfelder J, Pfeil EM, Voss JH, Merten N, Eryilmaz F, Heycke N, Rick U, Inoue A, Kehraus S, Deupi X, Müller CE, König GM, Crüsemann M, Kostenis E. Patt J, et al. Among authors: voss jh. J Biol Chem. 2021 Jan-Jun;296:100472. doi: 10.1016/j.jbc.2021.100472. Epub 2021 Feb 25. J Biol Chem. 2021. PMID: 33639168 Free PMC article.
Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates.
Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaaßen VJ, Schlegel JG, Vielmuth C, Voß JH, Labahn J, Müller CE. Claff T, et al. Among authors: voss jh. Angew Chem Int Ed Engl. 2022 May 23;61(22):e202115545. doi: 10.1002/anie.202115545. Epub 2022 Mar 24. Angew Chem Int Ed Engl. 2022. PMID: 35174942 Free PMC article.
34 results