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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: kuschak m. 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. 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.
Heterologous Expression, Biosynthetic Studies, and Ecological Function of the Selective Gq-Signaling Inhibitor FR900359.
Crüsemann M, Reher R, Schamari I, Brachmann AO, Ohbayashi T, Kuschak M, Malfacini D, Seidinger A, Pinto-Carbó M, Richarz R, Reuter T, Kehraus S, Hallab A, Attwood M, Schiöth HB, Mergaert P, Kikuchi Y, Schäberle TF, Kostenis E, Wenzel D, Müller CE, Piel J, Carlier A, Eberl L, König GM. Crüsemann M, et al. Among authors: kuschak m. Angew Chem Int Ed Engl. 2018 Jan 15;57(3):836-840. doi: 10.1002/anie.201707996. Epub 2017 Dec 20. Angew Chem Int Ed Engl. 2018. PMID: 29194875