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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: kuppers j. Nat Commun. 2021 Jan 8;12(1):144. doi: 10.1038/s41467-020-20418-3. Nat Commun. 2021. PMID: 33420046 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: kuppers j. 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.
BIM-46174 fragments as potential ligands of G proteins.
Küppers J, Benkel T, Annala S, Schnakenburg G, Kostenis E, Gütschow M. Küppers J, et al. Medchemcomm. 2019 Aug 21;10(10):1838-1843. doi: 10.1039/c9md00269c. eCollection 2019 Oct 1. Medchemcomm. 2019. PMID: 32180917 Free PMC article.
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