Direct pharmacological G protein modulation in the lung

Avatar Fleischmann

Prof. Dr. Bernd Fleischmann

Siegmund-Freud-Str. 25

53127 Bonn

Avatar Wenzel

Jun.-Prof. Dr. Daniela Wenzel

Sigmund-Freud-Str. 25

53127 Bonn

Team members

Alexander Seidinger, Alexander.seidinger@ruhr-uni-bochum.de

Jennifer Dietrich, jdie@uni-bonn.de

Jana Lewandowski, Jana.Lewandowski@ruhr-uni-bochum.de

Publications

Schlegel JG, Tahoun M, Seidinger A, Voss JH, Kuschak M, Kehraus S, Schneider M, Matthey M, Fleischmann BK, König GM, Wenzel D, Müller CE. (2021) Macrocyclic Gq Protein Inhibitors FR900359 and/or YM-254890-Fit for Translation? ACS Pharmacol Transl Sci. doi: 10.1021/acsptsci.1c00021. PMID: 33860209; PMCID: PMC8033771.

Kuschak M, Schlegel JG, Schneider M, Kehraus S, Voss JH, Seidinger A, Matthey M, Wenzel D, Fleischmann BK, König GM, Müller CE. (2020) Sensitive LC-MS/MS Method for the Quantification of Macrocyclic Gαq Protein Inhibitors in Biological Samples. Front Chem. doi: 10.3389/fchem.2020.00833. PMID: 33173765; PMCID: PMC7540253.

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. (2020) Cell-permeable high-affinity tracers for Gq proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors. Br J Pharmacol. doi: 10.1111/bph.14960. Epub 2020 Feb 11. PMID: 31881095; PMCID: PMC7070167.

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, Koenig GM (2017); Heterologous expression, biosynthetic studies and ecological function of the selective Gq-signaling inhibitor FR900359, Angew. Chem. Int. Ed., doi: 10.1002/anie.201707996

Matthey M, Roberts R, Seidinger A, Simon A, Schröder R, Kuschak M, Annala S, König GM, Müller CE, Hall IP, Kostenis E, Fleischmann BK, Wenzel D (2017); Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma, Sci Transl Med., 2, 407, doi:10.1126/scitranslmed.aag2288

Schrage R, Schmitz AL, Gaffal E, Annala S, Kehraus S, Wenzel D, Büllesbach KM, Bals T, Inoue A, Shinjo Y, Galandrin S, Shridhar N, Hesse M, Grundmann M, Merten N, Charpentier TH, Martz M, Butcher AJ, Slodczyk T, Armando S, Effer M, Namkung Y, Jenkins L, Horn V, Stößel A, Dargatz H, Tietze D, Imhof D, Galés C, Drewke C, Müller CE, Hölzel M, Milligan G, Tobin AB, Gomeza J, Dohlmann HG, Sondek J, Harden K, Bouvier M, Laporte SA, Aoki J, Fleischmann BK, Mohr K, König GM, Tüting T and Kostenis E (2015); The experimental power of FR900359 to study Gq-regulated biological processes, Nat Commun, 6, 10156, doi: 10.1038/ncomms10156

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