Dr. René Richarz, rricharz@uni-bonn.de

Wiebke Hanke, wiebke.hanke@freenet.de

Sophie Klöppel, s6sokloe@uni-bonn.de

Hanke W, Alenfelder J, Liu J, Gutbrod P, Kehraus S, Crüsemann M, Dörmann P, Kostenis E, Scholz M, König GM. The Bacterial Gq Signal Transduction Inhibitor FR900359 Impairs Soil-Associated Nematodes. J Chem Ecol. 2023 Jul 15. doi: 10.1007/s10886-023-01442-1. Epub ahead of print. PMID: 37453001.

Wirtz DA, Schneberger N, Klöppel S, Richarz R, Geyer M, König GM, Hagelueken G, Crüsemann M. Adenylation Domain-Guided Recruitment of Trans-Acting Nonheme Monooxygenases in Nonribosomal Peptide Biosynthesis. ACS Chem Biol. 2023 Jun 27. doi: 10.1021/acschembio.3c00106. Epub ahead of print. PMID: 37366538.

Krome AK, Becker T, Kehraus S, Schiefer A, Gütschow M, Chaverra-Muñoz L, Hüttel S, Jansen R, Stadler M, Ehrens A, Pogorevc D, Müller R, Hübner MP, Hesterkamp T, Pfarr K, Hoerauf A, Wagner KG, König GM. Corallopyronin A: antimicrobial discovery to preclinical development. Nat Prod Rep. 2022 Jun 22. doi: 10.1039/d2np00012a. Epub ahead of print. PMID: 35730490.

Wirtz DA, Ludwig KC, Arts M, Marx CE, Krannich S, Barac P, Kehraus S, Josten M, Henrichfreise B, Müller A, König GM, Peoples AJ, Nitti A, Spoering AL, Ling LL, Lewis K, Crüsemann M, Schneider T. (2021) Biosynthesis and Mechanism of Action of the Cell Wall Targeting Antibiotic Hypeptin. Angew Chem Int Ed Engl. 60(24):13579-13586. doi: 10.1002/anie.202102224. Epub 2021 May 7. PMID: 33768646; PMCID: PMC8252469.

Klöppel S, Richarz R, Wirtz DA, Vasenda N, König GM, Crüsemann M. (2021) A Specialized Dehydrogenase Provides l-Phenyllactate for FR900359 Biosynthesis. Chembiochem. doi: 10.1002/cbic.202100569. Epub ahead of print. PMID: 34846772. 

Hanke W, Patt J, Alenfelder J, Voss JH, Zdouc MM, Kehraus S, Kim JB, Grujičić GV, Namasivayam V, Reher R, Müller CE, Kostenis E, Crüsemann M, König GM. (2021) Feature-Based Molecular Networking for the Targeted Identification of Gq-Inhibiting FR900359 Derivatives. J Nat Prod. doi: 10.1021/acs.jnatprod.1c00194. Epub 2021 Jul 1. PMID: 34197116.

Hermes C, König GM, Crüsemann M. (2021) The chromodepsins - chemistry, biology and biosynthesis of a selective Gq inhibitor natural product family. Nat Prod Rep. doi: 10.1039/d1np00005e. Epub ahead of print. PMID: 33998635.

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.

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. (2021) An experimental strategy to probe Gq contribution to signal transduction in living cells. J Biol Chem. doi: https://doi.org/10.1016/j.jbc.2021.100472 

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. (2021) Thioesterase-mediated side chain transesterification generates potent Gq signaling inhibitor FR900359. Nat Commun. doi: 10.1038/s41467-020-20418-3.

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.

Malfacini D, Patt J, Annala S, Harpsøe K, Eryilmaz F, Reher R, Crüsemann M, Hanke W, Zhang H, Tietze D, Gloriam DE, Bräuner-Osborne H, Strømgaard K, König GM, Inoue A, Gomeza J, Kostenis E. (2019) Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity. J Biol Chem. doi: 10.1074/jbc.RA118.007250

Imhof D, Reher R, Kühl T, Annala S, Benkel T, Kaufmann D, Nubbemeyer B, Odhiambo JP, Heimer P, Bäuml CA, Kehraus S, Crüsemann M, Kostenis E, Tietze D, König GM. (2018) Deciphering specificity determinants for FR900359-derived Gαq inhibitors based on computational and structure-activity studies. ChemMedChem doi: 10.1002/cmdc.201800304

Grundmann M, Merten N, Malfacini D, Inoue A, Preis P, Simon K, Rüttiger N, Ziegler N, Benkel T, Schmitt NK, Ishida S, Müller I, Reher R, Kawakami K, Inoue A, Rick U, Kühl T, Imhof D, Aoki J,  König GM, Hoffmann C, Gomeza J, Wess J, Kostenis E (2018); Lack of beta-arrestin signaling in the absence of active G proteins, Nat Commun, doi:10.1038/s41467-017-02661-3

Reher R, Kuschak M, Heycke N, Annala S, Kehraus S, Dai HF, Müller CE, Kostenis E, König GM, Crüsemann M. (2018) Applying Molecular Networking for the Detection of Natural Sources and Analogues of the Selective Gq Protein Inhibitor FR900359. J Nat Prod. doi: 10.1021/acs.jnatprod.8b00222 

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

Murat S, Bigot M, Chapron J, König GM, Kostenis E, Battaglia G, Nicoletti F, Bourinet E, Bockaert J, Marin P, Vandermoere F. (2018) 5-HT2A receptor-dependent phosphorylation of mGlu2 receptor at Serine 843 promotes mGlu2receptor-operated Gi/o signaling. Mol Psychiatry doi: 10.1038/s41380-018-0069-6

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

Klepac K, Kilic A, Gnad T, Brown LM, Herrmann B, Wildermann A, Balkow A, Glöde A, Simon K, Lidell ME, Betz MJ, Enerbäck S, Wess J, Freichel M, Blüher M, König G, Kostenis E, Insel PA and Pfeifer A (2016); The Gq signalling pathway inhibits brown and beige adipose tissue, Nat commun, 7, 10895, doi: 10.1038/ncomms10895

chrage 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