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Project 6 - Kostenis lab

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Univ.-Prof. Dr. Evi Kostenis

University of Bonn

Pharmaceutical Institute

Dept of Pharmaceutical Biology

Nussallee 6

D-53115 Bonn

Phone:  0228/73-2678

Fax :       0228/73-3250

Mail :      [Email protection active, please enable JavaScript.]

 

Molecular modes of action and application  of cell-permeable inhibitors for heterotrimeric G proteins

 

Team members

Funda Eryilmaz, [Email protection active, please enable JavaScript.]

Julian Patt, [Email protection active, please enable JavaScript.]

Julian Zeiner, [Email protection active, please enable JavaScript.]

Tobias Benkel, [Email protection active, please enable JavaScript.]

Dr. Nicole Merten, [Email protection active, please enable JavaScript.]

Dr. Jesús Gomeza, [Email protection active, please enable JavaScript.]

Nina Heycke, [Email protection active, please enable JavaScript.]

Ulrike Rick, [Email protection active, please enable JavaScript.]

 

Publications

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.2021.100472DOI-icon.jpg

 

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.DOI-icon.jpg

 

Annala S, Feng X, Shridhar N, Eryilmaz F, Patt J, Yang J, Pfeil EM, Cervantes-Villagrana RD, Inoue A, Häberlein F, Slodczyk T, Reher R, Kehraus S, Monteleone S, Schrage R, Heycke N, Rick U, Engel S, Pfeifer A, Kolb P, König G, Bünemann M, Tüting T, Vázquez-Prado J, Gutkind JS, Gaffal E, Kostenis E (2019) Direct targeting of Gαq and Gα11 oncoproteins in cancer cells Sci. Signal. doi: 10.1126/scisignal.aau5948DOI-icon.jpg

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 DOI-icon.jpg

 

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.201800304DOI-icon.jpg

 

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/s41380-018-0069-6DOI-icon.jpg

 

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 proteinsNat Commun, doi:10.1038/s41467-017-02661-3DOI-icon.jpg

 

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

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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

 

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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