2024

Kostenis E, Jürgenliemke L, Alenfelder J. G protein-mediated signal transduction: a molecular choreography of G protein activation after GTP binding. Signal Transduct Target Ther. 2024 Jul 16;9(1):188. doi: 10.1038/s41392-024-01903-3. PMID: 39013896; PMCID: PMC11252409.

Seidinger A, Roberts R, Bai Y, Müller M, Pfeil E, Matthey M, Rieck S, Alenfelder J, König GM, Pfeifer A, Kostenis E, Klinke A, Fleischmann BK, Wenzel D. Pharmacological Gq inhibition induces strong pulmonary vasorelaxation and reverses pulmonary hypertension. EMBO Mol Med. 2024 Aug;16(8):1930-1956. doi: 10.1038/s44321-024-00096-0. Epub 2024 Jul 8. PMID: 38977926; PMCID: PMC11319782.

Mengoni M, Braun AD, Seedarala S, Bonifatius S, Kostenis E, Schanze D, Zenker M, Tüting T, Gaffal E. Transactivation of Met signaling by oncogenic Gnaq drives the evolution of melanoma in Hgf-Cdk4 mice. Cancer Gene Ther. 2024 Jun;31(6):884-893. doi: 10.1038/s41417-024-00744-0. Epub 2024 Feb 15. PMID: 38360887; PMCID: PMC11192630.

Bonifer C, Hanke W, Mühle J, Löhr F, Becker-Baldus J, Nagel J, Schertler GFX, Müller CE, König GM, Hilger D, Glaubitz C. Structural response of G protein binding to the cyclodepsipeptide inhibitor FR900359 probed by NMR spectroscopy. Chem Sci. 2024 Jul 4;15(32):12939-12956. doi: 10.1039/d4sc01950d. PMID: 39148790; PMCID: PMC11323312.

2023

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.

Kostenis E, Bravo S, Gomeza J. Giving ERK a jERK from the endosome. Trends Pharmacol Sci. 2023 44(3):131-133. doi: 10.1016/j.tips.2022.12.004. Epub 2023 Jan 3. PMID: 36604224.

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.

Voss JH, Crüsemann M, Bartling CRO, Kehraus S, Inoue A, König GM, Strømgaard K, Müller CE. Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors. iScience. 2023 Mar 23;26(4):106492. doi: 10.1016/j.isci.2023.106492. PMID: 37091255; PMCID: PMC10119753.

Voss JH, Al-Hroub H, Gedschold R, Dietrich JM, Gaffal E, Toma M, Kehraus S, König GM, Brust P, Fleischmann BK, Wenzel D, Deuther-Conrad W, Müller CE. Imaging of Gαq Proteins in Mouse and Human Organs and Tissues. Pharmaceutics. 2022 Dec 24;15(1):57. doi: 10.3390/pharmaceutics15010057. PMID: 36678686; PMCID: PMC9865079.

Kostenis E, Gomeza J, Miess-Tanneberg E, Blum NK, Benkel T, Chevigné A, Hoffmann C, Kolb P, Nikolaev V, Waldhoer M, Szpakowska M, Inoue A, Schulz S. Reply to: How carvedilol does not activate β2-adrenoceptors. Nat Commun. 2023 Nov 30;14(1):7867. doi: 10.1038/s41467-023-42849-4. PMID: 38036502; PMCID: PMC10689814.

Kostenis E, Bravo S, Gomeza J. Giving ERK a jERK from the endosome. Trends Pharmacol Sci. 2023 Mar;44(3):131-133. doi: 10.1016/j.tips.2022.12.004. Epub 2023 Jan 3. PMID: 36604224.

2022

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.

Benkel, T., Zimmermann, M., Zeiner, J. et al. How Carvedilol activates β₂-adrenoceptors. Nat Commun 13, 7109 (2022). https://doi.org/10.1038/s41467-022-34765-w.

Klöppel S, Richarz R, Wirtz DA, Vasenda N, König GM, Crüsemann M. A Specialized Dehydrogenase Provides l-Phenyllactate for FR900359 Biosynthesis. Chembiochem. 2022 May 18;23(10):e202100569. doi: 10.1002/cbic.202100569. Epub 2021 Dec 9. PMID: 34846772; PMCID: PMC9299796.

Voss JH, Müller CE. Heterotrimeric G Protein α-Subunits - Structures, Peptide-Derived Inhibitors, and Mechanisms. Curr Med Chem. 2022;29(42):6359-6378. doi: 10.2174/0929867329666220308112424. PMID: 35260051.

Voss JH, Mahardhika AB, Inoue A, Müller CE. Agonist-Dependent Coupling of the Promiscuous Adenosine A2B Receptor to Gα Protein Subunits. ACS Pharmacol Transl Sci. 2022 May 3;5(5):373-386. doi: 10.1021/acsptsci.2c00020. PMID: 35592437; PMCID: PMC9112290.

2021

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
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
A Specialized Dehydrogenase Provides l-Phenyllactate for FR900359 Biosynthesis
Chembiochem. doi: 10.1002/cbic.202100569. Epub ahead of print. PMID: 34846772.  

Schlegel JG, Tahoun M, Seidinger A, Voss JH, Kuschak M, Kehraus S, Schneider M, Matthey M, Fleischmann BK, König GM, Wenzel D, Müller CE
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.

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

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
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.

Voss JH, Nagel J, Rafehi M, Guixà-González R, Malfacini D, Patt J, Kehraus S, Inoue A, König GM, Kostenis E, Deupi X, Namasivayam V, Müller CE
Unraveling binding mechanism and kinetics of macrocyclic Gαq protein inhibitors
Pharmacol Res. doi: 10.1016/j.phrs.2021.105880. Epub 2021 Sep 17. PMID: 34506902.

Hermes C, König GM, Crüsemann M
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.

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
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

2020

Holze J, Bermudez M, Pfeil EM, Kauk M, Bödefeld T, Irmen M, Matera C, Dallanoce C, De Amici M, Holzgrabe U, König GM, Tränkle C, Wolber G, Schrage R, Mohr K, Hoffmann C, Kostenis E, Bock A
Ligand-Specific Allosteric Coupling Controls G-Protein-Coupled Receptor Signaling
ACS Pharmacol Transl Sci. 3(5):859-867. doi: 10.1021/acsptsci.0c00069. PMID: 33073186; PMCID: PMC7551708. 

Pfeil EM, Brands J, Merten N, Vögtle T, Vescovo M, Rick U, Albrecht IM, Heycke N, Kawakami K, Ono Y, Ngako Kadji FM, Hiratsuka S, Aoki J, Häberlein F, Matthey M, Garg J, Hennen S, Jobin ML, Seier K, Calebiro D, Pfeifer A, Heinemann A, Wenzel D, König GM, Nieswandt B, Fleischmann BK, Inoue A, Simon K, Kostenis E
Heterotrimeric G Protein Subunit Gαq Is a Master Switch for Gβγ-Mediated Calcium Mobilization by Gi-Coupled GPCRs
Mol Cell. doi: 10.1016/j.molcel.2020.10.027. Epub 2020 Nov 16. PMID: 33202251.

Kuschak M, Schlegel JG, Schneider M, Kehraus S, Voss JH, Seidinger A, Matthey M, Wenzel D, Fleischmann BK, König GM, Müller CE
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
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.

2019

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
Direct targeting of Gαq and Gα11 oncoproteins in cancer cells
Sci. Signal doi: 10.1126/scisignal.aau5948

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
Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity
J Biol Chem. doi: 10.1074/jbc.RA118.007250

Tietze D, Kaufmann D, Tietze AA, Voll A, Reher R, Koenig GM, Hausch F
Structural and dynamical basis of G protein inhibition by YM-254890 and FR900359: an inhibitor in action
J Chem Inf Model. doi: 10.1021/acs.jcim.9b00433

Küppers J, Benkel T, Annala S, Schnakenburg G, Kostenis E, Gütschow M. BIM-46174 fragments as potential ligands of G proteins. Medchemcomm. 2019 Aug 21;10(10):1838-1843. doi: 10.1039/c9md00269c. PMID: 32180917;

2018

Gutkind JS, Kostenis E
Arrestins as rheostats of GPCR signaling
Nat Rev Mol Cell Biol, doi: 10.1038/s41580-018-0041-y. 

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
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
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
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

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, Imhof D. Deciphering Specificity Determinants for FR900359-Derived Gq α Inhibitors Based on Computational and Structure-Activity Studies. ChemMedChem. 2018 Aug 20;13(16):1634-1643. doi: 10.1002/cmdc.201800304. Epub 2018 Jul 3. PMID: 29873888.

2017

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
Heterologous Expression, Biosynthetic Studies, and Ecological Function of the Selective Gq-Signaling Inhibitor FR900359
Angew Chem Int Ed Engl. 57(3):836-840. doi: 10.1002/anie.201707996. Epub 2017 Dec 20. PMID: 29194875.

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
Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma
Sci Transl Med., 2, 407, doi: 10.1126/scitranslmed.aag2288

2016

Küppers J, Schulz-Fincke AC, Palus J, Giurg M, Skarżewski J and  Gütschow M
Convergent synthesis of two fluorescent Ebselen-coumarin heterodimers
Pharmaceuticals, 9, 43, doi: 10.3390/ph9030043

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
The Gq signalling pathway inhibits brown and beige adipose tissue
Nat. Commun., 7, 10895, doi: 10.1038/ncomms10895

2015

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
The experimental power of FR900359 to study Gq-regulated biological processes
Nat. Commun., 6, 10156, doi: 10.1038/ncomms10156

2024

Matthees ESF, Filor JC, Jaiswal N, Reichel M, Youssef N, D'Uonnolo G, Szpakowska M, Drube J, König GM, Kostenis E, Chevigné A, Godbole A, Hoffmann C. GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism. Commun Biol. 2024 Jul 3;7(1):802. doi: 10.1038/s42003-024-06490-1. PMID: 38956302; PMCID: PMC11220067.

Metzger PJ, Zhang A, Carlson BA, Sun H, Cui Z, Li Y, Jahnke MT, Layton DR, Gupta MB, Liu N, Kostenis E, Gavrilova O, Chen M, Weinstein LS. A human obesity-associated MC4R mutation with defective Gq/11α signaling leads to hyperphagia in mice. J Clin Invest. 2024 Jan 4;134(4):e165418. doi: 10.1172/JCI165418. PMID: 38175730; PMCID: PMC10869179.

2023

Lorza-Gil E, Kaiser G, Carlein C, Hoffmann MDA, König GM, Haug S, Prates Roma L, Rexen Ulven E, Ulven T, Kostenis E, Birkenfeld AL, Häring HU, Ullrich S, Gerst F. Glucose-stimulated insulin secretion depends on FFA1 and Gq in neonatal mouse islets. Diabetologia. 2023 Aug;66(8):1501-1515. doi: 10.1007/s00125-023-05932-5. 

Alter C, Henseler AS, Owenier C, Hesse J, Ding Z, Lautwein T, Bahr J, Hayat S, Kramann R, Kostenis E, Scheller J, Schrader J. IL-6 in the infarcted heart is preferentially formed by fibroblasts and modulated by purinergic signaling. J Clin Invest. 2023 Jun 1;133(11):e163799. doi: 10.1172/JCI163799. PMID: 36943408; PMCID: PMC10232006.

Ribes A, Garcia C, Gratacap MP, Kostenis E, Martinez LO, Payrastre B, Sénard JM, Galés C, Pons V. Platelet P2Y1 receptor exhibits constitutive G protein signaling and β-arrestin 2 recruitment. BMC Biol. 2023 Feb 1;21(1):14. doi: 10.1186/s12915-023-01528-y. PMID: 36721118; PMCID: PMC9890698.

Wagdi A, Malan D, Sathyanarayanan U, Beauchamp JS, Vogt M, Zipf D, Beiert T, Mansuroglu B, Dusend V, Meininghaus M, Schneider L, Kalthof B, Wiegert JS, König GM, Kostenis E, Patejdl R, Sasse P, Bruegmann T. Author Correction: Selective optogenetic control of Gq signaling using human Neuropsin. Nat Commun. 2023 Jan 4;14(1):58. doi: 10.1038/s41467-022-35612-8. Erratum for: Nat Commun. 2022 Apr 1;13(1):1765. PMID: 36599836; PMCID: PMC9813341.

2022

Liu JJ, Eyring KW, König GM, Kostenis E, Tsien RW. Oxytocin-Modulated Ion Channel Ensemble Controls Depolarization, Integration and Burst Firing in CA2 Pyramidal Neurons. J Neurosci. 2022 Oct 12;42(41):7707-7720. doi: 10.1523/JNEUROSCI.0921-22.2022. Epub 2022 Sep 8. PMID: 36414006; PMCID: PMC9581561.

Drube J, Haider RS, Matthees ESF, Reichel M, Zeiner J, Fritzwanker S, Ziegler C, Barz S, Klement L, Filor J, Weitzel V, Kliewer A, Miess-Tanneberg E, Kostenis E, Schulz S, Hoffmann C
GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation
Nat Commun. 2022 Jan 27;13(1):540. doi: 10.1038/s41467-022-28152-8. PMID: 35087057; PMCID: PMC8795447.

Wagdi A, Malan D, Sathyanarayanan U, Beauchamp JS, Vogt M, Zipf D, Beiert T, Mansuroglu B, Dusend V, Meininghaus M, Schneider L, Kalthof B, Wiegert JS, König GM, Kostenis E, Patejdl R, Sasse P, Bruegmann T.
Selective optogenetic control of Gq signaling using human Neuropsin
Nat Commun. 13(1):1765. doi: 10.1038/s41467-022-29265-w. PMID: 35365606.

Kimura T, Pydi SP, Wang L, Haspula D, Cui Y, Lu H, König GM, Kostenis E, Steinberg GR, Gavrilova O, Wess J
Adipocyte Gq signaling is a regulator of glucose and lipid homeostasis in mice
Nat Commun. 13(1):1652. doi: 10.1038/s41467-022-29231-6. PMID: 35351896.

Kolb P, Kenakin T, Alexander SPH, Bermudez M, Bohn LM, Breinholt CS, Bouvier M, Hill SJ, Kostenis E, Martemyanov KA, Neubig RR, Onaran HO, Rajagopal S, Roth BL, Selent J, Shukla AK, Sommer ME, Gloriam DE
Community guidelines for GPCR ligand bias: IUPHAR review 32
Br J Pharmacol. doi: 10.1111/bph.15811. Epub ahead of print. PMID: 35106752. 

Liu L, Dattaroy D, Simpson KF, Barella LF, Cui Y, Xiong Y, Jin J, König GM, Kostenis E, Roman JC, Kaestner KH, Doliba NM, Wess J
Gq signaling in α cells is critical for maintaining euglycemia
JCI Insight. 6(24):e152852. doi: 10.1172/jci.insight.152852. PMID: 34752420; PMCID: PMC8783673. 

Wright SC, Cañizal MCA, Benkel T, Simon K, Le Gouill C, Matricon P, Namkung Y, Lukasheva V, König GM, Laporte SA, Carlsson J, Kostenis E, Bouvier M, Schulte G, Hoffmann C
FZD5 is a Gαq-coupled receptor that exhibits the functional hallmarks of prototypical GPCRs
Sci Signal. 11(559):eaar5536. doi: 10.1126/scisignal.aar5536. PMID: 30514810. 

Palmer CB, Meyrath M, Canals M, Kostenis E, Chevigné A, Szpakowska M
Atypical opioid receptors: unconventional biology and therapeutic opportunities
Pharmacol Ther. 2022 May;233:108014. doi: 10.1016/j.pharmthera.2021.108014. Epub 2021 Oct 5. PMID: 34624426.

2021 

Lorza-Gil E, Kaiser G, Rexen Ulven E, König GM, Gerst F, Oquendo MB, Birkenfeld AL, Häring HU, Kostenis E, Ulven T, Ullrich S
FFA2-, but not FFA3-agonists inhibit GSIS of human pseudoislets: a comparative study with mouse islets and rat INS-1E cells
Sci Rep. 5;10(1):16497. doi: 10.1038/s41598-020-73467-5. PMID: 33020504; PMCID: PMC7536384. 

Meyrath M, Szpakowska M, Zeiner J, Massotte L, Merz MP, Benkel T, Simon K, Ohnmacht J, Turner JD, Krüger R, Seutin V, Ollert M, Kostenis E, Chevigné A
The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides
Nat Commun. 11(1):3033. doi: 10.1038/s41467-020-16664-0. PMID: 32561830; PMCID: PMC7305236. 

Küppers J, Benkel T, Annala S, Kimura K, Reinelt L, Fleischmann BK, Kostenis E, Gütschow M
Tetrahydroimidazo[1,2-a]pyrazine Derivatives: Synthesis and Evaluation as Gαq -Protein Ligands
Chemistry. 26(55):12615-12623. doi: 10.1002/chem.202001446. Epub 2020 Sep 7. PMID: 32428383; PMCID: PMC7590114. 

Gröper J, König GM, Kostenis E, Gerke V, Raabe CA, Rescher U
Exploring Biased Agonism at FPR1 as a Means to Encode Danger Sensing
Cells. 9(4):1054. doi: 10.3390/cells9041054. PMID: 32340221; PMCID: PMC7226602. 

White AD, Jean-Alphonse FG, Fang F, Peña KA, Liu S, König GM, Inoue A, Aslanoglou D, Gellman SH, Kostenis E, Xiao K, Vilardaga JP
Gq/11-dependent regulation of endosomal cAMP generation by parathyroid hormone class B GPCR
Proc Natl Acad Sci U S A. 117(13):7455-7460. doi: 10.1073/pnas.1918158117. Epub 2020 Mar 17. PMID: 32184323; PMCID: PMC7132270. 

Küppers J, Benkel T, Annala S, Schnakenburg G, Kostenis E, Gütschow M
BIM-46174 fragments as potential ligands of G proteins
Medchemcomm. 10(10):1838-1843. doi: 10.1039/c9md00269c. PMID: 32180917; PMCID: PMC7053702. 

Floeser A, Becker K, Kostenis E, König G, Krasel C, Kolb P, Buenemann M
Disentangling bias between Gq, GRK2, and arrestin3 recruitment to the M3 muscarinic acetylcholine receptor
Elife. 10:e58442. doi: 10.7554/eLife.58442. PMID: 34851820.

Longden TA, Mughal A, Hennig GW, Harraz OF, Shui B, Lee FK, Lee JC, Reining S, Kotlikoff MI, König GM, Kostenis E, Hill-Eubanks D, Nelson MT
Local IP3 receptor-mediated Ca2+ signals compound to direct blood flow in brain capillaries
Sci Adv. doi: 10.1126/sciadv.abh0101. PMID: 34290098.

2020

Wenzel J, Hansen CE, Bettoni C, Vogt MA, Lembrich B, Natsagdorj R, Huber G, Brands J, Schmidt K, Assmann JC, Stölting I, Saar K, Sedlacik J, Fiehler J, Ludewig P, Wegmann M, Feller N, Richter M, Müller-Fielitz H, Walther T, König GM, Kostenis E, Raasch W, Hübner N, Gass P, Offermanns S, de Wit C, Wagner CA, Schwaninger M
Impaired endothelium-mediated cerebrovascular reactivity promotes anxiety and respiration disorders in mice
Proc Natl Acad Sci U S A. doi: 10.1073/pnas.1907467117.

Boesgaard MW, Harpsøe K, Malmberg M, Underwood CR, Inoue A, Mathiesen JM, König GM, Kostenis E, Gloriam DE, Bräuner-Osborne H
Delineation of molecular determinants for FR900359 inhibition of Gq/11 unlocks inhibition of Gαs
J Biol Chem. 295(40):13850-13861. doi: 10.1074/jbc.RA120.013002. Epub 2020 Aug 4. PMID: 32753482; PMCID: PMC7535923.

2019

Coombs C, Georgantzoglou A, Walker HA, Patt J, Merten N, Poplimont H, Busch-Nentwich EM, Williams S, Kotsi C, Kostenis E, Sarris M
Chemokine receptor trafficking coordinates neutrophil clustering and dispersal at wounds in zebrafish
Nat Commun. doi: 10.1038/s41467-019-13107-3.

Ebner JK, König GM, Kostenis E, Siegert P, Aktories K, Orth JHC
Activation of Gq signaling by Pasteurella multocida toxin inhibits the osteoblastogenic-like actions of Activin A in C2C12 myoblasts, a cell model of fibrodysplasia ossificans progressiva
Bone. doi: 10.1016/j.bone.2019.07.031

Kienitz MC, Niemeyer A, König GM, Kostenis E, Pott L, Rinne A
Biased signaling of Ca2+-sensing receptors in cardiac myocytes regulates GIRK channel activity
J Mol Cell Cardiol. doi: 10.1016/j.yjmcc.2019.03.022

Feng X, Arang N, Rigiracciolo DC, Lee JS, Yeerna H, Wang Z, Lubrano S, Kishore A, Pachter JA, König GM, Maggiolini M, Kostenis E, Schlaepfer DD, Tamayo P, Chen Q, Ruppin E, Gutkind JS
A Platform of Synthetic Lethal Gene Interaction Networks Reveals that the GNAQ Uveal Melanoma Oncogene Controls the Hippo Pathway through FAK
Cancer Cell. doi: 10.1016/j.ccell.2019.01.009

2018

Murat S, Bigot M, Chapron J, König GM, Kostenis E, Battaglia G, Nicoletti F, Bourinet E, Bockaert J, Marin P, Vandermoere F
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

Nimmagadda SC, Frey S, Edelmann B, Hellmich C, Zaitseva L, König GM, Kostenis E, Bowles KM, Fischer T
Bruton's tyrosine kinase and RAC1 promote cell survival in MLL-rearranged acute myeloid leukemia
Leukemia. 32(3):846-849. doi: 10.1038/leu.2017.324. Epub 2017 Nov 7. PMID: 29109446; PMCID: PMC5843904.

Redka DS, Gütschow M, Grinstein S, Canton J. Differential ability of proinflammatory and anti-inflammatory macrophages to perform macropinocytosis. Mol Biol Cell. 2018 Jan 1;29(1):53-65. doi: 10.1091/mbc.E17-06-0419. Epub 2017 Nov 1. PMID: 29093026; PMCID: PMC5746066.

2017

Klose CSN, Mahlakõiv T, Moeller JB, Rankin LC, Flamar AL, Kabata H, Monticelli LA, Moriyama S, Putzel GG, Rakhilin N, Shen X, Kostenis E, König GM, Senda T, Carpenter D, Farber DL, Artis D
The neuropeptide neuromedin U stimulates innate lymphoid cells and type 2 inflammation
Nature. 549(7671):282-286. doi: 10.1038/nature23676. Epub 2017 Sep 6. PMID: 28869965; PMCID: PMC6066372.

Holdfeldt A, Dahlstrand Rudin A, Gabl M, Rajabkhani Z, König GM, Kostenis E, Dahlgren C, Forsman H
Reactivation of Gαi-coupled formyl peptide receptors is inhibited by Gαq-selective inhibitors when induced by signals generated by the platelet-activating factor receptor
J Leukoc Biol. 102(3):871-880. doi: 10.1189/jlb.2A0317-086RR. Epub 2017 Jul 31. PMID: 28760822.

Brüser A, Zimmermann A, Crews BC, Sliwoski G, Meiler J, König GM, Kostenis E, Lede V, Marnett LJ and Schöneberg T
Prostaglandin E2 glyceryl ester is an endogenous agonist ot the nucleotide receptor P2Y6
Sci. Rep., 7, 2380, doi: 10.1038/s41598-017-02414-8

Kanarak AM, Wagner A, Küppers J, Gütschow M, Postina R and Kojro E
Crosstalk between angiotensin and the nonamyloidogenic pathway of Alzheimer´s amyloid precursor protein
FEBS J, 284, 742, doi: 10.1111/febs.14015

Canton J, Schlam D, Breuer C, Gütschow M, Glogauer M, Grinstein S
Calcium-sensing receptors signal constitutive macropinocytosis and facilitate the uptake of NOD2 ligands in macrophages
Nat. Commun., 7, 11284, doi:  10.1038/ncomms11284

Kranawetvogl A, Küppers J, Gütschow M, Worek F, Thiermann H, Elsinghorst PW, John H. Identification of novel disulfide adducts between the thiol containing leaving group of the nerve agent VX and cysteine containing tripeptides derived from human serum albumin. Drug Test Anal. 2017 Aug;9(8):1192-1203. doi: 10.1002/dta.2144. Epub 2017 Mar 3. PMID: 27935238.

Klose CSN, Mahlakõiv T, Moeller JB, Rankin LC, Flamar AL, Kabata H, Monticelli LA, Moriyama S, Putzel GG, Rakhilin N, Shen X, Kostenis E, König GM, Senda T, Carpenter D, Farber DL, Artis D. The neuropeptide neuromedin U stimulates innate lymphoid cells and type 2 inflammation. Nature. 2017 Sep 14;549(7671):282-286. doi: 10.1038/nature23676. Epub 2017 Sep 6. PMID: 28869965; PMCID: PMC6066372.

2016

Bolognini D, Moss CE, Nilsson K, Petersson AU, Donnelly I, Sergeev E,  König GM, Kostenis E, Kurowska-Stolarska M, Miller A, Dekker N, Tobin AB, Milligan G
A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias
J Biol Chem., 291(36), 18915-32, doi: 10.1074/jbc.M116.736157

Chang GW, Hsiao CC, Peng YM, Vieira Braga FA, Kragten NA, Remmerswaal EB, van de Garde MD, Straussberg R, König GM, Kostenis E, Knäuper V, Meyaard L, van Lier RA, van Gisbergen KP, Lin HH, Hamann J
The adhesion G protein-coupled receptor GPR56/ADGRG1 is an inhibitory receptor on human NK cells
Cell Rep., 15(8), 1757-70, doi: 10.1016/j.celrep.2016.04.053

Bradley SJ K, Wiegmann CH, Iglesias MM, Kong KC, Butcher AJ, Plouffe B, Goupil E, Bourgognon JM, Macedo-Hatch T, LeGouill C, Russel K, Laporte SA, König GM, Kostenis E, Bouvier M, Chung KF, Amrani Y and Tobin AB
Mapping physiological G protein-coupled receptor signaling pathways reveals a role for receptor phosphorylation in airway contraction
PNAS, 113(16), 4524-29 doi: 10.1073/pnas.1521706113

Carlier A, Fehr L, Pinto-Carbó M, Schäberle T, Reher R, Dessein S, König G, Eberl L
The genome analysis of Candidatus Burkholderia crenata reveals that secondary metabolism may be a key function of the Ardisia crenata leaf nodule symbiosis
Environ Microbiol. 18(8):2507-22. doi: 10.1111/1462-2920.13184. Epub 2016 Jan 21. PMID: 26663534.

Canton J, Schlam D, Breuer C, Gütschow M, Glogauer M, Grinstein S. Calcium-sensing receptors signal constitutive macropinocytosis and facilitate the uptake of NOD2 ligands in macrophages. Nat Commun. 2016 Apr 6;7:11284. doi: 10.1038/ncomms11284. PMID: 27050483; PMCID: PMC4823870.