ORCID: https://orcid.org/0000-0003-2259-9002
SCOPUS ID: 57208886656
Peer reviewed articles
37 Mechanism and function of GPR3 regulated by a negative allosteric modulator. Geng Chen, Jana Blahova, Nico Staffen, Harald Hübner, Nadja Nunhöfer, Chen Qiu, Peter Gmeiner*, Dorothee Weikert*, Yang Du*, Jun Xu* Nat. Commun. 2025, 16, 7988. DOI: 10.1038/s41467-025-63422-1
36 Discovery of a functionally selective serotonin receptor (5-HT1AR) agonist for the treatment of pain. Annika Ullrich, Johannes Schneider, Joao M. Braz, Eduard Neu, Nico Staffen, Markus Stanek, Jana Blahova, Tamsanqa Hove, Tamara Albert, Stefan Löber, Karnika Bhardwaj, Sian Rodriguez-Rosado, Elissa Fink, Tim Rasmussen, Harald Hübner, Asuka Inoue, Brian K. Shoichet, Allan I. Basbaum*, Bettina Böttcher*, Dorothee Weikert*, Peter Gmeiner* Sci. Adv. 11, 2025, 25 eadv9267. DOI: 10.1126/sciadv.adv9267
35 Synthesis and characterization of photoswitchable covalent ligands for the β2-adrenoceptor Ulrike Wirth, Eduard Neu, Davide Provasi, Steffen Feustel, Maximilian F. Schmidt, Harald Hübner, Dorothee Weikert, Marta Filizola*, Burkhard König*, Peter Gmeiner* Angew. Chem. Int. Ed. 2025, e2024240038, DOI: 10.1002/anie.202424038
34 A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR. Lior Peri, Donna Maatzov, Dominic R. Huxley, Alon Rainish, Fabrizio Fierro, Liel Sapir, Tara Pfeiffer, Lukas Waterloo, Harald Huebner, Yoav Peleg, Peter Gmeiner, Peter J. McCormick, Dorothee Weikert*, Masha Y. Niv*, Moran Shalev-Benami*. Nat. Commun. 2024, 15, 9991. DOI: 10.1038/s41467-024-54157-6
33 Development of a fluorescent ligand for the intracellular allosteric binding site of the neurotensin receptor 1. Hannah Vogt, Patrick Shinkwin, Max E. Huber, Nico Staffen, Harald Huebner, Peter Gmeiner, Matthias Schiedel, Dorothee Weikert*. ACS Pharmacol. Transl. Sci. 2024, 7, 1533-1545. DOI: 10.1021/acsptsci.4c00086
32 The beer component hordenine inhibits alcohol addiction-associated behaviours in mice. Yan Li, Christina Vogel, Liubov S. Kalinichenko, Harald Huebner, Dorothee Weikert, Natascha Schaefer, Peter Gmeiner, Carmen Villmann, Monika Pischetsrieder, Christian P. Mueller*. Addict. Biol. 2023, 28, 8, e13305. DOI: 10.1111/adb.13305
31 Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief. Alan Hegron, Chloe J. Peach, Raquel Tonello, Philipp Seemann, Shavonne Teng, Rocco Latorre, Harald Huebner, Dorothee Weikert, Jeanette Rientjes, Nicholas A. Veldhuis, Daniel P. Poole, Dane D. Jensen, Alex R. B. Thomsen, Brian L. Schmidt, Wendy L. Imlach, Peter Gmeiner, Nigel W. Bunnett*. Proc. Natl. Acad. Sci. U.S.A. 2023, 120, 22, e2220979120. DOI: 10.1073/pnas.2220979120
30 Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands. Fabrizio Fierro, Lior Peri, Harald Huebner, Alina Tabor-Schkade, Lukas Waterloo, Stefan Loeber, Tara Pfeiffer, Dorothee Weikert, Tamir Dingjan, Eitan Margulis, Peter Gmeiner*, Masha Y Niv.* Cell. Mol. Life Sci. 2023, 80, 114. DOI: 10.1007/s00018-023-04765-0
29 Discovery of 2-aminopyrimidines as potent agonists for the bitter taste receptor TAS2R14. Lukas Waterloo, Harald Huebner, Fabrizio Fierro, Tara Pfeiffer, Regine Brox, Stefan Loeber, Dorothee Weikert, Masha Y. Niv*, Peter Gmeiner*. J. Med. Chem. 2023, 66, 5, 3499-3521. DOI: 10.1021/acs.jmedchem.2c01997
28 Phosphoproteomic analysis of dopamine D2 receptor signaling reveals interplay of G protein- and beta-arrestin-mediated effects. Deborah Wenk, Shahbaz Khan, Vladimir Ignatchenko, Harald Huebner, Peter Gmeiner, Dorothee Weikert, Monika Pischetsrieder, Thomas Kislinger*. J. Proteome Res. 2023, 22, 1, 259-271. DOI: 10.1021/acs.jproteome.2c00707
27 Small molecule tools to study cellular target engagement for the intracellular allosteric binding site of GPCRs. Max E. Huber, Lara Toy, Maximilian F. Schmidt, Dorothee Weikert, Matthias Schiedel*. Chem. Eur. J., 2023, 29, e202202565. DOI: 10.1002/chem.202202565
26 Analysis of hyperforin (St. John’s wort) action at TRPC6 channel leads to the development of a new class of antidepressant drugs. Yamina El Hamdaoui, Fang Zheng, Nikolas Fritz, Lian Ye, Mai A. Tran, Kevin Schwickert, Tanja Schirmeister, Albert Braeuning, Dajana Lichtenstein, Ute A. Hellmich, Dorothee Weikert, Markus Heinrich, Giulia Treccani, Michael K. E. Schäfer, Gabriel Nowak, Bernd Nürnberg, Christian Alzheimer, Christian P. Müller*, Kristina Friedland*. Mol. Psychiatry 2022, 27, 5070–5085. DOI: 10.1038/s41380-022-01804-3
25 Structure-based discovery of nonopioid analgesics acting through the alpha2A-adrenergic receptor. Elissa A. Fink, Jun Xu, Harald Huebner, Joao M. Braz, Philipp Seemann, Charlotte Avet, Veronica Craik, Dorothee Weikert, Maximilian F. Schmidt, Chase M. Webb, Nataliya A. Tolmachova, Yurii S. Moroz, Xi-Ping Huang, Chakrapani Kalyanaraman, Stefan Gahbauer, Geng Chen, Zheng Liu, Matthew P. Jacobson, John J. Irwin, Michel Bouvier*, Yang Du*, Brian K. Shoichet*, Allan I. Basbaum*, Peter Gmeiner*. Science 2022, 377, eabn7065. DOI: 10.1126/science.abn7065
24 Fluorescent ligands targeting the intracellular allosteric binding site of the chemokine receptor CCR2. Lara Toy, Max E. Huber, Maximilian F. Schmidt, Dorothee Weikert, Matthias Schiedel*. ACS Chem. Biol., 2022, 17 2142-22152. DOI: 10.1021/acschembio.2c00263
23 Structural insights into ligand recognition, activation, and signaling of the alpha2A adrenergic receptor. Jun Xu, Sheng Cao, Harald Huebner, Dorothee Weikert, Geng Chen, Qiuyuan Lu, Daopeng Yuan*, Peter Gmeiner*, Zheng Liu*, Yang Du*. Sci. Adv. 2022, 8, eabj5347. DOI: 10.1126/sciadv.abj5347
22 A chemical biology toolbox targeting the intracellular binding site of CCR9: Fluorescent ligands, new drug leads and PROTACs. Max E. Huber, Lara Toy, Maximilian F. Schmidt, Hannah Vogt, Julian Budzinski, Martin F. J. Wiefhoff, Nicole Merten, Evi Kostenis, Dorothee Weikert, Matthias Schiedel*, Angew. Chem. Int. Ed. 2022, 61, e202116782. DOI: 10.1002/anie.202116782
21 Functional reconstitution of dopamine D2 receptor into a supported model membrane in a nanometric confinement. Rurika Nagai, Ayane Sugimachi, Yasushi Tanimoto, Kenichi G. N. Suzuki, Fumio Hayashi, Dorothee Weikert, Peter Gmeiner, Rinshi S. Kasai*, Kenichi Morigaki*. Adv. Biology 2021, 5, 2100636. DOI: 10.1002/adbi.202100636
20 Bivalent ligands promote endosomal trafficking of the dopamine D3 receptor-neurotensin receptor 1 heterodimer. Julian Budzinski, Simone Maschauer, Hiroyuki Kobayashi, Pierre Couvineau, Hannah Vogt, Peter Gmeiner, Anna Roggenhofer, Olaf Prante, Michel Bouvier*, Dorothee Weikert*. Commun. Biol. 2021, 4, 1062. DOI: 10.1038/s42003-021-02574-4
19 Functionally selective activation of the dopamine receptor D2 is mirrored by the protein expression profiles. Deborah Wenk, Vladimir Ignatchenko, Andrew Macklin, Harald Hübner, Peter Gmeiner, Dorothée Weikert, Monika Pischetsrieder*, Thomas Kislinger. Sci. Rep. 2021, 11, 3501. DOI: 10.1038/s41598-021-83038-x
18 Homobivalent Dopamine D2 Receptor Ligands Modulate the Dynamic Equilibrium of D2 Monomers and Homo- and Heterodimers. Tamara Ullmann, Marie Gienger, Julian Budzinski, Jan Hellmann, Harald Hübner, Peter Gmeiner*, Dorothee Weikert*. ACS Chem. Biol. 2021, 16, 371-379. DOI: 10.1021/acschembio.0c00895
17 Fluorescent ligands for dopamine D2/D3 receptors. Anni Allikalt, Nirupam Purkayastha, Khajidmaa Flad, Maximilian F. Schmidt, Alina Tabor, Peter Gmeiner, Harald Hübner, Dorothee Weikert*. Sci. Rep. 2020, 10, 21842. DOI: 10.1038/s41598-020-78827-9
16 Structure-based development of a subtype-selective orexin 1 receptor antagonist. Jan Hellmann, Matthäus Drabek, Jie Yin, Jakub Gunera, Theresa Pröll, Frank Kraus, Christopher J. Langmead, Harald Hübner, Dorothee Weikert, Peter Kolb*, Daniel M. Rosenbaum*, Peter Gmeiner*.PNAS 2020, 117, 18059-18067. DOI: 10.1073/pnas.2002704117
15 Discovery of novel nonpeptidic PAR2 ligands Ilona Klösel, Maximilian F. Schmidt, Jonas Kaindl, Harald Hübner, Dorothee Weikert, Peter Gmeiner*. ACS Med. Chem. Lett. 2020, 11, 1316-1323. DOI: 10.1021/acsmedchemlett.0c00154
14 Rational design of agonists for bitter taste receptor TAS2R14: from modeling to bench and back. Antonella Di Pizio, Lukas A. W. Waterloo, Regine Brox, Stefan Löber, Dorothee Weikert, Maik Behrens, Peter Gmeiner*, Masha Y. Niv*. Cell. Mol. Life Sci. 2020, 77, 531-542. DOI: 10.1007/s00018-019-03194-2
13 Differential allosteric modulation within dopamine D2R – neurotensin NTS1R and D2R – serotonin 5-HT2AR receptor complexes gives bias to intracellular calcium signalling. Michael Plach, Thorsten Schäfer, Dasiel Oscar Borroto-Escuela, Dorothée Weikert, Peter Gmeiner, Kjell Fuxe, Kristina Friedland*. Sci. Rep. 2019, 9, 16312. DOI: 10.1038/s41598-019-52540-8
12 Hybridization of β-adrenergic agonists and antagonists confers G protein bias. Markus Stanek, Louis-Philippe Picard, Maximilian F. Schmidt, Jonas M. Kaindl, Harald Hübner, Michel Bouvier, Dorothee Weikert*, Peter Gmeiner*. J. Med. Chem. 2019, 62, 5111-5131. DOI: 10.1021/acs.jmedchem.9b00349
11 Structure-based design and discovery of new M2 receptor agonists. Inbar Fish, Anne Stößel, Katrin Eitel, Celine Valant, Sabine Albold, Harald Huebner, Dorothee Möller, Mary J. Clark, Roger K. Sunahara, Arthur Christopoulos, Brian K. Shoichet*, Peter Gmeiner*. J. Med. Chem. 2017, 60, 9239-9250. DOI: 10.1021/acs.jmedchem.7b01113
10 Visualization of ligand-induced dopamine D2S and D2L receptor internalization by TIRF microscopy. Alina Tabor, Dorothee Möller, Harald Hübner, Johannes Kornhuber, Peter Gmeiner*. Sci. Rep. 2017, 7, 10894. DOI: 10.1038/s41598-017-11436-1
9 Structure-guided screening for functionally selective D2 dopamine receptor ligands from a virtual chemical library. Barbara Männel, Mariama Jaiteh, Alexey Zeifman, Alena Randakova, Dorothee Möller, Harald Hübner, Peter Gmeiner*, Jens Carlsson*. ACS Chem. Biol. 2017, 12, 2652-2661. DOI: 10.1021/acschembio.7b00493
8 β-Arrestin biased dopamine D2 receptor partial agonists: synthesis and pharmacological evaluation. Barbara Männel, Harald Hübner, Dorothée Möller, Peter Gmeiner*. Bioorg. Med. Chem. 2017, 25, 5613-5628. DOI: 10.1016/j.bmc.2017.08.037
7 Hydroxy-substituted heteroarylpiperazines: Novel scaffolds for β-arrestin-biased D2R agonists. Barbara Männel, Daniela Dengler, Jeremy Shonberg, Harald Hübner, Dorothee Möller, Peter Gmeiner*. J. Med. Chem. 2017, 60, 4693-4713. DOI: 10.1021/acs.jmedchem.7b00363
6 Discovery of G protein-biased dopaminergics with a pyrazolo[1,5-a]pyridine substructure. Dorothee Möller, Ashutosh Banerjee, Taygun C. Uzuneser, Marika Skultety, Tobias Huth, Bianca Plouffe, Harald Hübner, Christian Alzheimer, Kristina Friedland, Christian P. Müller, Michel Bouvier*, Peter Gmeiner*. J. Med. Chem. 2017, 60, 2908-2929. DOI: 10.1021/acs.jmedchem.6b01857
5 Structure-guided development of heterodimer-selective GPCR ligands. Harald Hübner, Tamara Schellhorn, Marie Gienger, Carolin Schaab, Jonas Kaindl, Laurin Leeb, Timothy Clark, Dorothee Möller*, Peter Gmeiner*. Nat. Commun. 2016, 7, 12298. DOI: 10.1038/ncomms12298
4 Arrestin-bound rhodopsin: a molecular structure and its impact on the development of biased GPCR ligands. / Die Rhodopsin-Arrestin-Kristallstruktur und ihre Bedeutung für die Entwicklung funktionell selektiver GPCR-Wirkstoffe. Dorothee Möller, Peter Gmeiner*. Angew. Chem. Int. Ed. 2015, 54, 13166-13168. DOI: 10.1002/anie.201507724. Angew. Chem. 2015, 127, 13362-13364. DOI: 10.1002/ange.201507724
3 1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: quantitative structure selectivity investigations, docking, synthesis and biological evaluation. Dorothee Möller, Ismail Salama, Ralf C. Kling, Harald Hübner, Peter Gmeiner*, Bioorg. Med. Chem. 2015, 23, 6195-6209. DOI: 10.1016/j.bmc.2015.07.050
2 Functionally selective dopamine D2, D3 receptor partial agonists. Dorothee Möller, Ralf C. Kling, Marika Skultety, Kristina Leuner, Harald Hübner, and Peter Gmeiner*, J. Med. Chem. 2014, 57, 4861-4875. DOI: 10.1021/jm5004039
1 Pharmacological profile of 2-bromoterguride at human dopamine D2, porcine serotonin 5-HT2A and α2C-adrenergic receptors, and its antipsychotic-like effects in rats. Florian Jantschak, Jan Brosda, Robert T. Franke, Heidrun Fink, Dorothee Möller, Harald Hübner, Peter Gmeiner, and Heinz H. Pertz*, JPET 2013, 347, 57-68. DOI: 10.1124/jpet.113.205997
Preprints
6 The role of intrinsically disordered domains in regulating G protein-coupled receptor signaling. Xu, R. Qiu, A. M. Garces, H. Hübner, X. Xu, D. Weikert, P., M. T. Lerch, B. K. Kobilka BioRxiv 2025, doi: 10.1101/2025.09.10.675278
5 Intracellular binding pocket revealed in the human bitter taste receptor TAS2R14. L. Peri, D. Matzov, D. R. Huxley, A. Rainish, F. Fierro, L. Sapir, T. Pfeiffer, L. Waterloo, H. Hübner, D. Weikert, Y. Peleg, P. Gmeiner, P. McCormick, M. Y. Niv, M. Shalev-Benami BioRxiv 2024, doi: 10.1101/2024.04.10.588278
4 Discovery of a functionally selective serotonin 5-HT1A receptor agonist for the treatment of pain. A. Ullrich, J. Schneider, J. M. Braz, E. Neu, N. Staffen, M. Stanek, J. Bláhová, T. Hove, T. Albert, A. Allikalt, S. Löber, K. Bhardwaj, S. Rodriguez-Rosado, E. Fink, T. Rasmussen, H. Hübner, A. Inoue, B. K. Shoichet, A. J. Basbaum, B. Böttcher, D. Weikert, P. Gmeiner BioRxiv 2023, doi: 10.1101/2023.09.11.557127
3 Discovery of 2-aminopyrimidines as potent agonists for the bitter taste receptor TAS2R14. L. Waterloo, T. Pfeiffer, H. Hübner, F. Fierro, R. Brox, S. Löber, D. Weikert, M. Y. Niv, P. Gmeiner ChemRxiv 2022, doi: 10.26434/chemrxiv-2022-7zc11
2 Fluorescent ligands targeting the intracellular allosteric binding site of the chemokine receptor CCR2. L. Toy, M. E. Huber, M. F. Schmidt, D. Weikert, M. Schiedel ChemRxiv 2022, doi: 10.26434/chemrxiv-2022-wg6cg-v3
1 Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands. F. Fierro, L. Peri, H. Hübner, A. Tabor-Schkade, L. Waterloo, S. Löber, T. Pfeiffer, D. Weikert, T. Dingjan, E. Margulis, P. Gmeiner, M. Y. Niv BioRxiv 2022, doi: 10.1101/2022.11.24.517821
Invited talks & Short Presentations
- 2026: Frontiers in Medicinal Chemistry, Münster, Germany „Harnessing Non-Canonical GPCR Binding Pockets for Drug Development“
- 2025: DPhG Annual Meeting, Freiburg, Germany “Unlocking bitter taste: Ligand recognition by the bitter taste receptor TAS2R14”
- 2025: Frontiers in Medicinal Chemistry (GDCh), Erlangen, Germany “Elucidation of non-canonical GPCR binding pockets employing nanoBRET”
- 2024: Lunchbreak Seminar, Emil-Fischer-Graduate School, FAU NeW, Erlangen, Germany “1+1 = 2? Studies on GPCR dimer signal transduction”
- 2021: Online-flash presentation, ERNEST – European Research Network on Signal Transduction, Bari, Italy “Bivalent ligands promote dopamine D3 receptor/neurotensin receptor 1 heterodimer-selective trafficking”
- 2019: Flash presentation, GPCR Workshop, Kona, Hawaii, USA “Orexin receptor antagonists with selectivity for OX1R over OX2R”
- 2019: DPhG Annual Meeting, Heidelberg, Germany “Bivalent ligands targeting dopamine receptor heterodimers”
- 2019: Academia meets HTB, Boehringer Ingelheim, Biberach, Germany “Biological evaluation of heterodimer-specific GPCR ligands“
- 2018: Early Career Scientist Forum on GPCR Signal Transduction (ECSF-GPCR), Berlin, Germany “Conformationally restricted adrenaline analogs selectively activating β2-adrenoreceptors“
- 2017: Flash presentation, GPCR Workshop, Kona, Hawaii, USA “Conformationally restricted adrenaline analogs selectively activating β2-AR“
- 2016: EU COST action GLISTEN: Meeting, Erlangen, Germany “D2R/NTS1R heterodimer-selective ligands“
- 2016: Festakt zur Zeugnisübergabe, Studiengang Pharmazie/Lebensmittelchemie, Erlangen, Germany „Struktur und Funktion G-Protein gekoppelter Rezeptoren“
- 2014: EU COST action GLISTEN: Spring Meeting, Barcelona, Spain “Biased ligands for Dopamine D2/D3 receptors”