Dr. Anette Kaiser

Dr. Anette Kaiser

+49 341 97 36839

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Evolution of neuropeptide GPCR specificity and signaling

G protein-coupled receptors are a main pharmacological target as they are involved in numerous physiological and pathophysiological functions. Understanding the function and regulation of these complex proteins is key to the design of specific and efficacious pharmaceuticals. For instance, peptide-binding GPCRs are involved in neuroendocrine regulation, pain perception and regulation of energy homeostasis. Reflecting their essential physiologic functions, many neuropeptide GPCR systems are conserved down to basal animals. This deep evolutional conservation also opens avenues to study common and individual principles of receptor function. Moreover, relatively simple model organism might be used to study aspects of receptor signaling or test compounds in an in vivo context.

My research interest is how ligand specificity is accomplished in neuropeptide GPCRs, and how this translates into conformational changes that allow (selective) coupling to and activation of intracellular effector proteins. To address these questions, I use rational mutagenesis of receptor and ligands guided by structural models and measure multiple downstream pathways in cellulo. Moreover, protein-protein interactions are analyzed in cellular contexts to obtain spatio-temporal insights into receptor signaling.



Laugwitz Jeanette M, Haeri Haleh H, Kaiser Anette, Krug Ulrike, Hinderberger Dariush, Beck-Sickinger Annette G, Schmidt Peter. (2020) Probing the Y2 Receptor on Transmembrane, Intra- and Extra-Cellular Sites for EPR Measurements.  Molecules., 25(18):E4143.AbstractPDF
Krug Ulrike, Gloge Anika, Schmidt Peter, Becker-Baldus Johanna, Bernhard Frank, Kaiser Anette, Montag Cindy, Gauglitz Marcel, Vishnivetskiy Sergey A, Gurevich Vsevolod V, Beck-Sickinger Annette G, Glaubitz Clemens, Huster Daniel. (2020) The Conformational Equilibrium of the Neuropeptide Y2 Receptor in Bilayer Membranes.  Angew Chem Int Ed Engl. doi: 10.1002/anie.202006075AbstractPDF
Ziffert Isabelle, Kaiser Anette, Hoppenz Paul, Mörl Karin, Beck-Sickinger Annette G. (2020) Shuttling of Peptide-Drug Conjugates by G Protein-Coupled Receptors Is Significantly Improved by Pulsed Application.  ChemMedChem. doi: 10.1002/cmdc.202000490.AbstractPDF
Ziffert Isabelle, Kaiser Anette, Babilon Stefanie, Mörl Karin, Beck-Sickinger Annette G. (2020) Unusually persistent Gαi-signaling of the neuropeptide Y2 receptor depletes cellular Gi/o pools and leads to a Gi-refractory state. Cell Commun Signal., 18(1):49 AbstractPDF
Kaiser Anette, Wanka Lizzy, Ziffert Isabelle, Beck-Sickinger Annette G. (2020) Biased agonists at the human Y1 receptor lead to prolonged membrane residency and extended receptor G protein interaction. Cell Mol Life Sci. doi: 10.1007/s00018-019-03432-7. AbstractPDF


Miron M. Gershkovich, Victoria E. Groß, Anette Kaiser, Simone Prömel (2019) Pharmacological and Functional Similarities of the Human Neuropeptide Y System in C. Elegans Challenges Phylogenetic Views on the FLP/NPR system. Cell Commun. Signal., 17:123.AbstractPDF
Esben M. Bech, Anette Kaiser, Kathrin Bellmann-Sickert, Søren S.-R. Nielsen, Kasper K. Sørensen, Lisbeth Elster, Nikos Hatzakis, Søren L. Pedersen, Annette G. Beck-Sickinger, and Knud J. Jensen (2019) Half-Life Extending Modification of Peptide YY(3-36) Direct Receptor-Mediated InternalizationAbstractPDF
Lisa Maria Kögler, Jan Stichel, Anette Kaiser, Annette G. Beck-Sickinger (2019) Cell-Free Expression and Photo-Crosslinking of the Human Neuropeptide Y2 Receptor. Front. Pharmacol., 10, 176.AbstractPDF
Brian J. Bender, Gerrit Vortmeier, Stefan Ernicke, Mathias Bosse, Anette Kaiser, Sylvia Els-Heindl, Ulrike Krug, Annette G. Beck-Sickinger, Jens Meiler, Daniel Huster (2019) Structural Model of Ghrelin Bound to its G Protein-Coupled Receptor. Structure, 27, 537-544.AbstractPDF


Lizzy Wanka, Stefanie Babilon, Anette Kaiser, Karin Mörl, Annette G. Beck-Sickinger (2018) Different mode of arrestin-3 binding at the human Y1 and Y2 receptor. Cell. Signal., 50, 58-71.AbstractPDF
Zhenlin Yang, Shuo Han, Max Keller, Anette Kaiser, Brian J. Bender, Mathias Bosse, Kerstin Burkert, Lisa M. Kögler, David Wifling, Guenther Berndhardt, Nicole Plank, Timo Littmann, Peter Schmidt, Cuiying Yi, Beibei Li, Sheng Ye, Rongguang Zhang, Bo Xu, Dan Larhammar, Raymond C. Stevens, Daniel Huster, Jens Meiler, Qiang Zhao, Annette G. Beck-Sickinger, Armin Buschauer, Beili Wu (2018) Structural basis of ligand binding modes at the nuropeptide Y Y1 Receptor. Nature, 556, 520-524.AbstractPDF
Anette Kaiser, Caroline Hempel, Lizzy Wanka, Mario Schubert, Heidi E. Hamm, Annette G. Beck-Sickinger (2018) G protein pre-assembly rescues efficacy of W6.48 toggle mutations in neuropeptide Y2 receptors. Mol. Pharm., 93, 387-401.AbstractPDF
Peter Schmidt, Brian J. Bender, Anette Kaiser, Khushboo Gulati, Holger A. Scheidt, Heidi E. Hamm, Jens Meiler, Annette G. Beck-Sickinger, Daniel Huster (2018) Improved In Vitro Folding of the Y2 G Protein-Coupled Receptor into Bicelles. Front. Mol. Biosci., 4:100 doi:10.3389/fmolb.2017.00100. eCollection 2017.AbstractPDF


Stefanie Schrottke, Anette Kaiser, Gerrit Vortmeier, Sylvia Els-Heindl, Dennis Worm, Mathias Bosse, Peter Schmidt, Holger A. Scheidt, Annette G. Beck-Sickinger and Daniel Huster (2017) Expression, Functional Characterization, and Solid-State NMR Investigation of the G Protein-Coupled GHS Receptors in Bilayer Membranes. Sci Rep. 7, 46128.AbstractPDF
Kerstin Burkert, Tristan Zellmann, Rene Meier, Anette Kaiser, Jan Stichel, Jens Meiler, Gopi K. Mittapalli, Edward Roberts and Annette G. Beck-Sickinger (2017) A Deep Hydrophobic Binding Cavity is the Main Interaction for Different Y2R Antagonists. ChemMedChem. 12, 75-85.AbstractPDF


Anette Kaiser, Paul Müller, Tristan Zellmann, Holger A. Scheidt, Lars Thomas, Mathias Bosse, Rene Meier, Jens Meiler, Daniel Huster, Annette G. Beck-Sickinger and Peter Schmidt (2015) Unwinding of the C-Terminal Residues of Neuropeptide Y is critical for Y2 Receptor Binding and Activation. Angew. Chemie Int. Ed. 54, 7446-7449.AbstractPDF
Ria Schönauer, Anette Kaiser, Cathleen Holze, Stefanie Babilon, Johannes Koebberling, Bernd Riedl and Annette G. Beck-Sickinger (2015) Flourescently labeled adrenomedullin allows realtime monitoring of adrenomedullin receptor trafficking in living cells. J. Pept. Sci. 21, 905-912.AbstractPDF


Veronika Mäde, Kathrin Bellmann-Sickert, Anette Kaiser, Jens Meiler and Annette G. Beck-Sickinger (2014) Position and length of fatty acids strongly affect receptor selectivity pattern of human pancreatic polypeptide analogues. ChemMedChem 9, 2463-74AbstractPDF


Kristina Witte, Anette Kaiser, Peter Schmidt, Victoria Splith, Lars Thomas, Sandra Berndt, Daniel Huster and Annette G. Beck-Sickinger (2013) Oxidative In Vitro Folding of a Cysteine Deficient Variant of the G Protein-coupled Neuropeptide Y Receptor Type 2 Improves Stability at High Concentration. Biol. Chem. 394, 1045-56. AbstractPDF


Anette Schreiber, Peter Schramm, Hans-Jörg Hofmann (2011) How many hydrogen-bonded α-turns are possible? J. Mol. Model. 17, 1393-1400. AbstractPDF
letzte Änderung: 16.06.2021


Dr. Anette Kaiser
Brüderstraße 34
04103 Leipzig

Telefon: +49 341 97 36839
Telefax: +49 341 97 36909