Koeck, Zoe and Schnelle, Kilian and Persechino, Margherita and Umbach, Simon and Schihada, Hannes and Januliene, Dovile and Parey, Kristian and Pockes, Steffen and Kolb, Peter and Doetsch, Volker and Moeller, Arne and Hilger, Daniel and Bernhard, Frank (2024) Cryo-EM structure of cell-free synthesized human histamine 2 receptor/Gs complex in nanodisc environment. NATURE COMMUNICATIONS, 15 (1): 1831. ISSN 2041-1723
Full text not available from this repository. (Request a copy)Abstract
Here we describe the cryo-electron microscopy structure of the human histamine 2 receptor (H2R) in an active conformation with bound histamine and in complex with G(s) heterotrimeric protein at an overall resolution of 3.4 & Aring;. The complex was generated by cotranslational insertion of the receptor into preformed nanodisc membranes using cell-free synthesis in E. coli lysates. Structural comparison with the inactive conformation of H2R and the inactive and G(q)-coupled active state of H1R together with structure-guided functional experiments reveal molecular insights into the specificity of ligand binding and G protein coupling for this receptor family. We demonstrate lipid-modulated folding of cell-free synthesized H2R, its agonist-dependent internalization and its interaction with endogenously synthesized H1R and H2R in HEK293 cells by applying a recently developed nanotransfer technique.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | MEMBRANE-PROTEINS; INTERNATIONAL UNION; EXPRESSION; H-1; INSERTION; DOCKING; PALMITOYLATION; PHARMACOLOGY; ACTIVATION; INSIGHTS |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 28 Jan 2026 06:00 |
| Last Modified: | 28 Jan 2026 06:00 |
| URI: | https://pred.uni-regensburg.de/id/eprint/65093 |
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