Detection of an Antagonist Bound to the Neurokinin a Receptor in Styrene–Maleic Acid Lipid Particles by <sup>19</sup> F Ultrafast Magic‐Angle Spinning Nuclear Magnetic Resonance Spectroscopy
G protein-coupled receptors (GPCRs) are major pharmacological targets, with ≈34% of FDA-approved drugs acting on this protein family. The frequent incorporation of fluorine into small-molecule ligands enables the use of <sup>19</sup>F nuclear magnetic resonance (NMR) as a sensitive and site-specific method to probe ligand behaviour. In this case study, we investigate the fluorinated antagonist GR159897 bound to the membrane-embedded neurokinin A receptor reconstituted in detergent-free styrene-maleic acid lipid particles (SMALPs) using <sup>19</sup>F ultrafast magic-angle spinning (MAS) solid-state NMR. We demonstrate that the environmental sensitivity of <sup>19</sup>F NMR resolves distinct ligand populations within the SMALP system and enables detection of receptor-associated ligand, highlighting the utility of <sup>19</sup>F solid-state NMR for probing GPCR-ligand interactions.
Authors
- Clemens Glaubitz (ORCID: https://orcid.org/0000-0002-3554-6586)
- Aditya Prasad Patra
- Christoph Reinhart (ORCID: https://orcid.org/0000-0002-3580-1807)
- Johanna Becker‐Baldus (ORCID: https://orcid.org/0000-0003-1995-7323)
- Samuel Seidl
- Chengkang Li
- Stefanie Kaiser
Institutions
- Goethe University Frankfurt (DE)
- University of Massachusetts Chan Medical School (US)
- Frankfurt Institute for Advanced Studies (DE)
- Max Planck Institute of Biophysics (DE)
- University Children's Hospital Zurich (CH)
- Allgemeine Gewerbeschule Basel (CH)
Publication Details
- Journal
- ChemBioChem
- Published
- 2026-03-23
- DOI
- https://doi.org/10.1002/cbic.202500963
- Primary Topic
- Advanced NMR Techniques and Applications
- Type
- article
- Field-Weighted Citation Impact
- 0.00