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- W4200272020 abstract "ABSTRACT Using a discrete, intracellular 19 F-NMR probe on transmembrane helix 6 (TM6) of the Neurotensin receptor 1 (NTS1), we aim to understand how ligands and transducers modulate the receptor’s structural ensemble in solution. For apo NTS1, 19 F-NMR spectra reveal an ensemble of at least three conformational substates (one inactive and two active-like) in equilibrium that exchange on the ms-s timescale. Dynamic NMR experiments reveal that these substates follow a linear three-site exchange process that is both thermodynamically and kinetically remodeled by orthosteric ligands. As previously observed in other GPCRs, the full agonist is insufficient to completely stabilize the active-like state. The inactive substate is abolished upon coupling to β-arrestin-1 or the C-terminal helix of Gα q , which comprises ⍰60% of the GPCR/G protein interface surface area. Whereas β-arrestin-1 exclusively selects for pre-existing active-like substates, the Gα q peptide induces a new substate. Both transducer molecules promote substantial line-broadening of active-like states suggesting contributions from additional μs-ms exchange processes. Together, our study suggests i) the NTS1 allosteric activation mechanism may be alternatively dominated by induced fit or conformational selection depending on the coupled transducer, and ii) the available static structures do not represent the entire conformational ensemble observed in solution." @default.
- W4200272020 created "2021-12-31" @default.
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- W4200272020 date "2021-12-10" @default.
- W4200272020 modified "2023-09-27" @default.
- W4200272020 title "The Effect of Ligands and Transducers on the Neurotensin Receptor 1 (NTS1) Conformational Ensemble" @default.
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- W4200272020 doi "https://doi.org/10.1101/2021.12.08.471782" @default.
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