Journal article
Probing the environment of neurotensin whilst bound to the neurotensin receptor by solid state NMR.
- Abstract:
- A functionally active analogue of neurotensin, neurotensin(8-13), has been observed whilst bound to the agonist-binding site of the rat neurotensin receptor by nuclear magnetic resonance (NMR). Through the application of slow magic angle sample spinning and high-power proton decoupling, sufficient resolution and sensitivity were obtained in the carbon-13 spectrum to allow an assignment of many of the side chain resonances arising from uniformly carbon-13/nitrogen-15-labelled neurotensin(8-13) whilst bound to the neurotensin receptor. Significant perturbations in carbon-13 chemical shift were observed upon the binding of the neurotensin(8-13) to the receptor. Most importantly significant shifts were observed in both the carboxy terminus and tyrosine side chain of the neurotensin(8-13), suggesting that these sites are important in the interaction of the neurotensin with the agonist-binding site on the neurotensin receptor. Conversely, no perturbations were observed for the carbon-13 sites within the guanidinium groups of the arginine side chains, indicating little interaction with the receptor-binding site, or a shielding of the local environment by the surrounding nitrogen atoms. These NMR observations lend further support to previous structure-activity studies, site-directed mutagenesis and modelling studies of the agonist-binding site of the neurotensin receptor, from which the same specific residues for which NMR perturbations were observed are important for neurotensin receptor activation by neurotensin.
- Publication status:
- Published
Actions
Access Document
- Publisher copy:
- 10.1016/s0014-5793(02)02656-x
Authors
- Journal:
- FEBS letters More from this journal
- Volume:
- 518
- Issue:
- 1-3
- Pages:
- 111-115
- Publication date:
- 2002-05-01
- DOI:
- EISSN:
-
1873-3468
- ISSN:
-
0014-5793
- Language:
-
English
- Keywords:
- Pubs id:
-
pubs:100595
- UUID:
-
uuid:1749b06c-6d63-41ce-8724-df7594b5c185
- Local pid:
-
pubs:100595
- Source identifiers:
-
100595
- Deposit date:
-
2012-12-19
- ARK identifier:
Terms of use
- Copyright date:
- 2002
If you are the owner of this record, you can report an update to it here: Report update to this record