The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality
The availability of solid state structures of opioid receptors has prompted us to reconsider a crucial question concerning bioactive peptides: can their conformation be studied without any knowledge of the structure of their receptors? The meaning of this query depends mainly on the extreme conforma...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2014-10-01
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| Series: | Frontiers in Molecular Biosciences |
| Subjects: | |
| Online Access: | http://journal.frontiersin.org/Journal/10.3389/fmolb.2014.00014/full |
| _version_ | 1819236991234998272 |
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| author | Domenico eSanfelice Piero Andrea Temussi |
| author_facet | Domenico eSanfelice Piero Andrea Temussi |
| author_sort | Domenico eSanfelice |
| collection | DOAJ |
| description | The availability of solid state structures of opioid receptors has prompted us to reconsider a crucial question concerning bioactive peptides: can their conformation be studied without any knowledge of the structure of their receptors? The meaning of this query depends mainly on the extreme conformational flexibility of small peptides, and amongst them the best known of bioactive peptides, enkephalin. All solution studies of enkephalin hint at an inextricable mixture of quasi isoenergetic conformers. In this study we refer to the only NMR work that yielded inter-residue NOEs, performed at very low temperature. We show that the conformers found in the equilibrium mixture at low temperature are indeed compatible with a good occupancy of the receptor active site. |
| first_indexed | 2024-12-23T13:13:13Z |
| format | Article |
| id | doaj.art-c5e078e174fc4bdd82106802daf24e45 |
| institution | Directory Open Access Journal |
| issn | 2296-889X |
| language | English |
| last_indexed | 2024-12-23T13:13:13Z |
| publishDate | 2014-10-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Molecular Biosciences |
| spelling | doaj.art-c5e078e174fc4bdd82106802daf24e452022-12-21T17:45:41ZengFrontiers Media S.A.Frontiers in Molecular Biosciences2296-889X2014-10-01110.3389/fmolb.2014.00014102364The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming realityDomenico eSanfelice0Piero Andrea Temussi1MRC NIMRUniversità di Napoli Federico IIThe availability of solid state structures of opioid receptors has prompted us to reconsider a crucial question concerning bioactive peptides: can their conformation be studied without any knowledge of the structure of their receptors? The meaning of this query depends mainly on the extreme conformational flexibility of small peptides, and amongst them the best known of bioactive peptides, enkephalin. All solution studies of enkephalin hint at an inextricable mixture of quasi isoenergetic conformers. In this study we refer to the only NMR work that yielded inter-residue NOEs, performed at very low temperature. We show that the conformers found in the equilibrium mixture at low temperature are indeed compatible with a good occupancy of the receptor active site.http://journal.frontiersin.org/Journal/10.3389/fmolb.2014.00014/fullPeptidesreceptorsDockingNMROpioids |
| spellingShingle | Domenico eSanfelice Piero Andrea Temussi The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality Frontiers in Molecular Biosciences Peptides receptors Docking NMR Opioids |
| title | The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality |
| title_full | The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality |
| title_fullStr | The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality |
| title_full_unstemmed | The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality |
| title_short | The conformation of enkephalin bound to its receptor: An ‘elusive goal’ becoming reality |
| title_sort | conformation of enkephalin bound to its receptor an elusive goal becoming reality |
| topic | Peptides receptors Docking NMR Opioids |
| url | http://journal.frontiersin.org/Journal/10.3389/fmolb.2014.00014/full |
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