Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach
The dimeric peptide 1 (BVD-74D, as a diastereomeric mixture) is a potent and selective Neuropeptide Y Y4 receptor agonist. It represents a valuable candidate in developing traceable ligands for pharmacological studies of Y4 receptors, and as a lead compound for anti-obesity drugs. Its optically pure...
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| Format: | Article |
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American Chemical Society
2016
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| Online Access: | https://eprints.nottingham.ac.uk/34144/ |
| _version_ | 1848794783546343424 |
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| author | Liu, Mengjie Mountford, Simon J. Richardson, Rachel R. Groenen, Marleen Holliday, Nicholas D. Thompson, Philip E. |
| author_facet | Liu, Mengjie Mountford, Simon J. Richardson, Rachel R. Groenen, Marleen Holliday, Nicholas D. Thompson, Philip E. |
| author_sort | Liu, Mengjie |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | The dimeric peptide 1 (BVD-74D, as a diastereomeric mixture) is a potent and selective Neuropeptide Y Y4 receptor agonist. It represents a valuable candidate in developing traceable ligands for pharmacological studies of Y4 receptors, and as a lead compound for anti-obesity drugs. Its optically pure stereoisomers along with analogues and fluorescently labelled variants were prepared by exploiting alkene metathesis reactions. The (2R,7R)- diaminosuberoyl containing peptide, (R,R)-1 had markedly higher affinity and agonist efficacy than its (S,S)-counterpart. Furthermore the sulfo-Cy5 labelled (R,R)-14 retained high agonist potency as a novel fluorescent ligand for imaging Y4 receptors. |
| first_indexed | 2025-11-14T19:21:41Z |
| format | Article |
| id | nottingham-34144 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:21:41Z |
| publishDate | 2016 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-341442020-05-04T17:56:49Z https://eprints.nottingham.ac.uk/34144/ Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach Liu, Mengjie Mountford, Simon J. Richardson, Rachel R. Groenen, Marleen Holliday, Nicholas D. Thompson, Philip E. The dimeric peptide 1 (BVD-74D, as a diastereomeric mixture) is a potent and selective Neuropeptide Y Y4 receptor agonist. It represents a valuable candidate in developing traceable ligands for pharmacological studies of Y4 receptors, and as a lead compound for anti-obesity drugs. Its optically pure stereoisomers along with analogues and fluorescently labelled variants were prepared by exploiting alkene metathesis reactions. The (2R,7R)- diaminosuberoyl containing peptide, (R,R)-1 had markedly higher affinity and agonist efficacy than its (S,S)-counterpart. Furthermore the sulfo-Cy5 labelled (R,R)-14 retained high agonist potency as a novel fluorescent ligand for imaging Y4 receptors. American Chemical Society 2016-06-13 Article PeerReviewed Liu, Mengjie, Mountford, Simon J., Richardson, Rachel R., Groenen, Marleen, Holliday, Nicholas D. and Thompson, Philip E. (2016) Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach. Journal of Medicinal Chemistry . ISSN 1520-4804 http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b00310 doi:10.1021/acs.jmedchem.6b00310 doi:10.1021/acs.jmedchem.6b00310 |
| spellingShingle | Liu, Mengjie Mountford, Simon J. Richardson, Rachel R. Groenen, Marleen Holliday, Nicholas D. Thompson, Philip E. Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach |
| title | Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach |
| title_full | Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach |
| title_fullStr | Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach |
| title_full_unstemmed | Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach |
| title_short | Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach |
| title_sort | optically pure, structural and fluorescent analogues of a dimeric y4 receptor agonist derived by an olefin metathesis approach |
| url | https://eprints.nottingham.ac.uk/34144/ https://eprints.nottingham.ac.uk/34144/ https://eprints.nottingham.ac.uk/34144/ |