Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15
Traceable truncated Neuropeptide Y (NPY) analogues with Y₁ receptor (Y₁R) affinity and selectivity are highly desirable tools in studying receptor location, regulation, and biological functions. A range of fluorescently labeled analogues of a reported Y₁R/Y₄R preferring ligand BVD-15 have been prepa...
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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/41450/ |
| _version_ | 1848796276423917568 |
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| author | Liu, Mengjie Richardson, Rachel R. Mountford, Simon J. Zhang, Lei Tempone, Matheus H. Herzog, Herbert Holliday, Nicholas D. Thompson, Philip E. |
| author_facet | Liu, Mengjie Richardson, Rachel R. Mountford, Simon J. Zhang, Lei Tempone, Matheus H. Herzog, Herbert Holliday, Nicholas D. Thompson, Philip E. |
| author_sort | Liu, Mengjie |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | Traceable truncated Neuropeptide Y (NPY) analogues with Y₁ receptor (Y₁R) affinity and selectivity are highly desirable tools in studying receptor location, regulation, and biological functions. A range of fluorescently labeled analogues of a reported Y₁R/Y₄R preferring ligand BVD-15 have been prepared and evaluated using high content imaging techniques. One peptide, [Lys²(sCy5), Arg⁴]BVD-15, was characterized as an Y₁R antagonist with a pKD of 7.2 measured by saturation analysis using fluorescent imaging. The peptide showed 8-fold lower affinity for Y₄R (pKD = 6.2) and was a partial agonist at this receptor. The suitability of [Lys²(sCy5), Arg⁴]BVD-15 for Y₁R and Y₄R competition binding experiments was also demonstrated in intact cells. The nature of the label was shown to be critical with replacement of sCy5 by the more hydrophobic Cy5.5 resulting in a switch from Y₁R antagonist to Y₁R partial agonist. |
| first_indexed | 2025-11-14T19:45:25Z |
| format | Article |
| id | nottingham-41450 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:45:25Z |
| publishDate | 2016 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-414502020-05-04T18:07:14Z https://eprints.nottingham.ac.uk/41450/ Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 Liu, Mengjie Richardson, Rachel R. Mountford, Simon J. Zhang, Lei Tempone, Matheus H. Herzog, Herbert Holliday, Nicholas D. Thompson, Philip E. Traceable truncated Neuropeptide Y (NPY) analogues with Y₁ receptor (Y₁R) affinity and selectivity are highly desirable tools in studying receptor location, regulation, and biological functions. A range of fluorescently labeled analogues of a reported Y₁R/Y₄R preferring ligand BVD-15 have been prepared and evaluated using high content imaging techniques. One peptide, [Lys²(sCy5), Arg⁴]BVD-15, was characterized as an Y₁R antagonist with a pKD of 7.2 measured by saturation analysis using fluorescent imaging. The peptide showed 8-fold lower affinity for Y₄R (pKD = 6.2) and was a partial agonist at this receptor. The suitability of [Lys²(sCy5), Arg⁴]BVD-15 for Y₁R and Y₄R competition binding experiments was also demonstrated in intact cells. The nature of the label was shown to be critical with replacement of sCy5 by the more hydrophobic Cy5.5 resulting in a switch from Y₁R antagonist to Y₁R partial agonist. American Chemical Society 2016-08-11 Article PeerReviewed Liu, Mengjie, Richardson, Rachel R., Mountford, Simon J., Zhang, Lei, Tempone, Matheus H., Herzog, Herbert, Holliday, Nicholas D. and Thompson, Philip E. (2016) Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15. Bioconjugate Chemistry, 27 (9). pp. 2166-2175. ISSN 1520-4812 Neuropeptide Y Fluorescent ligand G protein coupled receptor High content imaging http://pubs.acs.org/doi/abs/10.1021/acs.bioconjchem.6b00376 doi:10.1021/acs.bioconjchem.6b00376 doi:10.1021/acs.bioconjchem.6b00376 |
| spellingShingle | Neuropeptide Y Fluorescent ligand G protein coupled receptor High content imaging Liu, Mengjie Richardson, Rachel R. Mountford, Simon J. Zhang, Lei Tempone, Matheus H. Herzog, Herbert Holliday, Nicholas D. Thompson, Philip E. Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 |
| title | Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 |
| title_full | Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 |
| title_fullStr | Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 |
| title_full_unstemmed | Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 |
| title_short | Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 |
| title_sort | identification of a cyanine-dye labeled peptidic ligand for y₁r and y₄r, based upon the neuropeptide y c-terminal analogue, bvd-15 |
| topic | Neuropeptide Y Fluorescent ligand G protein coupled receptor High content imaging |
| url | https://eprints.nottingham.ac.uk/41450/ https://eprints.nottingham.ac.uk/41450/ https://eprints.nottingham.ac.uk/41450/ |