Berlicki, Lukasz, Kaske, Melanie, Gutierrez-Abad, Raquel, Bernhardt, Günther, Illa, Ona, Ortuño, Rosa, Cabrele, Chiara, Buschauer, Armin and Reiser, Oliver (2013) Replacement of Thr32 and Gln34 in the C-terminal neuropeptide Y fragment 25-36 by cis-cyclobutane- and cis-cyclopentane β-amino acids shifts selectivity toward the Y4 receptor. Journal of Medicinal Chemistry 56 (21), pp. 8422-8431.
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Abstract
Neuropeptide Y (NPY) and pancreatic polypeptide (PP) control central and peripheral processes by activating the G protein coupled receptors YxR (x = 1,2,4,5). We present analogs of the C-terminal fragments 25-36 and 32-36 of NPY and PP containing (1R,2S)-cyclobutane (βCbu) or (1R,2S)-cyclopentane (βCpe), which display exclusively Y4R affinity. In particular, [βCpe34]-NPY-(25-36) is a Y4R ...
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| Item type: | Article | ||||||
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| Date: | 3 September 2013 | ||||||
| Additional Information (public): | Supporting Information available | ||||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Oliver Reiser | ||||||
| Projects: | GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands" | ||||||
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| Keywords: | Neuropeptide Y, pancreatic polypeptide, Y receptors, Y4 receptor, beta-amino acid, gamma-amino acid, cyclobutane, cyclopentane, pentacin | ||||||
| Dewey Decimal Classification: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy | ||||||
| Status: | Published | ||||||
| Refereed: | Yes, this version has been refereed | ||||||
| Created at the University of Regensburg: | Yes | ||||||
| Item ID: | 28752 |
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