Kruijtzer, J.A.W., Nijenhuis, W.A.J., Wanders, N., Gispen, W.H., Liskamp, R.M.J. and Adan, R.A.H. (2005) Peptoid−peptide hybrids as potent novel melanocortin receptor ligands. Journal of Medicinal Chemistry, 48(13), pp. 4224-4230. (doi: 10.1021/jm0490033)
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Abstract
All possible peptoid−peptide hybrids of an MC4 receptor agonist were synthesized and investigated on cells expressing different melanocortin (MC) receptor subtypes and for rat grooming behavior. In general, receptor selectivity remained while affinity and potency were decreased. The length of the functional group of Trp was more important for MC3 and MC5 than for MC4 receptor binding. In general, the potency of the peptoid−peptide hybrids to increase rat excessive grooming behavior correlated well with MC4 receptor pharmacology.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Liskamp, Professor Robert |
| Authors: | Kruijtzer, J.A.W., Nijenhuis, W.A.J., Wanders, N., Gispen, W.H., Liskamp, R.M.J., and Adan, R.A.H. |
| College/School: | College of Science and Engineering > School of Chemistry |
| Journal Name: | Journal of Medicinal Chemistry |
| ISSN: | 0022-2623 |
| ISSN (Online): | 1520-4804 |
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