Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 17, Pages 5176-5181Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.025
Keywords
Melanocortin receptors; Melanocortin agonists; N-capping; Peptidomimetics; Conformational analysis; Molecular modeling
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Funding
- Skin Cancer Foundation
- [RO1CA114095]
- [RO1DK057080]
- NATIONAL CANCER INSTITUTE [R01CA114095, R01CA135454] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [R01DK057080] Funding Source: NIH RePORTER
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A series of 30 RCO-HfR-NH2 derivatives show preference for the mouse MC1R vs MC3-5Rs. trans-4-HOC6H4CH=CHCO-HfR-NH2 (13) [EC50 (nM): MC1R 83, MC3R 20500, MC4R 18130 and MC5R 935; ratio 1: 246: 217: 11] is 11 times more potent than the lead compound LK-394 Ph(CH2)(3)CO-HfR-NH2 (2) and only 11 times less potent than the native tridecapeptide alpha-MSH at mMC1R. Differences in conformations of 2 and 13 are discussed. (C) 2009 Elsevier Ltd. All rights reserved.
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