Preparation of human Melanocortin-4 receptor agonist libraries: linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2
| Autor: | Waleed Danho, Lida Qi, Xin-Jie Chu, Vijay Gore, Li Chen, Joseph Swistok, Adrian Wai-Hing Cheung, Grazyna Kurylko, David Joseph Bartkovitz, Keith A. Yagaloff |
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| Rok vydání: | 2005 |
| Předmět: |
Agonist
medicine.drug_class Stereochemistry Clinical Biochemistry Glycine Pharmaceutical Science Peptide Biochemistry Pentapeptide repeat Structure-Activity Relationship Peptide Library Drug Discovery medicine Humans Amino Acid Sequence Peptide library Molecular Biology chemistry.chemical_classification Organic Chemistry In vitro Melanocortin 4 receptor chemistry Molecular Medicine Receptor Melanocortin Type 4 Oligopeptides |
| Zdroj: | Bioorganicmedicinal chemistry letters. 15(24) |
| ISSN: | 0960-894X |
| Popis: | Two libraries of hMC4R agonists, X-Y-DPhe(7)-Arg(8)-2-Nal(9)-Z-NH(2) and X-Y-DPhe(7)-Arg(8)-Trp(9)-Z-NH(2), totaling 185 peptides were prepared using Irori radiofrequency tagging technology and Argonaut Quest 210 Synthesizer, where X stands for N-caps, Y for His(6) surrogates and Z for Gly(10) surrogates. As a result of this study, His-modified pentapeptides with Trp were found to be more hMC4R potent than the corresponding 2-Nal analogs, novel N-caps and Gly surrogates were identified and 19 new peptides which are potent hMC4R agonists (EC(50) 1-15nM) and selective against hMC1R were discovered. |
| Databáze: | OpenAIRE |
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