Structure–activity relationship of cyclic peptide penta-c[Asp-His6-DPhe7-Arg8-Trp9-Lys]-NH2 at the human melanocortin-1 and -4 receptors: His6 substitution
| Autor: | Keith A. Yagaloff, Xin-Jie Chu, Lucia Franco, Mitch Yeon, Grazyna Kurylko, Lida Qi, Li Chen, Adrian Wai-Hing Cheung, Karen Rowan, Joseph Swistok, Waleed Danho |
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| Rok vydání: | 2003 |
| Předmět: |
Agonist
Magnetic Resonance Spectroscopy Cell Survival medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Peptides Cyclic Biochemistry Partial agonist Pentapeptide repeat Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Tumor Cells Cultured Peptide synthesis medicine Humans Structure–activity relationship Histidine Receptor Molecular Biology chemistry.chemical_classification Receptors Melanocortin Organic Chemistry Cyclic peptide Amino Acid Substitution Receptors Corticotropin chemistry Receptor Melanocortin Type 4 Molecular Medicine Melanocortin |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 13:1307-1311 |
| ISSN: | 0960-894X |
| Popis: | A series of MT-II related cyclic peptides, based on potent but non-selective hMC4R agonist (Penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2)) was prepared in which His(6) residue was systematically substituted. Two of the most interesting peptides identified in this study are Penta-c[Asp-5-ClAtc-DPhe-Arg-Trp-Lys]-NH(2) and Penta-c[Asp-5-ClAtc-DPhe-Cit-Trp-Lys]-NH(2) which are potent hMC4R agonists and are either inactive or weak partial agonists (not tested for their antagonist activities) in hMC1R, hMC3R and hMC5R agonist assays. |
| Databáze: | OpenAIRE |
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