Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides
| Autor: | Lucia Franco, Joseph Swistok, Karen Rowan, David Joseph Bartkovitz, Li Chen, Adrian Wai-Hing Cheung, Lida Qi, Xin-Jie Chu, Mitch Yeon, Keith A. Yagaloff, Grazyna Kurylko, Waleed Danho |
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| Rok vydání: | 2005 |
| Předmět: |
Agonist
medicine.drug_class Stereochemistry Carboxylic acid Clinical Biochemistry Carboxylic Acids Pharmaceutical Science Peptide Biochemistry Pentapeptide repeat Chemical synthesis Sensitivity and Specificity Substrate Specificity Inhibitory Concentration 50 Cyclohexanes Drug Discovery medicine Humans Amino Acid Sequence Receptor Molecular Biology chemistry.chemical_classification Molecular Structure Chemistry Organic Chemistry Molecular Medicine Receptor Melanocortin Type 4 Melanocortin Selectivity Receptor Melanocortin Type 1 |
| Zdroj: | Bioorganicmedicinal chemistry letters. 15(22) |
| ISSN: | 0960-894X |
| Popis: | Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His6 with phenyl-containing rigid templates in achieving good hMC4R agonist potency and selectivity against hMC1R in linear pentapeptides. |
| Databáze: | OpenAIRE |
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