Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ3-homo-amino acids
| Autor: | Anika Lasota, Dagmara Tymecka, Aleksandra Olma, Piotr Kosson, Aleksandra Misicka, Adriana Muchowska, Oliwia Frączak |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Pharmacology chemistry.chemical_classification Chemistry Stereochemistry Organic Chemistry General Medicine Plasma protein binding Dermorphin Ligand (biochemistry) Biochemistry Amino acid 03 medical and health sciences chemistry.chemical_compound DAMGO 030104 developmental biology 0302 clinical medicine Enzyme Structural Biology Drug Discovery Molecular Medicine Tyrosine Selectivity Molecular Biology 030217 neurology & neurosurgery |
| Zdroj: | Journal of Peptide Science. 22:222-227 |
| ISSN: | 1075-2617 |
| Popis: | In this study, proteinogenic amino acids residues of dimeric dermorphin pentapeptides were replaced by the corresponding β(3)-homo-amino acids. The potency and selectivity of hybrid α/β dimeric dermorphin pentapeptides were evaluated by competetive receptor binding assay in the rat brain using [3H]DAMGO (a μ ligand) and [3H]DELT (a δ ligand). Tha analog containing β(3)-homo-Tyr in place of Tyr (Tyr-D-Ala-Phe-Gly-β(3)-homo-Tyr-NH-)2 showed good μ receptor affinity and selectivity (IC50 = 0.302, IC50 ratio μ/δ = 68) and enzymatic stability in human plasma. |
| Databáze: | OpenAIRE |
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