Dimeric Dermorphin Analogues Containing β3-Homo-Amino Acids: Synthesis, Binding Affinities and Metabolic Stability

Frączak, Oliwia; Lasota, Anika; Muchowska, Adriana; Kossoń, Piotr; Tymecka, Dagmara; Misicka, Aleksandra; Olma, Aleksandra

doi:10.17952/24aps.2015.077

Peptides 2015, Proceedings of the 24th American Peptide Symposium 2015

DOI: 10.17952/24aps.2015.077

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Dimeric Dermorphin Analogues Containing β3-Homo-Amino Acids: Synthesis, Binding Affinities and Metabolic Stability

Oliwia Frączak¹,

Anika Lasota²,

Adriana Muchowska³

et al.

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2016

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Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ³-homo-amino acids

et al. 2016

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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.

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Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ³-homo-amino acids

et al. 2016

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Dimeric Dermorphin Analogues Containing β3-Homo-Amino Acids: Synthesis, Binding Affinities and Metabolic Stability

Cited by 1 publication

References 3 publications

Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ³-homo-amino acids

Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ³-homo-amino acids

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Dimeric Dermorphin Analogues Containing β3-Homo-Amino Acids: Synthesis, Binding Affinities and Metabolic Stability

Cited by 1 publication

References 3 publications

Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ3-homo-amino acids

Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ3-homo-amino acids

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Product

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Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ³-homo-amino acids

Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified withβ³-homo-amino acids