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Bioorg Med Chem Lett. 2013 Sep 1;23(17):4975-8. doi: 10.1016/j.bmcl.2013.06.065. Epub 2013 Jul 2.

Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.

Author information

1
Department of Chemistry and Biochemistry, University of Arizona, 1306 East University Boulevard, Tucson, AZ 85721, USA.

Abstract

The optimization and truncation of our lead peptide-derived ligand TY005 possessing eight amino-acid residues was performed. Among the synthesized derivatives, NP30 (Tyr(1)-DAla(2)-Gly(3)-Phe(4)-Gly(5)-Trp(6)-O-[3',5'-Bzl(CF3)2]) showed balanced and potent opioid agonist as well as substance P antagonist activities in isolated tissue-based assays, together with significant antinociceptive and antiallodynic activities in vivo.

KEYWORDS:

Bifunctional compounds; NMR structure; Neutokinin-1 receptor antagonists; Opioid receptor agonists; Truncation of peptide sequence

PMID:
23899615
PMCID:
PMC3810412
DOI:
10.1016/j.bmcl.2013.06.065
[Indexed for MEDLINE]
Free PMC Article

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