|Title||Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.|
|Publication Type||Journal Article|
|Year of Publication||2013|
|Authors||Nair P, Yamamoto T, Largent-Milnes TM, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma S-W, Vanderah TW, Lai J, Porreca F, Hruby VJ|
|Journal||Bioorg Med Chem Lett|
|Date Published||2013 Sep 1|
|Keywords||Amino Acid Sequence, Analgesics, Animals, Humans, Ligands, Neurokinin-1 Receptor Antagonists, Peptides, Rats, Receptors, Neurokinin-1, Receptors, Opioid, delta, Receptors, Opioid, mu|
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.
|Alternate Journal||Bioorg. Med. Chem. Lett.|
|PubMed Central ID||PMC3810412|
|Grant List||DA-06284 / DA / NIDA NIH HHS / United States |
DA-13449 / DA / NIDA NIH HHS / United States
P01 DA006284 / DA / NIDA NIH HHS / United States
R01 DA013449 / DA / NIDA NIH HHS / United States
Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Faculty Member Reference:
Victor Hruby, Ph.D.
Josephine Lai , Ph.D.
Tally Largent-Milnes, PhD
Edita Navratilova, Ph.D.
Frank Porreca, Ph.D.
Todd Vanderah, Ph.D.