[HTML][HTML] Ligands for κ-opioid and ORL1 receptors identified from a conformationally constrained peptide combinatorial library

JAJ Becker, A Wallace, A Garzon, P Ingallinella… - Journal of Biological …, 1999 - ASBMB
We have screened a synthetic peptide combinatorial library composed of 2× 10 7 β-turn-
constrained peptides in binding assays on four structurally related receptors, the human
opioid receptors μ, δ, and κ and the opioid receptor-like ORL1. Sixty-six individual peptides
were synthesized from the primary screening and tested in the four receptor binding assays.
Three peptides composed essentially of unnatural amino acids were found to show high
affinity for human κ-opioid receptor. Investigation of their activity in agonist-promoted …