Darker J G, Porter R A, Eggleston D S, Smart D, Brough S J, Sabido-David C, Jerman J C
Discovery Chemistry, SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
Bioorg Med Chem Lett. 2001 Mar 12;11(5):737-40. doi: 10.1016/s0960-894x(01)00043-9.
Truncated peptide analogues of orexin-A were prepared and their biological activity assesed at the orexin-1 receptor. Progressive N-terminal deletions identified the minimum C-terminal sequence required for maintaining a significant agonist effect, whilst an alanine scan and other pertinent substitutions identified key side-chain and stereochemical requirements for receptor activation.
