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Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor
J G Darker1, R A Porter, D S Eggleston
1Discovery Chemistry, SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. john_darker-1@sbphrd.com
Bioorganic & Medicinal Chemistry Letters
|March 27, 2001
Abstract:
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.