Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor

Autor:	Jeffrey C. Jerman, Darren Smart, Roderick A. Porter, John G. Darker, Cibele Sabido-David, Drake S. Eggleston, Stephen J. Brough
Rok vydání:	2001
Předmět:	Agonist Receptors Neuropeptide medicine.drug_class Stereochemistry Clinical Biochemistry Molecular Sequence Data Pharmaceutical Science CHO Cells Biochemistry Receptors G-Protein-Coupled Orexin-A Structure-Activity Relationship Orexin Receptors Cricetinae Drug Discovery medicine Structure–activity relationship Animals Humans Amino Acid Sequence Receptor Molecular Biology Peptide sequence Alanine Orexins Chemistry Organic Chemistry Neuropeptides Intracellular Signaling Peptides and Proteins Biological activity Stereoisomerism Orexin Protein Structure Tertiary Mutagenesis Site-Directed Molecular Medicine Calcium Carrier Proteins Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 11(5)
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a4a764db6bc0d948791ff9f2d624c70 https://pubmed.ncbi.nlm.nih.gov/11266181 Zobrazit plný text záznamu Full Text from ScienceDirect