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.
MeSH terms
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Amino Acid Sequence
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Animals
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CHO Cells
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Calcium / metabolism*
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Carrier Proteins / chemical synthesis
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Carrier Proteins / chemistry*
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Carrier Proteins / pharmacology*
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Cricetinae
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Humans
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Intracellular Signaling Peptides and Proteins*
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Molecular Sequence Data
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Mutagenesis, Site-Directed
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Neuropeptides / chemical synthesis
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Neuropeptides / chemistry*
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Neuropeptides / pharmacology*
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Orexin Receptors
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Orexins
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Protein Binding
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Protein Structure, Tertiary
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Receptors, G-Protein-Coupled
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Receptors, Neuropeptide / agonists*
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Receptors, Neuropeptide / metabolism
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Carrier Proteins
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HCRT protein, human
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Intracellular Signaling Peptides and Proteins
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Neuropeptides
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Orexin Receptors
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Orexins
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Receptors, G-Protein-Coupled
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Receptors, Neuropeptide
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Calcium