Abstract
Replacing Cys(5) by Pen (penicillamine, beta,beta-dimethylcysteine) in the cyclic C-terminal U-II octapeptide, U-II(4-11), we have obtained a potent urotensin II (U-II) receptor agonist. Conformational analysis of solution NMR data indicated that the putative biologically active conformation of U-II is stabilized by introduction of a Pen residue. To the best of our knowledge, this is the most potent U-II receptor agonist reported to date.
MeSH terms
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Animals
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Binding, Competitive
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CHO Cells
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Cricetinae
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Cysteine / chemistry
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Disulfides / chemistry*
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Humans
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Conformation
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology
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Penicillamine / chemistry*
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / chemistry
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Peptides, Cyclic / pharmacology
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Radioligand Assay
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Receptors, Cell Surface / agonists*
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Receptors, G-Protein-Coupled*
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Structure-Activity Relationship
Substances
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Disulfides
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Oligopeptides
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Peptides, Cyclic
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Receptors, Cell Surface
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Receptors, G-Protein-Coupled
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UTS2R protein, human
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aspartyl-cyclo(penicillamyl-phenylalanyl-tryptophyl-lysyl-tyrosyl-cysteinyl)valine
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Penicillamine
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Cysteine