Two new classes of conopeptides inhibit the alpha1-adrenoceptor and noradrenaline transporter

Sharpe, Iain A., Gehrmann, John, Loughnan, Marion L., Thomas, Linda, Adams, Denise A., Atkins, Ann, Palant, Elka, Alewood, Paul F., Craik, David J., Adams, David J, and Lewis, Richard J. (2001) Two new classes of conopeptides inhibit the alpha1-adrenoceptor and noradrenaline transporter. Nature neuroscience, 4 (9). pp. 902-907.

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Cone snails use venom containing a cocktail of peptides ('conopeptides') to capture their prey. Many of these peptides also target mammalian receptors, often with exquisite selectivity. Here we report the discovery of two new classes of conopeptides. One class targets alpha1-adrenoceptors (rho-TIA from the fish-hunting Conus tulipa), and the second class targets the neuronal noradrenaline transporter (chi-MrIA and chi-MrIB from the mollusk-hunting C. marmoreus). rho-TIA and chi-MrIA selectively modulate these important membrane-bound proteins. Both peptides act as reversible non-competitive inhibitors and provide alternative avenues for the identification of inhibitor drugs

Item ID: 338
Item Type: Article (Research - C1)
ISSN: 1097-6256
Keywords: Amino Acid Sequence/genetics, Animals, Carrier Proteins/*antagonists & inhibitors, Imaging, Three-Dimensional Magnetic Resonance Spectroscopy, Male Molecular Sequence Data, Mollusk, Venoms/chemistry/*classification/genetics/*pharmacology Neurons/metabolism, Norepinephrine Plasma Membrane Transport Proteins, Rats, Wistar, Receptors, Adrenergic, alpha/*drug effects
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© 2001 Nature Publishing Group : This journal is available online - use hypertext links above.

Date Deposited: 15 Sep 2006
FoR Codes: 06 BIOLOGICAL SCIENCES > 0699 Other Biological Sciences @ 0%
06 BIOLOGICAL SCIENCES > 0601 Biochemistry and Cell Biology @ 0%
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