2j15

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[[Image:2j15.jpg|left|200px]]
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{{Seed}}
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[[Image:2j15.png|left|200px]]
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{{STRUCTURE_2j15| PDB=2j15 | SCENE= }}
{{STRUCTURE_2j15| PDB=2j15 | SCENE= }}
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'''CYCLIC MRIA: AN EXCEPTIONALLY STABLE AND POTENT CYCLIC CONOTOXIN WITH A NOVEL TOPOLOGICAL FOLD THAT TARGETS THE NOREPINEPHRINE TRANSPORTER.'''
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===CYCLIC MRIA: AN EXCEPTIONALLY STABLE AND POTENT CYCLIC CONOTOXIN WITH A NOVEL TOPOLOGICAL FOLD THAT TARGETS THE NOREPINEPHRINE TRANSPORTER.===
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==Overview==
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Conotoxins, disulfide-rich peptides from the venom of cone snails, have created much excitement over recent years due to their potency and specificity for ion channels and their therapeutic potential. One recently identified conotoxin, MrIA, a 13-residue member of the chi-conotoxin family, inhibits the human norepinephrine transporter (NET) and has potential applications in the treatment of pain. In the current study, we show that the beta-hairpin structure of native MrIA is retained in a synthetic cyclic version, as is biological activity at the NET. Furthermore, the cyclic version has increased resistance to trypsin digestion relative to the native peptide, an intriguing result because the cleavage site for the trypsin is not close to the cyclization site. The use of peptides as drugs is generally hampered by susceptibility to proteolysis, and so, the increase in enzymatic stability against trypsin observed in the current study may be useful in improving the therapeutic potential of MrIA. Furthermore, the structure reported here for cyclic MrIA represents a new topology among a growing number of circular disulfide-rich peptides.
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The line below this paragraph, {{ABSTRACT_PUBMED_17064074}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17064074 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17064074}}
==About this Structure==
==About this Structure==
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2J15 is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J15 OCA].
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2J15 is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J15 OCA].
==Reference==
==Reference==
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[[Category: Walstrom, M E.]]
[[Category: Walstrom, M E.]]
[[Category: Toxin]]
[[Category: Toxin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:12:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:13:21 2008''

Revision as of 14:13, 27 July 2008

Image:2j15.png

Template:STRUCTURE 2j15

CYCLIC MRIA: AN EXCEPTIONALLY STABLE AND POTENT CYCLIC CONOTOXIN WITH A NOVEL TOPOLOGICAL FOLD THAT TARGETS THE NOREPINEPHRINE TRANSPORTER.

Template:ABSTRACT PUBMED 17064074

About this Structure

2J15 is a Single protein structure. Full experimental information is available from OCA.

Reference

Cyclic MrIA: a stable and potent cyclic conotoxin with a novel topological fold that targets the norepinephrine transporter., Lovelace ES, Armishaw CJ, Colgrave ML, Wahlstrom ME, Alewood PF, Daly NL, Craik DJ, J Med Chem. 2006 Nov 2;49(22):6561-8. PMID:17064074

Page seeded by OCA on Sun Jul 27 17:13:21 2008

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