2ajw

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[[Image:2ajw.gif|left|200px]]
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{{Seed}}
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[[Image:2ajw.png|left|200px]]
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{{STRUCTURE_2ajw| PDB=2ajw | SCENE= }}
{{STRUCTURE_2ajw| PDB=2ajw | SCENE= }}
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'''Structure of the cyclic conotoxin MII-6'''
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===Structure of the cyclic conotoxin MII-6===
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==Overview==
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Conotoxins (CTXs), with their exquisite specificity and potency, have recently created much excitement as drug leads. However, like most peptides, their beneficial activities may potentially be undermined by susceptibility to proteolysis in vivo. By cyclizing the alpha-CTX MII by using a range of linkers, we have engineered peptides that preserve their full activity but have greatly improved resistance to proteolytic degradation. The cyclic MII analogue containing a seven-residue linker joining the N and C termini was as active and selective as the native peptide for native and recombinant neuronal nicotinic acetylcholine receptor subtypes present in bovine chromaffin cells and expressed in Xenopus oocytes, respectively. Furthermore, its resistance to proteolysis against a specific protease and in human plasma was significantly improved. More generally, to our knowledge, this report is the first on the cyclization of disulfide-rich toxins. Cyclization strategies represent an approach for stabilizing bioactive peptides while keeping their full potencies and should boost applications of peptide-based drugs in human medicine.
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The line below this paragraph, {{ABSTRACT_PUBMED_16162671}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16162671 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16162671}}
==About this Structure==
==About this Structure==
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2AJW is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2AJW OCA].
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2AJW is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2AJW OCA].
==Reference==
==Reference==
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[[Category: Alpha-helix]]
[[Category: Alpha-helix]]
[[Category: Cyclic backbone]]
[[Category: Cyclic backbone]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:08:37 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 23:04:27 2008''

Revision as of 20:04, 27 July 2008

Image:2ajw.png

Template:STRUCTURE 2ajw

Structure of the cyclic conotoxin MII-6

Template:ABSTRACT PUBMED 16162671

About this Structure

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

Reference

Engineering stable peptide toxins by means of backbone cyclization: stabilization of the alpha-conotoxin MII., Clark RJ, Fischer H, Dempster L, Daly NL, Rosengren KJ, Nevin ST, Meunier FA, Adams DJ, Craik DJ, Proc Natl Acad Sci U S A. 2005 Sep 27;102(39):13767-72. Epub 2005 Sep 14. PMID:16162671

Page seeded by OCA on Sun Jul 27 23:04:27 2008

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