1wt7

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[[Image:1wt7.gif|left|200px]]
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{{STRUCTURE_1wt7| PDB=1wt7 | SCENE= }}
{{STRUCTURE_1wt7| PDB=1wt7 | SCENE= }}
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'''Solution structure of BuTX-MTX: a butantoxin-maurotoxin chimera'''
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===Solution structure of BuTX-MTX: a butantoxin-maurotoxin chimera===
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==Overview==
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Scorpion toxins interact with their target ion channels through multiple molecular contacts. Because a "gain of function" approach has never been described to evaluate the importance of the molecular contacts in defining toxin affinity, we experimentally examined whether increasing the molecular contacts between a toxin and an ion channel directly impacts toxin affinity. For this purpose, we focused on two scorpion peptides, the well-characterized maurotoxin with its variant Pi1-like disulfide bridging (MTX(Pi1)), used as a molecular template, and butantoxin (BuTX), used as an N-terminal domain provider. BuTX is found to be 60-fold less potent than MTX(Pi1) in blocking Kv1.2 (IC(50) values of 165 nM for BuTX versus 2.8 nM for MTX(Pi1)). Removal of its N-terminal domain (nine residues) further decreases BuTX affinity for Kv1.2 by 5.6-fold, which is in agreement with docking simulation data showing the importance of this domain in BuTX-Kv1.2 interaction. Transfer of the BuTX N-terminal domain to MTX(Pi1) results in a chimera with five disulfide bridges (BuTX-MTX(Pi1)) that exhibits 22-fold greater affinity for Kv1.2 than MTX(Pi1) itself, in spite of the lower affinity of BuTX as compared to MTX(Pi1). Docking experiments performed with the 3-D structure of BuTX-MTX(Pi1) in solution, as solved by (1)H-NMR, reveal that the N-terminal domain of BuTX participates in the increased affinity for Kv1.2 through additional molecular contacts. Altogether, the data indicate that acting on molecular contacts between a toxin and a channel is an efficient strategy to modulate toxin affinity.
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(as it appears on PubMed at http://www.pubmed.gov), where 15971207 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15971207}}
==About this Structure==
==About this Structure==
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1WT7 is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WT7 OCA].
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1WT7 is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WT7 OCA].
==Reference==
==Reference==
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[[Category: Scorpion toxin]]
[[Category: Scorpion toxin]]
[[Category: Toxin affinity]]
[[Category: Toxin affinity]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:06:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:05:53 2008''

Revision as of 00:05, 28 July 2008

Image:1wt7.png

Template:STRUCTURE 1wt7

Solution structure of BuTX-MTX: a butantoxin-maurotoxin chimera

Template:ABSTRACT PUBMED 15971207

About this Structure

1WT7 is a Single protein structure. Full experimental information is available from OCA.

Reference

Increasing the molecular contacts between maurotoxin and Kv1.2 channel augments ligand affinity., M'Barek S, Chagot B, Andreotti N, Visan V, Mansuelle P, Grissmer S, Marrakchi M, El Ayeb M, Sampieri F, Darbon H, Fajloun Z, De Waard M, Sabatier JM, Proteins. 2005 Aug 15;60(3):401-11. PMID:15971207

Page seeded by OCA on Mon Jul 28 03:05:53 2008

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