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1qs3

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{{STRUCTURE_1qs3| PDB=1qs3 | SCENE= }}
{{STRUCTURE_1qs3| PDB=1qs3 | SCENE= }}
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'''NMR SOLUTION CONFORMATION OF AN ANTITOXIC ANALOG OF ALPHA-CONOTOXIN GI'''
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===NMR SOLUTION CONFORMATION OF AN ANTITOXIC ANALOG OF ALPHA-CONOTOXIN GI===
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==Overview==
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The three-dimensional solution conformation of an 11-residue antitoxic analogue of alpha-conotoxin GI, des-Glu1-[Cys3Ala]-des-Cys13-conotoxin GI (CANPACGRHYS-NH(2), designated "GI-15" henceforth), has been determined using two-dimensional (1)H NMR spectroscopy. The disulfide loop region (1C-6C) and the C-terminal tail (8R-11S) are connected by a flexible hinge formed near 7G, and the pairwise backbone rmsds for the former and the latter are 0.58 and 0.65 A, respectively. Superpositioning GI-15 with the structure of alpha-conotoxin GI shows that the two share an essentially identical fold in the common first disulfide loop region (1C-6C). However, the absence of the second disulfide loop in GI-15 results in segmental motion of the C-terminal half, causing the key receptor subtype selectivity residue 8R (Arg9 in alpha-conotoxin GI) to lose its native spatial orientation. The combined features of structural equivalence in the disulfide loop and a mobile C-terminal tail appear to be responsible for the activity of GI-15 as a competitive antagonist against native toxin. Electrostatic surface potential comparisons of the first disulfide region of GI-15 with other alpha-conotoxins or receptor-bound states of acetylcholine and d-tubocurarine show a common protruding surface that may serve as the minimal binding determinant for the neuromuscular acetylcholine receptor alpha 1-subunit. On the basis of the original "Conus toxin macrosite model" [Olivera, B. M., Rivier, J., Scott, J. K., Hillyard, D. R., and Cruz, L. J. (1991) J. Biol. Chem. 266, 1923-1936], we propose a revised binding model which incorporates these results.
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(as it appears on PubMed at http://www.pubmed.gov), where 10508392 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10508392}}
==About this Structure==
==About this Structure==
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1QS3 is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QS3 OCA].
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1QS3 is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QS3 OCA].
==Reference==
==Reference==
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[[Category: Conotoxin]]
[[Category: Conotoxin]]
[[Category: Nicotinic acetylcholine receptor]]
[[Category: Nicotinic acetylcholine receptor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:38:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 21:50:44 2008''

Revision as of 18:50, 28 July 2008

Image:1qs3.png

Template:STRUCTURE 1qs3

NMR SOLUTION CONFORMATION OF AN ANTITOXIC ANALOG OF ALPHA-CONOTOXIN GI

Template:ABSTRACT PUBMED 10508392

About this Structure

1QS3 is a Single protein structure. Full experimental information is available from OCA.

Reference

NMR solution conformation of an antitoxic analogue of alpha-conotoxin GI: identification of a common nicotinic acetylcholine receptor alpha 1-subunit binding surface for small ligands and alpha-conotoxins., Mok KH, Han KH, Biochemistry. 1999 Sep 14;38(37):11895-904. PMID:10508392

Page seeded by OCA on Mon Jul 28 21:50:44 2008

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