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1jlp

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[[Image:1jlp.gif|left|200px]]
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{{STRUCTURE_1jlp| PDB=1jlp | SCENE= }}
{{STRUCTURE_1jlp| PDB=1jlp | SCENE= }}
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'''Solution Structure of the Noncompetitive Skeletal Muscle Nicotinic Acetylcholine Receptor Antagonist Psi-conotoxin PIIIF'''
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===Solution Structure of the Noncompetitive Skeletal Muscle Nicotinic Acetylcholine Receptor Antagonist Psi-conotoxin PIIIF===
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==Overview==
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A novel inhibitor of nicotinic acetylcholine receptors (nAChRs), psi-conotoxin Piiif, was isolated from the venom of Conus purpurascens and found to have the sequence GOOCCLYGSCROFOGCYNALCCRK-NH2. The sequence is highly homologous to that of psi-conotoxin Piiie, a previously identified noncompetitive inhibitor of Torpedo electroplax nAChR, also isolated from C. purpurascens. Both psi-conotoxins block Torpedo and mouse nicotinic acetylcholine receptors (nAChRs), but psi-Piiif is less potent by a factor of 10(1)-10(2). A high-resolution structure of psi-Piiif was determined by NMR and molecular modeling calculations. Psi-Piiif analogues containing [(13)C]-labeled cysteine at selected positions were synthesized to resolve spectral overlap of Cys side chain proton signals. The structures are well-converged, with backbone atom position RMSDs of 0.21 A for the main body of the peptide between residues 4 and 22 and 0.47 A for all residues. The overall backbone conformation is closely similar to psi-Piiie, the main difference being in the degree of conformational disorder at the two termini. Psi-Piiie and psi-Piiif have similar locations of positive charge density, although psi-Piiif has a lower overall charge. One disulfide bridge of psi-Piiif appears to undergo dynamic conformational fluctuations based on both the model and on experimental observation. Chimeras in which the three intercysteine loops were swapped between psi-Piiie and psi-Piiif were tested for inhibitory activity against Torpedo nAChRs. The third loop, which contains no charged residues in either peptide, is the prime determinant of potency in these psi-conotoxins.
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(as it appears on PubMed at http://www.pubmed.gov), where 12767216 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12767216}}
==About this Structure==
==About this Structure==
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1JLP is a [[Single protein]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1JLP OCA].
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1JLP is a [[Single protein]] structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1JLP OCA].
==Reference==
==Reference==
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[[Category: Amidated c-terminus]]
[[Category: Amidated c-terminus]]
[[Category: Multiple disulfide bond]]
[[Category: Multiple disulfide bond]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 21:22:44 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 20:26:31 2008''

Revision as of 17:26, 1 July 2008

Image:1jlp.png

Template:STRUCTURE 1jlp

Solution Structure of the Noncompetitive Skeletal Muscle Nicotinic Acetylcholine Receptor Antagonist Psi-conotoxin PIIIF

Template:ABSTRACT PUBMED 12767216

About this Structure

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

Reference

Characterization and three-dimensional structure determination of psi-conotoxin Piiif, a novel noncompetitive antagonist of nicotinic acetylcholine receptors., Van Wagoner RM, Jacobsen RB, Olivera BM, Ireland CM, Biochemistry. 2003 Jun 3;42(21):6353-62. PMID:12767216

Page seeded by OCA on Tue Jul 1 20:26:31 2008

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