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2mfx

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'''Unreleased structure'''
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{{STRUCTURE_2mfx| PDB=2mfx | SCENE= }}
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===Non-reducible analogues of alpha-conotoxin Vc1.1: [2,8]-cis dicarba Vc1.1===
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{{ABSTRACT_PUBMED_23768016}}
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The entry 2mfx is ON HOLD
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==Function==
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[[http://www.uniprot.org/uniprot/CA1A_CONVC CA1A_CONVC]] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This synthetic peptide (produced without hydroxyproline, nor 4-carboxyglutamate) is a neuronal nAChR antagonist that acts as a powerful analgesic. It blocks nAChRs composed of alpha-3 or -5/beta-2 (IC(50)=7.2 uM), alpha-3/beta-2 (IC(50)=7.3 uM), alpha-3/beta-4 (IC(50)=4.2 uM), alpha-3 or -5/beta-4 (IC(50)<30 uM), alpha-4/beta-2 (IC(50)<30 uM), alpha-4/beta-4 (IC(50)<30 uM) and alpha/beta/gamma/delta (IC(50)<30 uM) subunits.<ref>PMID:12779345</ref> <ref>PMID:15770155</ref>
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Authors: Robinson, S.D., Macraild, C.A., Van Lierop, B.J., Robinson, A.J., Norton, R.S.
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==About this Structure==
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[[2mfx]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MFX OCA].
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Description: Non-reducible analogues of alpha-conotoxin Vc1.1: [2,8]-cis dicarba Vc1.1
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==Reference==
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<ref group="xtra">PMID:023768016</ref><references group="xtra"/><references/>
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[[Category: Lierop, B J.Van.]]
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[[Category: Macraild, C A.]]
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[[Category: Norton, R S.]]
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[[Category: Robinson, A J.]]
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[[Category: Robinson, S D.]]
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[[Category: Dicarba]]
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[[Category: Toxin]]

Revision as of 10:21, 18 December 2013

Template:STRUCTURE 2mfx

Contents

Non-reducible analogues of alpha-conotoxin Vc1.1: [2,8]-cis dicarba Vc1.1

Template:ABSTRACT PUBMED 23768016

Function

[CA1A_CONVC] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This synthetic peptide (produced without hydroxyproline, nor 4-carboxyglutamate) is a neuronal nAChR antagonist that acts as a powerful analgesic. It blocks nAChRs composed of alpha-3 or -5/beta-2 (IC(50)=7.2 uM), alpha-3/beta-2 (IC(50)=7.3 uM), alpha-3/beta-4 (IC(50)=4.2 uM), alpha-3 or -5/beta-4 (IC(50)<30 uM), alpha-4/beta-2 (IC(50)<30 uM), alpha-4/beta-4 (IC(50)<30 uM) and alpha/beta/gamma/delta (IC(50)<30 uM) subunits.[1] [2]

About this Structure

2mfx is a 1 chain structure. Full experimental information is available from OCA.

Reference

  • van Lierop BJ, Robinson SD, Kompella SN, Belgi A, McArthur JR, Hung A, MacRaild CA, Adams DJ, Norton RS, Robinson AJ. Dicarba alpha-conotoxin Vc1.1 analogues with differential selectivity for nicotinic acetylcholine and GABAB receptors. ACS Chem Biol. 2013 Aug 16;8(8):1815-21. doi: 10.1021/cb4002393. Epub 2013 Jun, 17. PMID:23768016 doi:http://dx.doi.org/10.1021/cb4002393
  1. ↑ Sandall DW, Satkunanathan N, Keays DA, Polidano MA, Liping X, Pham V, Down JG, Khalil Z, Livett BG, Gayler KR. A novel alpha-conotoxin identified by gene sequencing is active in suppressing the vascular response to selective stimulation of sensory nerves in vivo. Biochemistry. 2003 Jun 10;42(22):6904-11. PMID:12779345 doi:http://dx.doi.org/10.1021/bi034043e
  2. ↑ Lang PM, Burgstahler R, Haberberger RV, Sippel W, Grafe P. A conus peptide blocks nicotinic receptors of unmyelinated axons in human nerves. Neuroreport. 2005 Apr 4;16(5):479-83. PMID:15770155

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