Peptide Information

General Information of This Peptide
Peptide ID
BTDP004031
Peptide Name
Alpha-conotoxin RgIA
Species
Conus regius (Crown cone)
Uniprot Name
CA1A_CONRE
Alphafold ID
P0C1D0
3D Structure
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2D Sequence
3D Structure
Source
RSCB PDB: 2JUQ
Sequence
SNKRKNAAMLDMIAQHAIRGCCSDPRCRYRCR
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Sequence Length
32
Mass (Da)
3725
Sequence Removed Signal Peptide
SNKRKNAAMLDMIAQHAIRGCCSDPRCRYRCR
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Disulfide Bond
21-27;22-31
PDB ID
2JUQ , 2JUR , 2JUS , 2JUT , 2MTO , 2MTT , 6HY7 , 7EGR
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Kingdom: Metazoa
Phylum: Mollusca
Class: Gastropoda
Order: Neogastropoda
Family: Conidae
Genus: Conus
Species: Conus regius
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    CHRNA9-CHRNA10 IC50
1.5 nM
 . . [1- 13]
 Target Info    nAChR alpha-7 IC50
>10 μM
 . . [1- 13]
 Target Info    nAChR alpha-7 IC50
1.8 μM
 . . [1- 13]
References
Ref 1 Alpha-RgIA: a novel conotoxin that specifically and potently blocks the alpha9alpha10 nAChR. Biochemistry. 2006 Feb 7;45(5):1511-7. doi: 10.1021/bi0520129.
Ref 2 Molecular mechanism for analgesia involving specific antagonism of alpha9alpha10 nicotinic acetylcholine receptors. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17880-4. doi: 10.1073/pnas.0608715103. Epub 2006 Nov 13.
Ref 3 Analgesic alpha-conotoxins Vc1.1 and Rg1A inhibit N-type calcium channels in rat sensory neurons via GABAB receptor activation. J Neurosci. 2008 Oct 22;28(43):10943-51. doi: 10.1523/JNEUROSCI.3594-08.2008.
Ref 4 Effects of cyclization on stability, structure, and activity of -conotoxin RgIA at the 910 nicotinic acetylcholine receptor and GABA(B) receptor. J Med Chem. 2011 Oct 13;54(19):6984-92. doi: 10.1021/jm201060r. Epub 2011 Sep 15.
Ref 5 Molecular basis for the differential sensitivity of rat and human 910 nAChRs to -conotoxin RgIA. J Neurochem. 2012 Sep;122(6):1137-44. doi: 10.1111/j.1471-4159.2012.07867.x. Epub 2012 Aug 3.
Ref 6 -conotoxin RgIA protects against the development of nerve injury-induced chronic pain and prevents both neuronal and glial derangement. Pain. 2014 Oct;155(10):1986-95. doi: 10.1016/j.pain.2014.06.023. Epub 2014 Jul 5.
Ref 7 Molecular interaction of -conotoxin RgIA with the rat 910 nicotinic acetylcholine receptor. Mol Pharmacol. 2015 May;87(5):855-64. doi: 10.1124/mol.114.096511. Epub 2015 Mar 4.
Ref 8 Corrections to "Molecular interaction of -conotoxin RgIA with the rat 910 nicotinic acetylcholine receptor". Mol Pharmacol. 2016 Oct;90(4):415-7. doi: 10.1124/mol.114.096511err.
Ref 9 Inhibition of 910 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain. Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):E1825-E1832. doi: 10.1073/pnas.1621433114. Epub 2017 Feb 21.
Ref 10 Dimerization of -Conotoxins as a Strategy to Enhance the Inhibition of the Human 7 and 910 Nicotinic Acetylcholine Receptors. J Med Chem. 2020 Mar 26;63(6):2974-2985. doi: 10.1021/acs.jmedchem.9b01536. Epub 2020 Mar 17.
Ref 11 The three-dimensional structure of the analgesic alpha-conotoxin, RgIA. FEBS Lett. 2008 Mar 5;582(5):597-602. doi: 10.1016/j.febslet.2008.01.027. Epub 2008 Jan 31.
Ref 12 Alpha-RgIA, a novel conotoxin that blocks the alpha9alpha10 nAChR: structure and identification of key receptor-binding residues. J Mol Biol. 2008 Apr 4;377(4):1216-27. doi: 10.1016/j.jmb.2008.01.082. Epub 2008 Feb 4.
Ref 13 Dicarba analogues of -conotoxin RgIA. Structure, stability, and activity at potential pain targets. J Med Chem. 2014 Dec 11;57(23):9933-44. doi: 10.1021/jm501126u. Epub 2014 Dec 1.
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