Peptide Information

General Information of This Peptide
Peptide ID
BTDP008352
Peptide Name
Beta/omega-theraphotoxin-Tp2a
Symonym
Protoxin-2; Protoxin-II
Species
Thrixopelma pruriens (Peruvian green velvet tarantula)
Uniprot Name
TXPR2_THRPR
Alphafold ID
P83476
3D Structure
Download
2D Sequence
3D Structure
Source
RSCB PDB: 2N9T
Sequence
YCQKWMWTCDSERKCCEGMVCRLWCKKKLW
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Sequence Length
30
Mass (Da)
3833
Sequence Removed Signal Peptide
YCQKWMWTCDSERKCCEGMVCRLWCKKKLW
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Disulfide Bond
2-16;9-21;15-25
PDB ID
2N9T , 5O0U , 5TCZ , 6MK4 , 6N4I , 6N4Q , 6N4R
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Arthropoda
Class: Arachnida
Order: Araneae
Family: Theraphosidae
Genus: Thrixopelma
Species: Thrixopelma pruriens
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    Kv1.5 Inhibition rate .
460 nM
Modifier
 [1- 20]
 Target Info    Kv1.2 Inhibition rate .
460 nM
Modifier
 [1- 20]
 Target Info    Kv1.3 Inhibition rate
2 %
460 nM
Modifier
 [1- 20]
 Target Info    Kv2.1 Inhibition rate
5 %
460 nM
Modifier
 [1- 20]
 Target Info    Cav3.3 Inhibition rate
8.9 %
1 μM
 . [1- 20]
 Target Info    Cav3.1 Inhibition rate
9 %
1 μM
 . [1- 20]
 Target Info    Cav1.2 Inhibition rate
29 %
1 μM
 . [1- 20]
 Target Info    Cav3.2 Inhibition rate
29 %
1 μM
 . [1- 20]
 Target Info    Cav3.1 Inhibition rate
81 %
5 μM
 . [1- 20]
 Target Info    Nav1.7 IC50
0.26 nM
 .
At -120mV
 [1- 20]
 Target Info    Nav1.7 IC50
0.26 - 3 nM
 . . [1- 20]
 Target Info    Nav1.7 IC50
1 - 1.5 nM
 . . [1- 20]
 Target Info    Nav1.7 IC50
15 nM
 .
At 0mV
 [1- 20]
 Target Info    Nav1.5 IC50
19 - 90 nM
 . . [1- 20]
 Target Info    Nav1.6 IC50
26 nM
 . . [1- 20]
 Target Info    Nav1.4 IC50
30 - 39 nM
 . . [1- 20]
 Target Info    Nav1.2 IC50
40 - 540 nM
 . . [1- 20]
 Target Info    Nav1.3 IC50
102 nM
 . . [1- 20]
 Target Info    Nav1.8 IC50
146 nM
 . . [1- 20]
 Target Info    Nav1.7 IC50
250 nM
 . . [1- 20]
 Target Info    Nav1.8 IC50
4.6 μM
 . . [1- 20]
 Target Info    Nav1.2 IC50
4.6 μM
 . . [1- 20]
 Target Info    Nav1.3 IC50
4.6 μM
 . . [1- 20]
 Target Info    Nav1.4 IC50
4.6 μM
 . . [1- 20]
 Target Info    Nav1.5 IC50
4.6 μM
 . . [1- 20]
 Target Info    Nav1.6 IC50
4.6 μM
 . . [1- 20]
References
Ref 1 Two tarantula peptides inhibit activation of multiple sodium channels. Biochemistry. 2002 Dec 17;41(50):14734-47. doi: 10.1021/bi026546a.
Ref 2 Differential phospholipid binding by site 3 and site 4 toxins. Implications for structural variability between voltage-sensitive sodium channel domains. J Biol Chem. 2005 Mar 25;280(12):11127-33. doi: 10.1074/jbc.M412552200. Epub 2005 Jan 4.
Ref 3 Molecular interactions of the gating modifier toxin ProTx-II with NaV 1.5: implied existence of a novel toxin binding site coupled to activation. J Biol Chem. 2007 Apr 27;282(17):12687-97. doi: 10.1074/jbc.M610462200. Epub 2007 Mar 5.
Ref 4 ProTx-I and ProTx-II: gating modifiers of voltage-gated sodium channels. Toxicon. 2007 Feb;49(2):194-201. doi: 10.1016/j.toxicon.2006.09.014. Epub 2006 Sep 27.
Ref 5 Inhibition of sodium channel gating by trapping the domain II voltage sensor with protoxin II. Mol Pharmacol. 2008 Mar;73(3):1020-8. doi: 10.1124/mol.107.041046. Epub 2007 Dec 21.
Ref 6 ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Mol Pharmacol. 2008 Nov;74(5):1476-84. doi: 10.1124/mol.108.047670. Epub 2008 Aug 26.
Ref 7 Evidence for multiple effects of ProTxII on activation gating in Na(V)1.5. Toxicon. 2008 Sep 1;52(3):489-500. doi: 10.1016/j.toxicon.2008.06.023. Epub 2008 Jul 9.
Ref 8 The tarantula toxins ProTx-II and huwentoxin-IV differentially interact with human Nav1.7 voltage sensors to inhibit channel activation and inactivation. Mol Pharmacol. 2010 Dec;78(6):1124-34. doi: 10.1124/mol.110.066332. Epub 2010 Sep 20.
Ref 9 Inhibition of the activation pathway of the T-type calcium channel Ca(V)3.1 by ProTxII. Toxicon. 2010 Sep 15;56(4):624-36. doi: 10.1016/j.toxicon.2010.06.009. Epub 2010 Jun 23.
Ref 10 Crystallographic insights into sodium-channel modulation by the 4 subunit. Proc Natl Acad Sci U S A. 2013 Dec 17;110(51):E5016-24. doi: 10.1073/pnas.1314557110. Epub 2013 Dec 2.
Ref 11 Block of T-type calcium channels by protoxins I and II. Mol Brain. 2014 May 9;7:36. doi: 10.1186/1756-6606-7-36.
Ref 12 High Proteolytic Resistance of Spider-Derived Inhibitor Cystine Knots. Int J Pept. 2015;2015:537508. doi: 10.1155/2015/537508. Epub 2015 Dec 30.
Ref 13 Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel. J Med Chem. 2015 Mar 12;58(5):2299-314. doi: 10.1021/jm501765v. Epub 2015 Feb 19.
Ref 14 Binary architecture of the Nav1.2-2 signaling complex. Elife. 2016 Feb 19;5:e10960. doi: 10.7554/eLife.10960.
Ref 15 Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor. Sci Rep. 2017 Jan 3;7:39662. doi: 10.1038/srep39662.
Ref 16 Chemical Synthesis, Proper Folding, Na(v) Channel Selectivity Profile and Analgesic Properties of the Spider Peptide Phlotoxin 1. Toxins (Basel). 2019 Jun 21;11(6):367. doi: 10.3390/toxins11060367.
Ref 17 Studies examining the relationship between the chemical structure of protoxin II and its activity on voltage gated sodium channels. J Med Chem. 2014 Aug 14;57(15):6623-31. doi: 10.1021/jm500687u. Epub 2014 Jul 24.
Ref 18 Interaction of Tarantula Venom Peptide ProTx-II with Lipid Membranes Is a Prerequisite for Its Inhibition of Human Voltage-gated Sodium Channel NaV1.7. J Biol Chem. 2016 Aug 12;291(33):17049-65. doi: 10.1074/jbc.M116.729095. Epub 2016 Jun 16.
Ref 19 Structural Basis of Nav1.7 Inhibition by a Gating-Modifier Spider Toxin. Cell. 2019 Feb 7;176(4):702-715.e14. doi: 10.1016/j.cell.2018.12.018. Epub 2019 Jan 17.
Ref 20 Structures of human Na(v)1.7 channel in complex with auxiliary subunits and animal toxins. Science. 2019 Mar 22;363(6433):1303-1308. doi: 10.1126/science.aaw2493. Epub 2019 Feb 14.
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