Peptide Information

General Information of This Peptide
Peptide ID
BTDP008684
Peptide Name
APETx2
Symonym
Toxin APETx2;Pi-actitoxin-Ael2b
Species
Anthopleura elegantissima (Green aggregating anemone) (Actinia elegantissima)
Uniprot Name
BDS2_ANTEL
Alphafold ID
P61542
3D Structure
Download
2D Sequence
3D Structure
Source
RSCB PDB: 1WXN
Sequence
GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD
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Sequence Length
42
Mass (Da)
4567
Sequence Removed Signal Peptide
GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD
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Disulfide Bond
4-37;6-30;20-38
PDB ID
1WXN , 2MUB
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Cnidaria
Class: Anthozoa
Order: Actiniaria
Family: Actiniidae
Genus: Anthopleura
Species: Anthopleura elegantissima
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    Kv11.1 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv1.4 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv4.1 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv4.1 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv4.3 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv2.2 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv4.2 Inhibition rate .
300 nM
 . [1- 10]
 Target Info    Kv3.4 Inhibition rate
17 %
1 μM
Heterotrimeric
 [1- 10]
 Target Info    Nav1.6 Inhibition rate
17 %
1 μM
Heterotrimeric
 [1- 10]
 Target Info    Kv3.4 Inhibition rate
38 %
3 μM
Heterotrimeric
 [1- 10]
 Target Info    Kv3.4 Inhibition rate
38 %
3 μM
 . [1- 10]
 Target Info    Nav1.8 Effective concentration 50
2.6 nM
 . . [1- 10]
 Target Info    Nav1.8 Effective concentration 50
55 nM
 . . [1- 10]
 Target Info    Nav1.2 Effective concentration 50
114 nM
 .
Heterotrimeric
 [1- 10]
 Target Info    ASIC3 IC50
37.3 nM
 .
Homomeric
 [1- 10]
 Target Info    ASIC3 IC50
57 - 87 nM
 .
Homomeric
 [1- 10]
 Target Info    ASIC2b-ASIC3 IC50
117 nM
 .
Heterotrimeric
 [1- 10]
 Target Info    ASIC3 IC50
175 nM
 .
Homomeric
 [1- 10]
 Target Info    ASIC1b-ASIC3 IC50
900 nM
 .
Heterotrimeric
 [1- 10]
 Target Info    Kv11 IC50
1.21 μM
 . . [1- 10]
 Target Info    Kv11 IC50
1.21 μM
 .
Heterotrimeric
 [1- 10]
 Target Info    ASIC1b-ASIC3 IC50
2 μM
 .
Heterotrimeric
 [1- 10]
 Target Info    Nav1.8 IC50
6.6 μM
 . . [1- 10]
References
Ref 1 A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. 2004 Apr 7;23(7):1516-25. doi: 10.1038/sj.emboj.7600177. Epub 2004 Mar 25.
Ref 2 ASIC3, a sensor of acidic and primary inflammatory pain. EMBO J. 2008 Nov 19;27(22):3047-55. doi: 10.1038/emboj.2008.213. Epub 2008 Oct 16.
Ref 3 Chemical synthesis and folding of APETx2, a potent and selective inhibitor of acid sensing ion channel 3. Toxicon. 2009 Jul;54(1):56-61. doi: 10.1016/j.toxicon.2009.03.014. Epub 2009 Mar 21.
Ref 4 Expression in Pichia pastoris and characterization of APETx2, a specific inhibitor of acid sensing ion channel 3. Toxicon. 2010 Dec;56(8):1388-97. doi: 10.1016/j.toxicon.2010.08.004. Epub 2010 Sep 9.
Ref 5 Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Br J Pharmacol. 2012 Apr;165(7):2167-77. doi: 10.1111/j.1476-5381.2011.01674.x.
Ref 6 A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. 2012 Dec;26(12):5141-51. doi: 10.1096/fj.12-218479. Epub 2012 Sep 12.
Ref 7 Cyclisation increases the stability of the sea anemone peptide APETx2 but decreases its activity at acid-sensing ion channel 3. Mar Drugs. 2012 Jul;10(7):1511-1527. doi: 10.3390/md10071511. Epub 2012 Jul 16.
Ref 8 Functional expression in Escherichia coli of the disulfide-rich sea anemone peptide APETx2, a potent blocker of acid-sensing ion channel 3. Mar Drugs. 2012 Jul;10(7):1605-1618. doi: 10.3390/md10071605. Epub 2012 Jul 23.
Ref 9 Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton-gated channels. Protein Sci. 2005 Aug;14(8):2003-10. doi: 10.1110/ps.051378905. Epub 2005 Jun 29.
Ref 10 Understanding the molecular basis of toxin promiscuity: the analgesic sea anemone peptide APETx2 interacts with acid-sensing ion channel 3 and hERG channels via overlapping pharmacophores. J Med Chem. 2014 Nov 13;57(21):9195-203. doi: 10.1021/jm501400p. Epub 2014 Nov 4.
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