Target Information

General Information of This Target
Target ID
BTDT00012
Target Name
Potassium voltage-gated channel subfamily H member 2 (Kcnh2)
Target Bioclass
Transporter and channel
Uniprot ID
O08962
3D Structure
Download
2D Sequence
3D Structure
Source
Predict by Alphafold2
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Alphafold Parameters: msa_mode: mmseqs2_uniref_env model_type: auto num_recycles: auto
Gene Name
Kcnh2
Gene ID
117018
Synonym
Erg; Ether-a-go-go-related gene potassium channel 1; Voltage-gated potassium channel subunit Kv11.1
Sequence
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPSTSWLASGRAKTFRLKLPALLALTARESPM
RTGSTGSPGAPGAVVVDVDLTPAAPSSESLALDEVSAMDNHVAGLGPAEERRALVGPASA
SPVASIPGPHPSPRAQSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGALPL
PPRHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREI
IAPKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLV
IYTAVFTPYSAAFLLKETEDGSQAPDCGYACQPLAVVDLLVDIMFIVDILINFRTTYVNA
NEEVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARK
LDRYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSHIGWLHNLGDQIGKPYN
SSGLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGN
VSAIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLK
GFPECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTA
LYFISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDL
LEVLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPSSAELESGFNRQRKRKLSFRRRTDKD
TEQPGEVSALGQGPARVGPGPSCRGQPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLV
PFSSPRPPGDSPGGEPLTEDGEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCP
APAPSLLNIPLSSPGRRSRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPP
AYSAVTTPGPGPTSTSPLLPVGPVPTLTLDSLSQVSQFVAFEELPAGAPELPQDGPTRRL
SLPGQLGALTSQPLHRHGSDPGS

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Family
the potassium channel family
Function
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr).

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Taxonomy ID
10116
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Rodentia
Family: Muridae
Genus: Rattus
Species: Rattus norvegicus
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Potassium channel toxin gamma-KTx 1.1 Dissociation constant
6.8 nM
 [1- 12]
 Toxin Info    Potassium channel toxin gamma-KTx 1.1 Dissociation constant
6.8 nM
 [1- 27]
 Toxin Info    Potassium channel toxin gamma-KTx 2.1 Dissociation constant
19 nM
 [1- 34]
 Toxin Info    Potassium channel toxin gamma-KTx 2.1 Dissociation constant
19 nM
 [1- 34]
 Toxin Info    APETx2 Inhibition rate . [35- 44]
References
Ref 1 A large number of novel Ergtoxin-like genes and ERG K+-channels blocking peptides from scorpions of the genus Centruroides. FEBS Lett. 2002 Dec 4;532(1-2):121-6. doi: 10.1016/s0014-5793(02)03652-9.
Ref 2 A toxin to nervous, cardiac, and endocrine ERG K+ channels isolated from Centruroides noxius scorpion venom. FASEB J. 1999 May;13(8):953-62.
Ref 3 Disulfide bridges of ergtoxin, a member of a new sub-family of peptide blockers of the ether-a-go-go-related K+ channel. FEBS Lett. 2000 Aug 18;479(3):156-7. doi: 10.1016/s0014-5793(00)01891-3.
Ref 4 Mapping the receptor site for ergtoxin, a specific blocker of ERG channels. FEBS Lett. 2002 Jan 2;510(1-2):45-9. doi: 10.1016/s0014-5793(01)03218-5.
Ref 5 Mapping the binding site of a human ether-a-go-go-related gene-specific peptide toxin (ErgTx) to the channel's outer vestibule. J Biol Chem. 2002 May 10;277(19):16403-11. doi: 10.1074/jbc.M200460200. Epub 2002 Feb 25.
Ref 6 Preferential closed channel blockade of HERG potassium currents by chemically synthesised BeKm-1 scorpion toxin. FEBS Lett. 2003 Jul 17;547(1-3):20-6. doi: 10.1016/s0014-5793(03)00662-8.
Ref 7 Species diversity and peptide toxins blocking selectivity of ether-a-go-go-related gene subfamily K+ channels in the central nervous system. Mol Pharmacol. 2006 May;69(5):1673-83. doi: 10.1124/mol.105.019729. Epub 2006 Feb 23.
Ref 8 Mechanism of block of the hERG K+ channel by the scorpion toxin CnErg1. Biophys J. 2007 Jun 1;92(11):3915-29. doi: 10.1529/biophysj.106.101956. Epub 2007 Mar 16.
Ref 9 Recombinant expression of the toxic peptide ErgTx1 and role of Met35 on its stability and function. Peptides. 2011 Mar;32(3):560-7. doi: 10.1016/j.peptides.2010.06.018. Epub 2010 Jun 30.
Ref 10 Positive selection-guided mutational analysis revealing two key functional sites of scorpion ERG K(+) channel toxins. Biochem Biophys Res Commun. 2012 Dec 7;429(1-2):111-6. doi: 10.1016/j.bbrc.2012.10.065. Epub 2012 Oct 24.
Ref 11 Solution structure of CnErg1 (Ergtoxin), a HERG specific scorpion toxin. FEBS Lett. 2003 Mar 27;539(1-3):138-42. doi: 10.1016/s0014-5793(03)00216-3.
Ref 12 Exploring structural features of the interaction between the scorpion toxinCnErg1 and ERG K+ channels. Proteins. 2004 Aug 1;56(2):367-75. doi: 10.1002/prot.20102.
Ref 13 Erratum to "From goal to outcome: Analyzing the progression of biomedical sciences PhD careers in a longitudinal study using an expanded taxonomy". FASEB Bioadv. 2023 Dec 1;6(1):40. doi: 10.1096/fba.2023-00134. eCollection 2024 Jan.
Ref 14 Retraction: Methionine-CBS axis promotes intracellular ROS levels by reprogramming serine metabolism. FASEB J. 2024 Jan 31;38(2):e23412. doi: 10.1096/fsb2.23412.
Ref 15 Gross Anatomy Teaching for Medical Undergraduates Through Computer-Based Simulation: Introduction and Evaluation of Effectiveness. Cureus. 2023 Nov 27;15(11):e49517. doi: 10.7759/cureus.49517. eCollection 2023 Nov.
Ref 16 Erratum to "The roles of HMGB1-produced DNA gaps in DNA protection and aging biomarker reversal". FASEB Bioadv. 2023 Jan 25;5(2):85-87. doi: 10.1096/fba.1365. eCollection 2023 Feb.
Ref 17 Erratum. FASEB Bioadv. 2021 Jun 3;3(7):558. doi: 10.1096/fba.1251. eCollection 2021 Jul.
Ref 18 WITHDRAWN: Adipocyte Deletion of ADAM17 Leads to Insulin Resistance in Association with Age and HFD in Mice. FASEB J. 2021 May;35 Suppl 1. doi: 10.1096/fasebj.2021.35.S1.00447.
Ref 19 RETRACTED: circTulp4 functions in Alzheimers disease pathogenesis by regulating its parental gene, Tulp4. Mol Ther. 2021 Jun 2;29(6):2167-2181. doi: 10.1016/j.ymthe.2021.02.008. Epub 2021 Feb 10.
Ref 20 BCL-2 Inhibitor Venetoclax Induces Autophagy-Associated Cell Death, Cell Cycle Arrest, and Apoptosis in Human Breast Cancer Cells. Onco Targets Ther. 2020 Dec 31;13:13357-13370. doi: 10.2147/OTT.S281519. eCollection 2020.
Ref 21 Anatomical Study of the Innervation of the Masseter Muscle and Its Correlation with Myofascial Trigger Points. J Pain Res. 2020 Dec 2;13:3217-3226. doi: 10.2147/JPR.S265717. eCollection 2020.
Ref 22 Withdrawn: A Controllable Protein Translation Strategy for Exploring Cellular Signal Transduction Based on Reading through Premature Termination Codons. FASEB J. 2020 Apr;34(S1):1. doi: 10.1096/fasebj.2020.34.s1.09195.
Ref 23 Withdrawn: Invisible State of MdmX and Design of its Inhibitors. FASEB J. 2020 Apr;34(S1):1. doi: 10.1096/fasebj.2020.34.s1.09193.
Ref 24 Experimental Biology 2020 Meeting Abstracts. FASEB J. 2020 Apr;34(S1):1. doi: 10.1096/fasebj.2020.34.s1.07600.
Ref 25 A novel small animal model for HIV-1 infection. FASEB J. 2005 Jul;19(9):1149-51. doi: 10.1096/fj.04-3184fje. Epub 2005 Apr 15.
Ref 26 Enhanced HIV-1 specific immune response by CpG ODN and HIV-1 immunogen-pulsed dendritic cells confers protection in the Trimera murine model of HIV-1 infection. FASEB J. 2005 Jul;19(9):1152-4. doi: 10.1096/fj.04-3185fje. Epub 2005 Apr 15.
Ref 27 Abnormalities in intracellular Ca2+ regulation in fetal vascular smooth muscle in pre-eclampsia: enhanced sensitivity to arachidonic acid. FASEB J. 2003 Feb;17(2):307-9. doi: 10.1096/fj.02-0507fje. Epub 2002 Dec 17.
Ref 28 An ERG channel inhibitor from the scorpion Buthus eupeus. J Biol Chem. 2001 Mar 30;276(13):9868-76. doi: 10.1074/jbc.M005973200. Epub 2001 Jan 2.
Ref 29 M-type K+ current inhibition by a toxin fron the scorpion Buthus eupeus. FEBS Lett. 1996 Apr 22;384(3):277-80. doi: 10.1016/0014-5793(96)00333-x.
Ref 30 BeKm-1 is a HERG-specific toxin that shares the structure with ChTx but the mechanism of action with ErgTx1. Biophys J. 2003 May;84(5):3022-36. doi: 10.1016/S0006-3495(03)70028-9.
Ref 31 Unique interaction of scorpion toxins with the hERG channel. J Mol Recognit. 2004 May-Jun;17(3):209-17. doi: 10.1002/jmr.667.
Ref 32 BeKm-1, a peptide inhibitor of human ether-a-go-go-related gene potassium currents, prolongs QTc intervals in isolated rabbit heart. J Pharmacol Exp Ther. 2011 Apr;337(1):2-8. doi: 10.1124/jpet.110.176883. Epub 2010 Dec 23.
Ref 33 Interaction simulation of hERG K+ channel with its specific BeKm-1 peptide: insights into the selectivity of molecular recognition. J Proteome Res. 2007 Feb;6(2):611-20. doi: 10.1021/pr060368g.
Ref 34 New binding site on common molecular scaffold provides HERG channel specificity of scorpion toxin BeKm-1. J Biol Chem. 2002 Nov 8;277(45):43104-9. doi: 10.1074/jbc.M204083200. Epub 2002 Jul 31.
Ref 35 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 36 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 37 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 38 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 39 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 40 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 41 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 42 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 43 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 44 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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