Target Information

General Information of This Target
Target ID
BTDT00081
Target Name
ATP-sensitive inward rectifier potassium channel 1 (Kcnj1)
Target Bioclass
Transporter and channel
Uniprot ID
P35560
3D Structure
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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
Kcnj1
Synonym
Romk1; ATP-regulated potassium channel ROM-K; Inward rectifier K(+) channel Kir1.1; KAB-1; Potassium channel, inwardly rectifying subfamily J member 1
Sequence
MGASERSVFRVLIRALTERMFKHLRRWFITHIFGRSRQRARLVSKEGRCNIEFGNVDAQS
RFIFFVDIWTTVLDLKWRYKMTVFITAFLGSWFLFGLLWYVVAYVHKDLPEFYPPDNRTP
CVENINGMTSAFLFSLETQVTIGYGFRFVTEQCATAIFLLIFQSILGVIINSFMCGAILA
KISRPKKRAKTITFSKNAVISKRGGKLCLLIRVANLRKSLLIGSHIYGKLLKTTITPEGE
TIILDQTNINFVVDAGNENLFFISPLTIYHIIDHNSPFFHMAAETLSQQDFELVVFLDGT
VESTSATCQVRTSYVPEEVLWGYRFVPIVSKTKEGKYRVDFHNFGKTVEVETPHCAMCLY
NEKDARARMKRGYDNPNFVLSEVDETDDTQM

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Family
the inward rectifier-type potassium channel family
Function
In the kidney, probably plays a major role in potassium homeostasis. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. This channel is activated by internal ATP and can be blocked by external barium.

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Taxonomy ID
10116
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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    Tertiapin Dissociation constant
2 nM
 [1- 9]
 Toxin Info    Kunitz-type serine protease inhibitor homolog delta-dendrotoxin Dissociation constant
152 nM
 [10], [11]
 Toxin Info    Potassium channel toxin alpha-KTx 1.2 Dissociation constant
410 nM
 [12], [13], [14]
 Toxin Info    Toxin 18-2 (N30A) Inhibition constant
190 nM
 [15]
 Toxin Info    Toxin 18-2 (R19A) Inhibition constant
260 nM
 [15]
 Toxin Info    Toxin 18-2 (K27A) Inhibition constant
4.01 μM
 [15]
 Toxin Info    Toxin 18-2 (R25A) Inhibition constant
18.97 μM
 [15]
 Toxin Info    Kunitz-type serine protease inhibitor homolog alpha-dendrotoxin Inhibition rate . [16]
 Toxin Info    Potassium channel toxin alpha-KTx 1.3 Inhibition rate . [15]
 Toxin Info    Mu-theraphotoxin-Pspp1 Inhibition rate . [17]
 Toxin Info    Potassium channel toxin alpha-KTx 3.2 Inhibition rate . [15]
 Toxin Info    Potassium channel toxin alpha-KTx 2.1 Inhibition rate . [15]
 Toxin Info    Potassium channel toxin alpha-KTx 2.2 Inhibition rate . [15]
 Toxin Info    Potassium channel toxin alpha-KTx 3.4 Inhibition rate . [15]
 Toxin Info    Potassium channel toxin alpha-KTx 1.1 Inhibition rate
10 %
 [15]
References
Ref 1 A novel high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry. 1998 Sep 22;37(38):13291-9. doi: 10.1021/bi981178p.
Ref 2 Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry. 1999 Oct 26;38(43):14286-93. doi: 10.1021/bi991205r.
Ref 3 Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry. 1999 Oct 26;38(43):14294-301. doi: 10.1021/bi991206j.
Ref 4 The bee venom peptide tertiapin underlines the role of I(KACh) in acetylcholine-induced atrioventricular blocks. Br J Pharmacol. 2000 Oct;131(3):569-77. doi: 10.1038/sj.bjp.0703611.
Ref 5 Titration of tertiapin-Q inhibition of ROMK1 channels by extracellular protons. Biochemistry. 2001 Mar 27;40(12):3601-5. doi: 10.1021/bi002584n.
Ref 6 Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner. J Pharmacol Exp Ther. 2005 Sep;314(3):1353-61. doi: 10.1124/jpet.105.085928. Epub 2005 Jun 9.
Ref 7 Tertiapin, a selective IKACh blocker, terminates atrial fibrillation with selective atrial effective refractory period prolongation. Pharmacol Res. 2006 Aug;54(2):136-41. doi: 10.1016/j.phrs.2006.03.021. Epub 2006 Apr 1.
Ref 8 Characterization of Kir1.1 channels with the use of a radiolabeled derivative of tertiapin. Biochemistry. 2006 Aug 22;45(33):10129-39. doi: 10.1021/bi060509s.
Ref 9 Solution structure of tertiapin determined using nuclear magnetic resonance and distance geometry. Proteins. 1993 Oct;17(2):124-37. doi: 10.1002/prot.340170203.
Ref 10 Snake venoms. The amino acid sequences of two proteinase inhibitor homologues from Dendroaspis angusticeps venom. Hoppe Seylers Z Physiol Chem. 1980 May;361(5):661-74. doi: 10.1515/bchm2.1980.361.1.661.
Ref 11 Energetic and structural interactions between delta-dendrotoxin and a voltage-gated potassium channel. J Mol Biol. 2000 Mar 10;296(5):1283-94. doi: 10.1006/jmbi.2000.3522.
Ref 12 Dynamic diversification from a putative common ancestor of scorpion toxins affecting sodium, potassium, and chloride channels. J Mol Evol. 1999 Feb;48(2):187-96. doi: 10.1007/pl00006457.
Ref 13 Analysis of the blocking activity of charybdotoxin homologs and iodinated derivatives against Ca2+-activated K+ channels. J Membr Biol. 1989 Aug;109(3):269-81. doi: 10.1007/BF01870284.
Ref 14 Neuromuscular effects of some potassium channel blocking toxins from the venom of the scorpion Leiurus quinquestriatus hebreus. Toxicon. 1994 Nov;32(11):1433-43. doi: 10.1016/0041-0101(94)90415-4.
Ref 15 Purification, characterization, and synthesis of an inward-rectifier K+ channel inhibitor from scorpion venom. Biochemistry. 1997 Jun 10;36(23):6936-40. doi: 10.1021/bi9702849.
Ref 16 A snake toxin inhibitor of inward rectifier potassium channel ROMK1. Biochemistry. 1998 Oct 20;37(42):14867-74. doi: 10.1021/bi980929k.
Ref 17 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 18 Engineered specific and high-affinity inhibitor for a subtype of inward-rectifier K+ channels. Proc Natl Acad Sci U S A. 2008 Aug 5;105(31):10774-8. doi: 10.1073/pnas.0802850105. Epub 2008 Jul 31.
Ref 19 Antidepressive effect of an inward rectifier K+ channel blocker peptide, tertiapin-RQ. PLoS One. 2020 Nov 13;15(11):e0233815. doi: 10.1371/journal.pone.0233815. eCollection 2020.
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