Target Information

General Information of This Target
Target ID
BTDT00227
Target Name
G protein-activated inward rectifier potassium channel 1 (Kcnj3);G protein-activated inward rectifier potassium channel 4 (Kcnj5)
Target Bioclass
Transporter and channel
Uniprot ID
P63251 ; P48548
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
Kcnj3;Kcnj5
Gene ID
50599 ; 29713
Synonym 1
Inward rectifier K(+) channel Kir3.1; KGA; KGB1; Potassium channel, inwardly rectifying subfamily J member 3
Synonym 2
Cardiac inward rectifier; Heart KATP channel; Inward rectifier K(+) channel Kir3.4; KATP-1; Potassium channel, inwardly rectifying subfamily J member 5
Sequence 1
MSALRRKFGDDYQVVTTSSSGSGLQPQGPGQGPQQQLVPKKKRQRFVDKNGRCNVQHGNL
GSETSRYLSDLFTTLVDLKWRWNLFIFILTYTVAWLFMASMWWVIAYTRGDLNKAHVGNY
TPCVANVYNFPSAFLFFIETEATIGYGYRYITDKCPEGIILFLFQSILGSIVDAFLIGCM
FIKMSQPKKRAETLMFSEHAVISMRDGKLTLMFRVGNLRNSHMVSAQIRCKLLKSRQTPE
GEFLPLDQLELDVGFSTGADQLFLVSPLTICHVIDAKSPFYDLSQRSMQTEQFEVVVILE
GIVETTGMTCQARTSYTEDEVLWGHRFFPVISLEEGFFKVDYSQFHATFEVPTPPYSVKE
QEEMLLMSSPLIAPAITNSKERHNSVECLDGLDDISTKLPSKLQKITGREDFPKKLLRMS
STTSEKAYSLGDLPMKLQRISSVPGNSEEKLVSKTTKMLSDPMSQSVADLPPKLQKMAGG
PTRMEGNLPAKLRKMNSDRFT

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Sequence 2
MAGDSRNAMNQDMEIGVTSQDHKKIPKQARDYIPIATDRTRLLPEGKKPRQRYMEKTGKC
NVHHGNVQETYRYLSDLFTTLVDLKWRFNLLVFTMVYTITWLFFGFIWWLIAYVRGDLDH
VGDQEWIPCVENLSGFVSAFLFSIETETTIGYGFRVITEKCPEGIILLLVQAILGSIVNA
FMVGCMFVKISQPKKRAETLMFSNNAVISMRDEKLCLMFRVGDLRNSHIVEASIRAKLIK
SRQTKEGEFIPLNQTDINVGFDTGDDRLFLVSPLIISHEINEKSPFWEMSRAQLEQEEFE
VVVILEGMVEATGMTCQARSSYMDTEVLWGHRFTPVLTLEKGFYEVDYNTFHDTYETNTP
SCCAKELAEMKRNGQLLQSLPSPPLLGGCAEAEKEAEAEHDEEEEPNGLSVSRATRGSM

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Family1
the inward inward rectifier-type potassium channel (TC 1.A.2.1) family.
Family2
the inward rectifier-type potassium channel (TC 1.A.2.1) family
Function 1
This potassium channel is controlled by G proteins. 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 receptor plays a crucial role in regulating; the heartbeat.

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Function 2
This potassium channel is controlled by G proteins. 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. Can be blocked by external barium.

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Taxonomy ID
10116
TCDB ID
. ; .
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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
8.6 nM
 [1- 9]
 Toxin Info    Potassium channel toxin alpha-KTx 1.1 Inhibition rate . [1]
 Toxin Info    Potassium channel toxin alpha-KTx 1.2 Inhibition rate
5 %
 [1]
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 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.
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