Target Information
General Information of This Target
| Target ID |
BTDT00139
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| Target Name |
Potassium voltage-gated channel subfamily B member 1 (KCNB1)
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| Target Bioclass |
Transporter and channel
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| Uniprot ID | ||||||
| 3D Structure | ||||||
| Gene Name |
KCNB1
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| Gene ID | ||||||
| Synonym |
Delayed rectifier potassium channel 1; Voltage-gated potassium channel subunit Kv2.1
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| Sequence |
MPAGMTKHGSRSTSSLPPEPMEIVRSKACSRRVRLNVGGLAHEVLWRTLDRLPRTRLGKL
RDCNTHDSLLEVCDDYSLDDNEYFFDRHPGAFTSILNFYRTGRLHMMEEMCALSFSQELD YWGIDEIYLESCCQARYHQKKEQMNEELKREAETLREREGEEFDNTCCAEKRKKLWDLLE KPNSSVAAKILAIISIMFIVLSTIALSLNTLPELQSLDEFGQSTDNPQLAHVEAVCIAWF TMEYLLRFLSSPKKWKFFKGPLNAIDLLAILPYYVTIFLTESNKSVLQFQNVRRVVQIFR IMRILRILKLARHSTGLQSLGFTLRRSYNELGLLILFLAMGIMIFSSLVFFAEKDEDDTK FKSIPASFWWATITMTTVGYGDIYPKTLLGKIVGGLCCIAGVLVIALPIPIIVNNFSEFY KEQKRQEKAIKRREALERAKRNGSIVSMNMKDAFARSIEMMDIVVEKNGENMGKKDKVQD NHLSPNKWKWTKRTLSETSSSKSFETKEQGSPEKARSSSSPQHLNVQQLEDMYNKMAKTQ SQPILNTKESAAQSKPKEELEMESIPSPVAPLPTRTEGVIDMRSMSSIDSFISCATDFPE ATRFSHSPLTSLPSKTGGSTAPEVGWRGALGASGGRFVEANPSPDASQHSSFFIESPKSS MKTNNPLKLRALKVNFMEGDPSPLLPVLGMYHDPLRNRGSAAAAVAGLECATLLDKAVLS PESSIYTTASAKTPPRSPEKHTAIAFNFEAGVHQYIDADTDDEGQLLYSVDSSPPKSLPG STSPKFSTGTRSEKNHFESSPLPTSPKFLRQNCIYSTEALTGKGPSGQEKCKLENHISPD VRVLPGGGAHGSTRDQSI Click to Show/Hide
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| Family |
the potassium channel family
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| Function |
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain, but also in the pancreas and cardiovascular system. Contributes to the regulation of the action potential (AP) repolarization, duration and frequency of repetitive AP firing in neurons, muscle cells and endocrine cells and plays a role in homeostatic attenuation of electrical excitability throughout the brain. Plays also a role in the regulation of exocytosis independently of its electrical function. Forms tetrameric potassium- selective channels through which potassium ions pass in accordance with their electrochemical gradient. The channel alternates between opened and closed conformations in response to the voltage difference across the membrane. Homotetrameric channels mediate a delayed-rectifier voltage-dependent outward potassium current that display rapid activation and slow inactivation in response to membrane depolarization. Can form functional homotetrameric and heterotetrameric channels that contain variable proportions of KCNB2; channel properties depend on the type of alpha subunits that are part of the channel. Can also form functional heterotetrameric channels with other alpha subunits that are non-conducting when expressed alone, such as KCNF1, KCNG1, KCNG3, KCNG4, KCNH1, KCNH2, KCNS1, KCNS2, KCNS3 and KCNV1, creating a functionally diverse range of channel complexes. Heterotetrameric channel activity formed with KCNS3 show increased current amplitude with the threshold for action potential activation shifted towards more negative values in hypoxic- treated pulmonary artery smooth muscle cells. Channel properties are also modulated by cytoplasmic ancillary beta subunits such as AMIGO1, KCNE1, KCNE2 and KCNE3, slowing activation and inactivation rate of the delayed rectifier potassium channels. In vivo, membranes probably contain a mixture of heteromeric potassium channel complexes, making it difficult to assign currents observed in intact tissues to any particular potassium channel family member. Major contributor to the slowly inactivating delayed- rectifier voltage-gated potassium current in neurons of the central nervous system, sympathetic ganglion neurons, neuroendocrine cells, pancreatic beta cells, cardiomyocytes and smooth muscle cells. Mediates the major part of the somatodendritic delayed-rectifier potassium current in hippocampal and cortical pyramidal neurons and sympathetic superior cervical ganglion (CGC) neurons that acts to slow down periods of firing, especially during high frequency stimulation. Plays a role in the induction of long-term potentiation (LTP) of neuron excitability in the CA3 layer of the hippocampus. Contributes to the regulation of glucose-induced action potential amplitude and duration in pancreatic beta cells, hence limiting calcium influx and insulin secretion. Plays a role in the regulation of resting membrane potential and contraction in hypoxia-treated pulmonary artery smooth muscle cells. May contribute to the regulation of the duration of both the action potential of cardiomyocytes and the heart ventricular repolarization QT interval. Contributes to the pronounced pro-apoptotic potassium current surge during neuronal apoptotic cell death in response to oxidative injury. May confer neuroprotection in response to hypoxia/ischemic insults by suppressing pyramidal neurons hyperexcitability in hippocampal and cortical regions. Promotes trafficking of KCNG3, KCNH1 and KCNH2 to the cell surface membrane, presumably by forming heterotetrameric channels with these subunits. Plays a role in the calcium-dependent recruitment and release of fusion-competent vesicles from the soma of neurons, neuroendocrine and glucose-induced pancreatic beta cells by binding key components of the fusion machinery in a pore-independent manner.
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| Taxonomy ID | ||||||
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| Click to Show/Hide the Complete Species Lineage | ||||||
Toxin Information Related to This Target
| Toxin Name | Activity Data Type | Activity Data | Reference |
|---|---|---|---|
| Toxin Info GxTx1E (S13C,K27[Pra],M35[Nle]) | Dissociation constant |
0.83 nM
|
[1] |
| Toxin Info Kappa-theraphotoxin-Pg1a | Dissociation constant |
5.1 nM
|
[2], [3], [4], [5] |
| Toxin Info GxTx1E (S13C,M35[Nle]) | Dissociation constant |
26.9 nM
|
[6] |
| Toxin Info Kappa-theraphotoxin-Gr1a | Dissociation constant |
102 nM
|
[3- 12] |
| Toxin Info Toxin LmKTx2 | Dissociation constant |
125 nM
|
[13] |
| Toxin Info GxTx1E (M35[Nle]) | Dissociation constant |
224 nM
|
[13] |
| Toxin Info GxTx1E (M35[Nle],P36A) | Dissociation constant |
250 nM
|
[13] |
| Toxin Info GxTx1E (M35A) | Dissociation constant |
306 nM
|
[13] |
| Toxin Info GxTx1E (P34A,M35[Nle]) | Dissociation constant |
348 nM
|
[13] |
| Toxin Info GxTx1E (G6A,M35[Nle]) | Dissociation constant |
379 nM
|
[13] |
| Toxin Info GxTx1E (E1A,M35[Nle]) | Dissociation constant |
414 nM
|
[13] |
| Toxin Info GxTx1E (K21A,M35[Nle]) | Dissociation constant |
440 nM
|
[13] |
| Toxin Info GxTx1E (G14A,M35[Nle]) | Dissociation constant |
461 nM
|
[13] |
| Toxin Info GxTx1E (F33A,M35[Nle]) | Dissociation constant |
491 nM
|
[13] |
| Toxin Info GxTx1E (V23A,M35[Nle]) | Dissociation constant |
516 nM
|
[13] |
| Toxin Info GxTx1E (S13A,M35[Nle]) | Dissociation constant |
545 nM
|
[13] |
| Toxin Info GxTx1E (P20A,M35[Nle]) | Dissociation constant |
652 nM
|
[13] |
| Toxin Info GxTx1E (K27A,M35[Nle]) | Dissociation constant |
763 nM
|
[13] |
| Toxin Info GxTx1E (P26A,M35[Nle]) | Dissociation constant |
813 nM
|
[13] |
| Toxin Info GxTx1E (N32A,M35[Nle]) | Dissociation constant |
1.228 μM
|
[13] |
| Toxin Info GxTx1E (L30A,M35[Nle]) | Dissociation constant |
2.474 μM
|
[13] |
| Toxin Info GxTx1E (W9A,M35[Nle]) | Dissociation constant |
5.837 μM
|
[13] |
| Toxin Info GxTx1E (W8A,M35[Nle]) | Dissociation constant |
9.641 μM
|
[13] |
| Toxin Info GxTx1E (G5A,M35[Nle]) | Dissociation constant |
13.652 μM
|
[13] |
| Toxin Info Omega-theraphotoxin-Gr1a | Dissociation constant |
19 μM
|
[10- 18] |
| Toxin Info GxTx1E (G12A,M35[Nle]) | Dissociation constant |
21.755 μM
|
[13] |
| Toxin Info GxTx1E (P16A,M35[Nle]) | Dissociation constant |
22.967 μM
|
[13] |
| Toxin Info GxTx1E (Y22A,M35[Nle]) | Dissociation constant |
35.337 μM
|
[13] |
| Toxin Info GxTx1E (F7A,M35[Nle]) | Dissociation constant |
89.033 μM
|
[13] |
| Toxin Info Potassium channel toxin ShK ([pTyr][AEEA]) | Inhibition rate | . | [19] |
| Toxin Info Jingzhaotoxin F7-15.33 | Inhibition rate | . | [20] |
| Toxin Info Apamin | Inhibition rate | . | [21- 38] |
| Toxin Info Kappa-stichotoxin-She3a | Inhibition rate | . | [39] |
| Toxin Info Mu-theraphotoxin-Cg1a | Inhibition rate | . | [40], [41], [42], [43] |
| Toxin Info U-actitoxin-Oulsp1 | Inhibition rate | . | [44] |
| Toxin Info Potassium channel toxin gamma-KTx 1.1 | Inhibition rate | . | [45- 56] |
| Toxin Info Beta/omega-theraphotoxin-Tp2a | Inhibition rate |
5 %
|
[57- 76] |
| Toxin Info Pi-stichotoxin-Hcr5b | Inhibition rate |
33 %
|
[77] |
| Toxin Info Kappa-actitoxin-Ael2e | Inhibition rate |
39 %
|
[78] |
| Toxin Info Beta/omega-theraphotoxin-Tp1a | Inhibition rate |
60 %
|
[57- 82] |
| Toxin Info Kappa-theraphotoxin-Pg1b | IC50 |
1.7 nM
|
[2] |
| Toxin Info Beta/omega-theraphotoxin-Tp1a | IC50 |
411 nM
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[57- 82] |
| Toxin Info Delta/kappa-theraphotoxin-Pm1a | IC50 |
430 nM
|
[83] |
| Toxin Info VsTx1 | IC50 |
1.22 μM
|
[84] |
| Toxin Info U20-theraphotoxin-Cg1a 1 | IC50 |
3.62 μM
|
[85] |
References
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