Target Information
General Information of This Target
| Target ID |
BTDT00057
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| Target Name |
Potassium voltage-gated channel subfamily A member 1
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| Target Bioclass |
Transporter and channel
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| Uniprot ID | ||||||
| 3D Structure | ||||||
| Gene ID | ||||||
| Synonym |
MBK1; MKI; Voltage-gated potassium channel subunit Kv1.1
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| Sequence |
MTVMSGENADEASTAPGHPQDGSYPRQADHDDHECCERVVINISGLRFETQLKTLAQFPN
TLLGNPKKRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRLRRPVNVPLDMFSEEIKFY ELGEEAMEKFREDEGFIKEEERPLPEKEYQRQVWLLFEYPESSGPARVIAIVSVMVILIS IVIFCLETLPELKDDKDFTGTIHRIDNTTVIYTSNIFTDPFFIVETLCIIWFSFELVVRF FACPSKTDFFKNIMNFIDIVAIIPYFITLGTEIAEQEGNQKGEQATSLAILRVIRLVRVF RIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEAEEAESHFSSIP DAFWWAVVSMTTVGYGDMYPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETE GEEQAQLLHVSSPNLASDSDLSRRSSSTISKSEYMEIEEDMNNSIAHYRQANIRTGNCTT ADQNCVNKSKLLTDV 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 and the central nervous system, but also in the kidney. Contributes to the regulation of the membrane potential and nerve signaling, and prevents neuronal hyperexcitability. 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. Can form functional homotetrameric channels and heterotetrameric channels that contain variable proportions of KCNA1, KCNA2, KCNA4, KCNA5, KCNA6, KCNA7, and possibly other family members as well; channel properties depend on the type of alpha subunits that are part of the channel. Channel properties are modulated by cytoplasmic beta subunits that regulate the subcellular location of the alpha subunits and promote rapid inactivation of 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. Homotetrameric KCNA1 forms a delayed- rectifier potassium channel that opens in response to membrane depolarization, followed by slow spontaneous channel closure. In contrast, a heterotetrameric channel formed by KCNA1 and KCNA4 shows rapid inactivation. Regulates neuronal excitability in hippocampus, especially in mossy fibers and medial perforant path axons, preventing neuronal hyperexcitability. May function as down-stream effector for G protein-coupled receptors and inhibit GABAergic inputs to basolateral amygdala neurons. May contribute to the regulation of neurotransmitter release, such as gamma-aminobutyric acid (GABA) release. Plays a role in regulating the generation of action potentials and preventing hyperexcitability in myelinated axons of the vagus nerve, and thereby contributes to the regulation of heart contraction. Required for normal neuromuscular responses. Regulates the frequency of neuronal action potential firing in response to mechanical stimuli, and plays a role in the perception of pain caused by mechanical stimuli, but does not play a role in the perception of pain due to heat stimuli. Required for normal responses to auditory stimuli and precise location of sound sources, but not for sound perception. The use of toxins that block specific channels suggest that it contributes to the regulation of the axonal release of the neurotransmitter dopamine. Required for normal postnatal brain development and normal proliferation of neuronal precursor cells in the brain. Plays a role in the reabsorption of Mg(2+) in the distal convoluted tubules in the kidney and in magnesium ion homeostasis, probably via its effect on the membrane potential.
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| Taxonomy ID | ||||||
| Click to Show/Hide the Complete Species Lineage | ||||||
Toxin Information Related to This Target
| Toxin Name | Activity Data Type | Activity Data | Reference |
|---|---|---|---|
| Toxin Info Potassium channel toxin alpha-KTx 2.1 | Dissociation constant |
>25 nM
|
[1], [2], [3], [4] |
| Toxin Info Potassium channel toxin ShK ([pTyrMe][AEEA]) | Dissociation constant |
0.112 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([Apa][AEEA]) | Dissociation constant |
0.142 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK (Y[AEEA] | Dissociation constant |
0.159 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([Pmp2Et]D[AEEA]) | Dissociation constant |
0.166 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([pTyr2Me][AEEA]) | Dissociation constant |
0.175 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([Cpa][AEEA]) | Dissociation constant |
0.319 nM
|
[5] |
| Toxin Info Potassium channel toxin alpha-KTx 23.1 | Dissociation constant |
0.8 nM
|
[6] |
| Toxin Info Potassium channel toxin ShK ([Pmp][AEEA]) | Dissociation constant |
1 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([Pmp2Et][AEEA]) | Dissociation constant |
1.1 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([PmpEtD][AEEA]) | Dissociation constant |
1.1 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([PmpD][AEEA]) | Dissociation constant |
1.4 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK (K22[Dap]) | Dissociation constant |
1.8 nM
|
[5] |
| Toxin Info Potassium channel toxin ShK ([pTyr][AEEA]) | Dissociation constant |
7 nM
|
[5] |
| Toxin Info Potassium channel toxin Bgk (F6A) | Dissociation constant |
7.3 nM
|
[7] |
| Toxin Info Kappa-actitoxin-Bgr1a | Dissociation constant |
17 nM
|
[7] |
| Toxin Info Potassium channel toxin ShK ([pTyrD][AEEA]) | Dissociation constant |
39 nM
|
[5] |
| Toxin Info Potassium channel toxin Bgk (Q24A) | Dissociation constant |
44 nM
|
[7] |
| Toxin Info Potassium channel toxin Bgk (W5A) | Dissociation constant |
61 nM
|
[7] |
| Toxin Info Potassium channel toxin Bgk (N19A) | Dissociation constant |
97 nM
|
[7] |
| Toxin Info Potassium channel toxin Bgk (H13A) | Dissociation constant |
109 nM
|
[7] |
| Toxin Info Potassium channel toxin Bgk (Y26A) | Dissociation constant |
210 nM
|
[7] |
| Toxin Info Potassium channel toxin Bgk (S23A) | Dissociation constant |
920 nM
|
[7] |
| Toxin Info Potassium channel toxin alpha-KTx 10.2 | Dissociation constant |
1 μM
|
[11] |
| Toxin Info Potassium channel toxin Bgk (K25A) | Dissociation constant |
5.497 μM
|
[7] |
| Toxin Info Toxin II.10.4 (T7P,D9Q) | Dissociation constant |
7.4 μM
|
[12] |
| Toxin Info Potassium channel toxin alpha-KTx 10.1 | Dissociation constant |
24.4 μM
|
[12] |
| Toxin Info MgTX (K28A) | Inhibition rate | . | [13] |
| Toxin Info Toxin MeKTx13-3 (D19K) | Inhibition rate | . | [14] |
| Toxin Info Toxin MeKTx13-3 (K6D,D19K) | Inhibition rate | . | [14] |
| Toxin Info Pi1 (K24A,Y33[pTyr]) | Inhibition rate | . | [15] |
| Toxin Info Pi1 (K24A,Y33A) | Inhibition rate | . | [15] |
| Toxin Info Anuroctoxin (F32T) | Inhibition rate | . | [16] |
| Toxin Info Anuroctoxin (N17A) | Inhibition rate | . | [16] |
| Toxin Info Anuroctoxin (N17A,F32T) | Inhibition rate | . | [16] |
| Toxin Info Neurotoxin HsTX1 (R14[Abu]) | Inhibition rate | . | [17] |
| Toxin Info ShKT domain-containing protein | Inhibition rate | . | [18], [19] |
| Toxin Info Jingzhaotoxin F7-15.33 | Inhibition rate | . | [20] |
| Toxin Info Potassium channel toxin alpha-KTx 2.1 | Inhibition rate | . | [3] |
| Toxin Info Potassium channel toxin alpha-KTx 23.2 | Inhibition rate | . | [21] |
| Toxin Info Potassium channel toxin alpha-KTx 4.6 | Inhibition rate | . | [22] |
| Toxin Info Potassium channel toxin alpha-KTx 6.12 | Inhibition rate | . | [23] |
| Toxin Info Scorpine-like peptide Ev37 | Inhibition rate | . | [24] |
| Toxin Info Mu-theraphotoxin-Pspp1 | Inhibition rate | . | [25] |
| Toxin Info Potassium channel toxin alpha-KTx 2.13 | Inhibition rate | . | [26] |
| Toxin Info Kunitz-type serine protease inhibitor Hg1 | Inhibition rate |
<50 %
|
[27], [28] |
| Toxin Info Beta-defensin 1 | Inhibition rate |
3 %
|
[29] |
| Toxin Info Beta-defensin 103 | Inhibition rate |
5 %
|
[30] |
| Toxin Info Kappa-theraphotoxin-Sc1a | Inhibition rate |
8 %
|
[31] |
| Toxin Info Potassium channel toxin ShK ([Pmp][AEEA],Q16K) | Inhibition rate |
10 %
|
[32] |
| Toxin Info Potassium channel toxin ShK ([Pmp][AEEA],Q16K,F27[Nle]) | Inhibition rate |
10 %
|
[32] |
| Toxin Info Kappa-theraphotoxin-Hm2a | Inhibition rate |
10 %
|
[31] |
| Toxin Info Delta-theraphotoxin-Hm1a | Inhibition rate |
12 %
|
[31- 35] |
| Toxin Info Fungal defensin plectasin | Inhibition rate |
16 %
|
[36] |
| Toxin Info Beta-defensin 3 | Inhibition rate |
19 %
|
[37] |
| Toxin Info Beta-defensin 104 | Inhibition rate |
19 %
|
[30] |
| Toxin Info Neurotoxin HsTX1 | Inhibition rate |
20 %
|
[17] |
| Toxin Info Potassium channel toxin alpha-KTx J123 | Inhibition rate |
20 %
|
[38] |
| Toxin Info Potassium channel toxin Sp4 | Inhibition rate |
20.85 %
|
[39] |
| Toxin Info Potassium channel toxin Sp4 | Inhibition rate |
21 %
|
[39] |
| Toxin Info Defensin BmKDfsin4 | Inhibition rate |
25 %
|
[40] |
| Toxin Info Potassium channel toxin KTx1 | Inhibition rate |
40 %
|
[41] |
| Toxin Info Potassium channel toxin KTx1 | Inhibition rate |
40 %
|
[41] |
| Toxin Info Kunitz-type serine protease inhibitor Hg1 | Inhibition rate |
45 %
|
[28] |
| Toxin Info Kunitz-type serine protease inhibitor homolog dendrotoxin K | Effective concentration 50 |
0.03 nM
|
[42] |
| Toxin Info Kunitz-type serine protease inhibitor homolog delta-dendrotoxin | Effective concentration 50 |
1.8 nM
|
[42] |
| Toxin Info Kunitz-type serine protease inhibitor homolog dendrotoxin I | Effective concentration 50 |
7.4 nM
|
[42] |
| Toxin Info Kunitz-type serine protease inhibitor homolog alpha-dendrotoxin | Effective concentration 50 |
9.4 nM
|
[42] |
| Toxin Info Kappa-stichotoxin-She3a | IC50 |
0.016 nM
|
[43] |
| Toxin Info ShK (Q16K)-Ala | IC50 |
0.0215 nM
|
[32] |
| Toxin Info Potassium channel toxin ShK (M21I) | IC50 |
0.14 nM
|
[32] |
| Toxin Info OsK1 (E15K,K19D) | IC50 |
0.19 nM
|
[44] |
| Toxin Info Potassium channel toxin ShK ([Pmp][AEEA]) | IC50 |
0.279 nM
|
[45] |
| Toxin Info OsK1 (E16K,K20D) | IC50 |
0.4 nM
|
[46] |
| Toxin Info Potassium channel toxin alpha-KTx 3.7 | IC50 |
0.6 nM
|
[46] |
| Toxin Info OsK1 (E16K) | IC50 |
0.63 nM
|
[46] |
| Toxin Info Toxin MeKTx13-3 (G11R,I28T,D33H) | IC50 |
0.65 nM
|
[47] |
| Toxin Info Defensin, beta 104 | IC50 |
0.83 nM
|
[48] |
| Toxin Info ShK-Lys | IC50 |
0.942 nM
|
[49] |
| Toxin Info MTX (N21Y,A22G,I25M,K27R,S28K,Y32N,G33R) | IC50 |
1 nM
|
[50] |
| Toxin Info PBTx3 (N24F) | IC50 |
1.327 nM
|
[48] |
| Toxin Info Potassium channel toxin ShK (K22[Dap]) | IC50 |
1.8 nM
|
[43] |
| Toxin Info Potassium channel toxin ShK ([pTyr][AEEA],M21[Nle]) | IC50 |
2.2 nM
|
[45] |
| Toxin Info OsK1 (K20D) | IC50 |
2.95 nM
|
[46] |
| Toxin Info Kunitz-type serine protease inhibitor homolog dendrotoxin I | IC50 |
3.1 nM
|
[51] |
| Toxin Info [P12,K16,D20]- OsK1 | IC50 |
3.18 nM
|
[46] |
| Toxin Info [pTyr][AEEA]RSCIDTIPKSRCTAFQCKHSMKYRLSFCRKTCGTC ([pTyr][AEEA]) | IC50 |
6.9 nM
|
[45] |
| Toxin Info Potassium channel toxin ShK ([pTyr][AEEA]) | IC50 |
7 nM
|
[45] |
| Toxin Info Potassium channel toxin alpha-KTx 6.3 | IC50 |
7 nM
|
[50] |
| Toxin Info Potassium channel toxin ShK ([Ppa][AEEA],M21[Nle]) | IC50 |
22 nM
|
[45] |
| Toxin Info OsK1 (E16K,K20D,T36Y) | IC50 |
34.4 nM
|
[46] |
| Toxin Info ScyTx (F2V,R6K,Q9E,D24V) | IC50 |
160 nM
|
[52] |
| Toxin Info OsK1 (E16A,K20D) | IC50 |
365 nM
|
[44] |
| Toxin Info Potassium channel toxin alpha-KTX 12 Sp2 | IC50 |
485 nM
|
[53] |
| Toxin Info Potassium channel toxin alpha-KTX 12 Sp2 | IC50 |
485 nM
|
[53] |
| Toxin Info Leiurotoxin I-like toxin P05 (R6K,Q9E,K20V,K25A,E27K) | IC50 |
26.6 μM
|
[52] |
References
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