Target Information
General Information of This Target
| Target ID |
BTDT00131
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|---|---|---|---|---|---|---|
| Target Name |
Potassium voltage-gated channel subfamily A member 1 (KCNA1)
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| Target Bioclass |
Transporter and channel
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| Uniprot ID | ||||||
| 3D Structure | ||||||
| Gene Name |
KCNA1
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| Gene ID | ||||||
| Synonym |
Voltage-gated K(+) channel HuKI; Voltage-gated potassium channel HBK1; Voltage-gated potassium channel subunit Kv1.1
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| Sequence |
MTVMSGENVDEASAAPGHPQDGSYPRQADHDDHECCERVVINISGLRFETQLKTLAQFPN
TLLGNPKKRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRLRRPVNVPLDMFSEEIKFY ELGEEAMEKFREDEGFIKEEERPLPEKEYQRQVWLLFEYPESSGPARVIAIVSVMVILIS IVIFCLETLPELKDDKDFTGTVHRIDNTTVIYNSNIFTDPFFIVETLCIIWFSFELVVRF FACPSKTDFFKNIMNFIDIVAIIPYFITLGTEIAEQEGNQKGEQATSLAILRVIRLVRVF RIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEAEEAESHFSSIP DAFWWAVVSMTTVGYGDMYPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETE GEEQAQLLHVSSPNLASDSDLSRRSSSTMSKSEYMEIEEDMNNSIAHYRQVNIRTANCTT ANQNCVNKSKLLTDV 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. Response to toxins that are selective for KCNA1, respectively for KCNA2, suggests that heteromeric potassium channels composed of both KCNA1 and KCNA2 play a role in pacemaking and regulate the output of deep cerebellar nuclear neurons. 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 | ||||||
| TCDB 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 U-AITX-Bg1c | . | . | [1] |
| Toxin Info Toxin APETx1 (P3T) | . | . | [2] |
| Toxin Info Toxin APETx1 (D42A) | . | . | [2] |
| Toxin Info Toxin APETx1 (F33A) | . | . | [2] |
| Toxin Info Toxin APETx1 (K18A) | . | . | [2] |
| Toxin Info Toxin APETx1 (L34A) | . | . | [2] |
| Toxin Info Toxin APETx1 (N23A) | . | . | [2] |
| Toxin Info Toxin APETx1 (R24A) | . | . | [2] |
| Toxin Info Toxin APETx1 (S22A) | . | . | [2] |
| Toxin Info Toxin APETx1 (S29A) | . | . | [2] |
| Toxin Info Toxin APETx1 (T19A) | . | . | [2] |
| Toxin Info Toxin APETx1 (T27A) | . | . | [2] |
| Toxin Info Toxin APETx1 (Y32A) | . | . | [2] |
| Toxin Info Toxin APETx1 (Y5A | . | . | [2] |
| Toxin Info Toxin APETx4 | . | . | [2] |
| Toxin Info Toxin APETx4 (K8A,A15F) | . | . | [2] |
| Toxin Info Toxin APETx2 | . | . | [1] |
| Toxin Info Toxin APETx2_A33F_L34A | . | . | [1] |
| Toxin Info Potassium channel toxin gamma-KTx 1.1 | Dissociation constant |
4.5 nM
|
[3] |
| Toxin Info BeKm1 (E9A) | Dissociation constant |
4.8 nM
|
[4] |
| Toxin Info BeKm1 (D34A) | Dissociation constant |
7.2 nM
|
[4] |
| Toxin Info BeKm1 (V29A) | Dissociation constant |
7.4 nM
|
[4] |
| Toxin Info Potassium channel toxin gamma-KTx 2.1 | Dissociation constant |
7.7 nM
|
[3] |
| Toxin Info BeKm1 (F32A) | Dissociation constant |
9.1 nM
|
[4] |
| Toxin Info BeKm1 (P2A) | Dissociation constant |
10.9 nM
|
[4] |
| Toxin Info Potassium channel toxin gamma-KTx 1.7 | Dissociation constant |
12.8 nM
|
[5] |
| Toxin Info CeErg4 | Dissociation constant |
14.2 nM
|
[6] |
| Toxin Info BeKm1 (Q12A) | Dissociation constant |
14.3 nM
|
[4] |
| Toxin Info BeKm1 (K6A) | Dissociation constant |
17.2 nM
|
[4] |
| Toxin Info BeKm1 (F36A) | Dissociation constant |
20.2 nM
|
[4] |
| Toxin Info BeKm1 (D4A) | Dissociation constant |
21.2 nM
|
[4] |
| Toxin Info BeKm1 (R1A) | Dissociation constant |
41.9 nM
|
[4] |
| Toxin Info BeKm1 (R27A) | Dissociation constant |
46.7 nM
|
[4] |
| Toxin Info BeKm1 (F14A) | Dissociation constant |
51.9 nM
|
[4] |
| Toxin Info ErgTx1 (Q18A,A35M) | Dissociation constant |
72.9 nM
|
[6] |
| Toxin Info BeKm1 (K23A) | Dissociation constant |
92.2 nM
|
[4] |
| Toxin Info BeKm1 (Y11A) | Dissociation constant |
92.4 nM
|
[4] |
| Toxin Info ErgTx1 | Dissociation constant |
303.4 nM
|
[7] |
| Toxin Info BeKm1 (F21A) | Dissociation constant |
328.6 nM
|
[4] |
| Toxin Info BeKm1 (R20A) | Dissociation constant |
444.8 nM
|
[4] |
| Toxin Info BeKm1 (K18A) | Dissociation constant |
544.3 nM
|
[4] |
| Toxin Info Potassium channel toxin alpha-KTx 15.2 | Dissociation constant |
1.9 μM
|
[8] |
| Toxin Info N.vectensis toxin 4 | Effect | . | [9] |
| Toxin Info N.vectensis toxin 5 | Effect | . | [9] |
| Toxin Info OsK1 (R12P,E16K,K20D) | Inhibition rate | . | [10] |
| Toxin Info OsK1 (E16K) | Inhibition rate | . | [10] |
| Toxin Info OsK1 (E16K) | Inhibition rate | . | [10] |
| Toxin Info Potassium channel toxin alpha-KTx 23.1 | Inhibition rate | . | [11] |
| Toxin Info Potassium channel toxin ShK ([Ppa][AEEA],M21[Nle]) | Inhibition rate | . | [12] |
| Toxin Info Potassium channel toxin ShK ([pTyr][AEEA]) | Inhibition rate | . | [13] |
| Toxin Info DiscrepinK6V) | Inhibition rate | . | [14] |
| Toxin Info Toxin MeKTx13-3 (D19K) | Inhibition rate | . | [15] |
| Toxin Info Toxin MeKTx13-3 (K6D,D19K) | Inhibition rate | . | [15] |
| Toxin Info OsK1 (E14A,K18D) | Inhibition rate | . | [16] |
| Toxin Info OsK1 (E15A,K19D) | Inhibition rate | . | [16] |
| Toxin Info Defensin domain protein | Inhibition rate | . | [17] |
| Toxin Info U-actitoxin-Oulsp2 | Inhibition rate | . | [18] |
| Toxin Info Defensin-like protein 1 | Inhibition rate | . | [19] |
| Toxin Info Crotamine | Inhibition rate | . | [20] |
| Toxin Info Kappa-actitoxin-Bcs3a | Inhibition rate | . | [21] |
| Toxin Info Kappa-actitoxin-Bcs3b | Inhibition rate | . | [21] |
| Toxin Info Kappa-conotoxin ViTx | Inhibition rate | . | [22], [23] |
| Toxin Info Mambaquaretin-1 | Inhibition rate | . | [24], [25], [26] |
| Toxin Info Potassium channel toxin alpha-KTx 1.11 | Inhibition rate | . | [27] |
| Toxin Info Potassium channel toxin alpha-KTx 1.15 | Inhibition rate | . | [28] |
| Toxin Info Potassium channel toxin alpha-KTx 1.16 | Inhibition rate | . | [29] |
| Toxin Info Potassium channel toxin alpha-KTx 1.17 | Inhibition rate | . | [29] |
| Toxin Info Potassium channel toxin alpha-KTx 15.6 | Inhibition rate | . | [14] |
| Toxin Info Potassium channel toxin alpha-KTx 2.14 | Inhibition rate | . | [30] |
| Toxin Info Potassium channel toxin alpha-KTx 3.13 | Inhibition rate | . | [31] |
| Toxin Info Potassium channel toxin alpha-KTx 19.1 | Inhibition rate | . | [32] |
| Toxin Info Potassium channel toxin alpha-KTx 4.1 | Inhibition rate | . | [14] |
| Toxin Info Potassium channel toxin alpha-KTx 4.6 | Inhibition rate | . | [33] |
| Toxin Info Potassium channel toxin alpha-KTx 8.2 | Inhibition rate | . | [34] |
| Toxin Info Potassium channel toxin alpha-KTx 8.6 | Inhibition rate | . | [34], [35] |
| Toxin Info Potassium channel toxin alpha-KTx 8.6 | Inhibition rate | . | [34] |
| Toxin Info Kappa-actitoxin-Bcs4a | Inhibition rate | . | [36] |
| Toxin Info Potassium channel toxin AbeTx1 | Inhibition rate | . | [37] |
| Toxin Info Potassium channel toxin AbeTx1 | Inhibition rate | . | [37] |
| Toxin Info Potassium channel toxin alpha-KTx 8.8 | Inhibition rate | . | [38] |
| Toxin Info Potassium channel toxin kappa-KTx 2.5 | Inhibition rate | . | [39] |
| Toxin Info U-actitoxin-Oulsp1 | Inhibition rate | . | [40] |
| Toxin Info Mu-scoloptoxin(15)-Ssm1a | Inhibition rate | . | [41] |
| Toxin Info Kappa-actitoxin-Ael2e | Inhibition rate | . | [42] |
| Toxin Info Potassium channel toxin alpha-KTx 32.1 | Inhibition rate | . | [43] |
| Toxin Info Apamin | Inhibition rate | . | [44- 61] |
| Toxin Info Potassium channel toxin alpha-KTx 20.1 | Inhibition rate | . | [62] |
| Toxin Info Potassium channel toxin alpha-KTx 3.11 | Inhibition rate | . | [63] |
| Toxin Info Mu-theraphotoxin-Pspp1 | Inhibition rate | . | [64] |
| Toxin Info Potassium channel toxin alpha-KTx 16.4 | Inhibition rate | . | [65] |
| Toxin Info Kappa-actitoxin-Ate1a | Inhibition rate | . | [66] |
| Toxin Info Toxin VmKTx1 | Inhibition rate | . | [67] |
| Toxin Info Potassium channel toxin alpha-KTx 1.10 | Inhibition rate | . | [14] |
| Toxin Info Potassium channel toxin alpha-KTx 6.13 | Inhibition rate | . | [14] |
| Toxin Info Potassium channel toxin alpha-KTx 2.13 | Inhibition rate | . | [68] |
| Toxin Info Potassium channel toxin alpha-KTx 21.1 | Inhibition rate | . | [69] |
| Toxin Info Potassium channel toxin alpha-KTx 3.6 | Inhibition rate | . | [31] |
| Toxin Info Potassium channel toxin ShK ([pTyr][AEEA]) | Inhibition rate | . | [12] |
| Toxin Info OsK1 (E16K,K20D) | Inhibition rate | . | [16] |
| Toxin Info KappaPI-actitoxin-Ael3a | Inhibition rate | . | [70], [71] |
| Toxin Info Toxin AmmTX3 (R18A) | Inhibition rate | . | [14] |
| Toxin Info Toxin AmmTX3 (R18A,A18R,K19A) | Inhibition rate | . | [14] |
| Toxin Info Discrepin (V6K,R19I,K20D,V21R | Inhibition rate | . | [14] |
| Toxin Info Potassium channel toxin alpha-KTx 3.7 | Inhibition rate | . | [10] |
| Toxin Info OsK1 (E16K,K20D) | Inhibition rate | . | [10] |
| Toxin Info [D20]- OsK1 | Inhibition rate | . | [10] |
| Toxin Info Fungal defensin plectasin | Inhibition rate |
4 %
|
[72] |
| Toxin Info Thrombin-like enzyme collinein-1 | Inhibition rate |
5 %
|
[73], [74], [75], [76] |
| Toxin Info Neutrophil defensin 1 | Inhibition rate |
6 %
|
[77] |
| Toxin Info Defensin BmKDfsin5 | Inhibition rate |
9 %
|
[78] |
| Toxin Info Mu-theraphotoxin-Cg2a 3 | Inhibition rate |
9 %
|
[79] |
| Toxin Info Defensin alpha 5 | Inhibition rate |
9 %
|
[77] |
| Toxin Info Potassium channel toxin alpha-KTx 12.2 | Inhibition rate |
11 %
|
[80] |
| Toxin Info Potassium channel toxin alpha-KTx 12.1 | Inhibition rate |
11 %
|
[80] |
| Toxin Info Beta/kappa-theraphotoxin-Cg1a | Inhibition rate |
11 %
|
[81- 85] |
| Toxin Info Defensin BmKDfsin4 | Inhibition rate |
12 %
|
[86] |
| Toxin Info Potassium channel toxin epsilon-KTx 1.1 | Inhibition rate |
12 %
|
[87] |
| Toxin Info Beta-defensin 1 | Inhibition rate |
13 %
|
[88] |
| Toxin Info BmK86-P1 | Inhibition rate |
13 %
|
[89] |
| Toxin Info Defensin domain protein | Inhibition rate |
15 %
|
[17] |
| Toxin Info U20-theraphotoxin-Cg1a 1 | Inhibition rate |
15 %
|
[79] |
| Toxin Info Discrepin (K20D,V21R | Inhibition rate |
18.5 %
|
[14] |
| Toxin Info Potassium channel toxin alpha-KTx Ctri9577 | Inhibition rate |
19 %
|
[90] |
| Toxin Info Discrepin (R19I,D20K) | Inhibition rate |
20.2 %
|
[14] |
| Toxin Info Potassium channel toxin epsilon-KTx 1.2 | Inhibition rate |
24 %
|
[87] |
| Toxin Info Potassium channel toxin alpha-KTx 15.1 | Inhibition rate |
25 %
|
[14] |
| Toxin Info Beta/kappa-theraphotoxin-Hlv1a | Inhibition rate |
25 %
|
[91] |
| Toxin Info Defensin BmKDfsin3 | Inhibition rate |
30 %
|
[78- 92] |
| Toxin Info Potassium channel toxin alpha-KTx 6.3 | Inhibition rate |
35 %
|
[14] |
| Toxin Info ProTx2 | Inhibition rate |
40 %
|
[91] |
| Toxin Info Pi-stichotoxin-Hcr5b | Inhibition rate |
52 %
|
[93] |
| Toxin Info Potassium channel toxin alpha-KTx 4.2 | Inhibition rate |
53 %
|
[14] |
| Toxin Info Potassium channel toxin alpha-KTx 1.6 | Inhibition rate |
60 %
|
[14] |
| Toxin Info Potassium channel toxin gamma-KTx 1.8 | Inhibition rate |
90 %
|
[5] |
| Toxin Info BeKm1 | IC50 |
0.014 nM
|
[94] |
| Toxin Info Potassium channel toxin gamma-KTx 1.10 | IC50 |
3.4 nM
|
[95] |
| Toxin Info Potassium channel toxin gamma-KTx 1.10 | IC50 |
3.4 nM
|
[95] |
| Toxin Info Potassium channel toxin gamma-KTx 2.2 | IC50 |
6.7 nM
|
[96] |
| Toxin Info Potassium channel toxin gamma-KTx 2.1 | IC50 |
7.7 nM
|
[97] |
| Toxin Info Potassium channel gamma toxin gamma-KTx 1.9 | IC50 |
16.9 nM
|
[98] |
| Toxin Info Potassium channel gamma toxin gamma-KTx 1.9 | IC50 |
16.9 nM
|
[98] |
| Toxin Info BeKm1 | IC50 |
27 nM
|
[94] |
| Toxin Info Kappa-actitoxin-Ael2a | IC50 |
34 nM
|
[3- 103] |
| Toxin Info BeKm1 | IC50 |
64.1 nM
|
[104] |
| Toxin Info BeKm1_R27K | IC50 |
80.5 nM
|
[104] |
| Toxin Info BeKm1 | IC50 |
88.6 nM
|
[104] |
| Toxin Info BeKm1 | IC50 |
280 nM
|
[104] |
| Toxin Info U21-theraphotoxin-Cg1b | IC50 |
612.6 nM
|
[79] |
| Toxin Info Delta-theraphotoxin-Cg1a 1 | IC50 |
626.9 nM
|
[83- 109] |
| Toxin Info U-Asilidin(12)-Dg3b | IC50 |
1 μM
|
[110], [111] |
| Toxin Info APETx2 | IC50 |
1.21 μM
|
[1- 119] |
| Toxin Info APETx2 | IC50 |
1.21 μM
|
[1- 119] |
| Toxin Info Toxin AmmTX3 (K6V) | IC50 |
3.2 μM
|
[14] |
| Toxin Info Discrepin (I19R,D20K,R21V) | IC50 |
3.5 μM
|
[14] |
| Toxin Info Beta/kappa-theraphotoxin-Gi1a | IC50 |
3.695 μM
|
[120] |
| Toxin Info Beta-theraphotoxin-Gr1a | IC50 |
4.2 μM
|
[121], [122], [123], [124] |
| Toxin Info Kappa-theraphotoxin-Gr2c | IC50 |
4.7 μM
|
[125], [122], [123], [124] |
| Toxin Info Beta-theraphotoxin-Gr1b | IC50 |
4.8 μM
|
[122], [123], [124] |
| Toxin Info Kappa-theraphotoxin-Gr3a | IC50 |
7.4 μM
|
[122- 130] |
| Toxin Info Potassium channel toxin alpha-KTx 15.3 | IC50 |
7.9 μM
|
[14] |
| Toxin Info Potassium channel toxin alpha-KTx 15.7 | IC50 |
7.9 μM
|
[14] |
| Toxin Info Mu/kappa-theraphotoxin-Ap1a | IC50 |
8.197 μM
|
[131] |
| Toxin Info Kappa-theraphotoxin-Aa1a | IC50 |
8.511 μM
|
[131] |
| Toxin Info M-theraphotoxin-Gr1a | IC50 |
11 μM
|
[122- 142] |
References
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