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Target id: 540

Nomenclature: Kv1.3

Family: Voltage-gated potassium channels (Kv)

Gene and Protein Information Click here for help
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 0 575 1p13.3 KCNA3 potassium voltage-gated channel subfamily A member 3 3,22,27
Mouse 6 0 528 3 46.59 cM Kcna3 potassium voltage-gated channel, shaker-related subfamily, member 3 11
Rat 6 0 525 2q34 Kcna3 potassium voltage-gated channel subfamily A member 3 17,68
Previous and Unofficial Names Click here for help
HGK5 | HLK3 | hPCN3 | MBK3 | MK3 | RCK3 | potassium voltage-gated channel subfamily A member 3 | RGK5 | potassium channel, voltage gated shaker related subfamily A, member 3 | potassium voltage-gated channel
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Associated Proteins Click here for help
Heteromeric Pore-forming Subunits
Name References
Kv1.1 14,37
Kv1.2 14,37
Kv1.4 14,37
Kv1.5 75
Kv1.6 37
Auxiliary Subunits
Name References
Kvβ2 7,50
Other Associated Proteins
Name References
SAP97 7,31
β1 integrin 7,41
MMP23 59
Functional Characteristics Click here for help
Ion Selectivity and Conductance Click here for help
Species:  Human
Rank order:  K+ [18.0 - 9.0 (median: 13.0) pS] > Rb+ [10.0 pS] > NH4+ [1.3 pS] > Cs+ [0.26 pS]
References:  9
Species:  Human
Macroscopic current rectification:  Delayed Rectifier K+ current
References:  9
Voltage Dependence Click here for help
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -33.0 2.6 7 T cells Rat
Inactivation  - -
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -14.1 - 17 T cells Rat
Inactivation  -33.0 612.0 17
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -30.0 - 27-28 Xenopus laevis oocyte Mouse
Inactivation  - 55.0 – 250.0 27
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -25.0 - 67 L929 Rat
Inactivation  -44.0 - 67

Download all structure-activity data for this target as a CSV file go icon to follow link

Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference
Vm24 Peptide Primary target of this compound Immunopharmacology Ligand Hs - 11.5 – 12.3 pKd - - 29
pKd 12.3 (Kd 5x10-13 M) [29]
Description: Measured in a patch clamp assay using synthetically produced peptide.
pKd 11.5 (Kd 2.9x10-12 M) [29]
Description: Measured in a patch clamp assay using endogenous peptide.
noxiustoxin Peptide Click here for species-specific activity table Mm - 9.0 pKd - - 28
pKd 9.0 (Kd 1x10-9 M) [28]
charybdotoxin Peptide Click here for species-specific activity table Hs - 7.5 – 9.7 pKd - - 3,26,61
pKd 7.5 – 9.7 [3,26,61]
charybdotoxin Peptide Click here for species-specific activity table Rn - 8.6 pKd - - 28
pKd 8.6 [28]
correolide Small molecule or natural product Hs Pore blocker 8.0 pKd - - 20
pKd 8.0 [20]
tetraethylammonium Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm - 2.0 pKd - - 28
pKd 2.0 (Kd 1x10-2 M) [28]
5-(4-phenoxybutoxy)psoralen Small molecule or natural product Mm - 8.7 pEC50 - - 64
pEC50 8.7 [64]
OSK1-K16-D20 Peptide Mm - 11.5 pIC50 - - 53
pIC50 11.5 [53]
ShK Toxin Peptide Click here for species-specific activity table Rn - 9.9 – 12.0 pIC50 - - 35,52,57
pIC50 9.9 – 12.0 [35,52,57]
HsTX1[R14A] Peptide Primary target of this compound Immunopharmacology Ligand Hs - 10.6 pIC50 - - 70
pIC50 10.6 (IC50 2.7x10-11 M) [70]
ShK(L5) Peptide Rn - 10.2 – 10.9 pIC50 - - 5
pIC50 10.2 – 10.9 [5]
margatoxin Peptide Click here for species-specific activity table Hs - 10.0 – 10.3 pIC50 - - 24,26
pIC50 10.0 – 10.3 (IC50 1x10-10 – 5x10-11 M) [24,26]
kaliotoxin Peptide Rn - 9.2 pIC50 - - 28
pIC50 9.2 [28]
correolide Small molecule or natural product Hs - 7.1 pIC50 - - 20
pIC50 7.1 (IC50 8.6x10-8 M) [20]
maurotoxin Peptide N/A - 6.8 pIC50 - - 60
pIC50 6.8 [60]
psora-4 Small molecule or natural product Immunopharmacology Ligand Hs - 6.1 pIC50 - - 30
pIC50 6.1 (IC50 7.24x10-7 M) [30]
Description: Inhibition of human Kv1.3 expressed in CGE22 cells measured by patch clamp assay.
WP1066 Small molecule or natural product Click here for species-specific activity table Hs - 5.5 pIC50 - - 43
pIC50 5.5 (IC50 3.2x10-6 M) [43]
View species-specific channel blocker tables
Channel Blocker Comments
No differences in activity of blockers reported between mouse, rat and human Kv1.3.

Kv1.3 is blocked by a large number of other scorpion and sea anemone toxins including HsTX1 (12 ρM), OSK1 (14 ρM), Pi2 (50 ρM), ShK-Dap22 (23 - 110 ρM), agiotoxin-2 (200 ρM), and BgK (39 nM)- data in brackets are IC50 values. This is in addition to the classical K+ channel blockers such as 4-AP (195 μM), TEA (10 mM) and the small molecules Psora-4 (3 nM), PAC (149 nM), UK-78282 (200 nM), and verapamil (6 μM). For extensive reviews of these and other blockers, see [12].

PEG-HsTX1[R14A] blocks Kv1.3 with an IC50 of 36 nM which is a 1300-fold loss in affinity compared to the non-PEGylated peptide [70].
Immunopharmacology Comments
Kv1.3 is involved in T cell proliferation, activation and cytokine secretion, most significantly in effector memory T lymphocytes (TEM cells) compared to naive and central memory T cells. TEM cells are major drivers of inflammation in a number of autoimmune diseases, including multiple sclerosis and rheumatoid arthritis, so pharmacological manipulation of Kv1.3 activity may be of clinical utility in immunomodulation [1,7,12,26].
Cell Type Associations
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
Comment:  Kv1.3 plays a role in macrophage function vis-a-vis proliferation and iNOS expression.
References:  21,72
Immuno Cell Type:  Dendritic cells
Cell Ontology Term:   dendritic cell (CL:0000451)
Comment:  Kv1.3 plays a role in DC function vis-a-vis expression of costimulatory molecules and cytokines, and chemotaxis.
References:  21,72
Immuno Cell Type:  T cells
Comment:  Kv1.3 blockade causes inhibition of T cell proliferation and cytokine secretion, particularly in CCR7-effector memory T cells.
References:  21,72
Tissue Distribution Click here for help
T- and B- lymphocytes, alveolar macrophages, monocyte derived macrophages, prostate epithelium, platelets, cerebral cortical grey matter
Species:  Human
Technique:  Immunohistochemistry, RT-PCR, Electrophysiology, RNA : GNF / SymAtlas
References:  7,14-15,45,47-48,54,77
Olfactory bulb, peritoneal and bone marrow derived macrophages, osteoclasts
Species:  Mouse
Technique:  Northern Blot, Immunohistochemistry, Electrophysiology
References:  2,19,74,79
Brain synaptic membranes, olfactory bulb, hippocampal microglia, cultured microglia, osteoclasts, cultured oligodendrocyte progenitor cells, platelets, choroid plexus, testis
Species:  Rat
Technique:  Immunohistochemistry, Northern Blot, RT-PCR, Electrophysiology
References:  2,13,18,23,33-34,36,40,48,65
Tissue Distribution Comments
Two mouse knock-out studies report effects on adipocytes [44,78].
Functional Assays Click here for help
Kv1.3 clone expressed in L929 cells
Species:  Mouse
Tissue:  L929 cells
Response measured:  K+ current by patch clamp
References:  5,28,53,64
Kv1.3 clone expression
Species:  Human
Tissue:  CHO or HEK293 cells
Response measured:  K+ current by patch clamp
References:  33,52
Patch clamp of T-lymphocytes
Species:  Rat
Tissue:  Isolated T-cells
Response measured:  K+ current by patch clamp
References:  6
Patch clamp of T-lymphocytes
Species:  Human
Tissue:  Isolated T-cells
Response measured:  K+ current by patch clamp
References:  3,7,9,15,22,41,76
Kv1.3 clone expression
Species:  Rat
Tissue:  Xenopus laevis Oocytes
Response measured:  K+ current by patch clamp
References:  17,35,68
125I-charybdotoxin or 125I-HgTX1 (A19Y / Y37F) binding assay
Species:  Human
Tissue:  T-lymphocytes
Response measured:  Displacement of 125I-charybdotoxin or 125I-HgTX1 (A19Y / Y37F)
References:  51,55,62
[3H] Dihydrocorreolide or [(3H)]-trans-NPCO-DSC binding assay in HEK293 cells expressing Kv1.3
Species:  Rat
Tissue:  HEK293 cells
Response measured:  Binding or Displacement
References:  32,63
86 Rb+ flux in CHO cells expressing Kv1.3 / T-lymphocytes
Species:  Human
Tissue:  CHO cells / T-lymphocytes
Response measured:  Rb+ efflux following depolarisation with high K+
References:  33
Patch clamp of T-lymphocytes
Species:  Mouse
Tissue:  Isolated T-cells
Response measured:  K+ current by patch clamp
References:  42,46,65
Physiological Functions Click here for help
Homomeric Kv1.3 channels in the olfactory bulb neurons carry 60 - 80% of the Kv current in these cells which shows an involvement in signal transduction. Kv1.3 -/- mice have a "Super Smeller" phenotype with a lower threshold for smell detection.
Species:  Mouse
Tissue:  Olfactory neurons, olfactory cortex
References:  8,19
Kv1.3 is involved in rat oligodendrocyte progenitor proliferation and G1/S phase progression.
Species:  Rat
Tissue:  Oligodendrocyte progenitor cells
References:  2,13
Kv1.3 is involved in proliferation, oxidative burst and microglia mediated neuronal killing
Species:  Rat
Tissue:  Cultured rat microglia
References:  23,36,40
Kv1.3 is involved in T-lymphocyte volume regulation and possibly apoptosis.
Species:  Human
Tissue:  Jurkat T-lymphocytes
References:  66,69
Kv1.3 is involved in T-lymphocyte volume regulation and possibly apoptosis.
Species:  Mouse
Tissue:  T-lymphocytes (CTLL-2)
References:  16
Kv1.3 is a voltage gated potassium channel in human T-lymphocytes, and regulates membrane potential and calcium signalling. Kv1.3 blockade results in inhibition of T-cell proliferation and cytokine secretion. It is more important in CCR7-effector memory T-cells than in naive and central memory T-cells.
Species:  Human
Tissue:  T-lymphocytes
References:  7,10,12,15,26,49,76
Kv1.3 is involved in the translocation of the glucose transporter, GLUT4, to the plasma membrane in adipocytes (based on biophysical properties of current, probably heteromultimer of various Kv1 channels and not a homomultimer of Kv1.3). This suggests that it is important in insulin sensitivity.
Species:  Mouse
Tissue:  Mouse adipocytes
References:  8,44,78
In macrophages, Kv1.3 is probably found as a heteromultimer with Kv1.5.
Kv1.3 blockers suppress proliferation of mouse bone marrow derived macrophages.
Species:  Mouse
Tissue:  Macrophages
References:  74-75
Kv1.3 homomeric channels are found in calyx of Held nerve terminals
Species:  Mouse
Tissue:  MNTB neurons
References:  25
Kv1.3 homomeric channels are found in calyx of Held nerve terminals
Species:  Mouse
Tissue:  MNTB neurons
References:  25
Physiological Functions Comments
Studies have also been carried out in macaque monkeys [58] and swine [39].
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0002078 abnormal glucose homeostasis PMID: 14981264 
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0004130 abnormal muscle cell glucose uptake PMID: 12588802 
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0001262 decreased body weight PMID: 12588802 
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0002727 decreased circulating insulin level PMID: 14981264 
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0008965 increased basal metabolism PMID: 12588802 
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0002891 increased insulin sensitivity PMID: 14981264 
Kcna3tm1Gvd Kcna3tm1Gvd/Kcna3tm1Gvd
involves: 129S1/Sv * C57BL/6
MGI:96660  MP:0005659 increased resistance to diet-induced obesity PMID: 12588802 
Kcna3tm1Lys Kcna3tm1Lys/Kcna3tm1Lys
involves: 129/Sv * C57BL/6
MGI:96660  MP:0002169 no abnormal phenotype detected PMID: 12878608 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Autoimmune disease
Synonyms: hypersensitivity reaction disease [Disease Ontology: DOID:0060056]
Disease Ontology: DOID:0060056
OMIM: 109100, 126200, 177900, 222100, 604302
Side effects:  Inhibition of effector memory T-cells could potentially lead to reactivation of viral infections such as CMV.
Therapeutic use:  ShK derivative and PAP-1 are in clinical development
References:  4,6-7,39,73,76
Gene Expression and Pathophysiology Click here for help
Kv1.3 expression is increased in activated effector memory T-cells and class-switched CD27+ memory B-cells. Naive and memory T-cells and IgD+ B-cells in contrast, up-regulate KCa3.1 following activation.
Tissue or cell type:  T-Lymphocytes
Pathophysiology:  Up-regulation of Kv1.3 has no real pathophysiological effect, but allows to selectively target effector memory T-cells.
Species:  Human
References:  7,76-77
SNPs associated with autoimmune pancreatitis
Tissue or cell type:  T-Lymphocytes
Pathophysiology:  Susceptibility to autoimmune pancreatitis
Species:  Human
References:  56
Gene Expression and Pathophysiology Comments
Kv1.3 -/- mouse has no immune phenotype [38].
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  SNP associated with impaired glucose tolerance and lower insulin sensitivity.
Nucleotide change:  1645T>C
Amino acids:  1
SNP accession: 
References:  71
Biologically Significant Variant Comments
A total of 99 SNPs have been identified in human KCNA3. For more information see the entry on GeneCards.
General Comments
Kv1.3 can coassemble with other members of the Kv1 family, in heteromultimers. It cannot, however, co-assemble with members of other Kv families.
Like other members of the family, it has an intronless coding region.


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