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Gene and Protein Information | |||||||
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 |
Database Links | |
Alphafold | P22001 (Hs), P16390 (Mm), P15384 (Rn) |
ChEMBL Target | CHEMBL4633 (Hs), CHEMBL4818 (Mm), CHEMBL4248 (Rn) |
DrugBank Target | P22001 (Hs) |
Ensembl Gene | ENSG00000177272 (Hs), ENSMUSG00000047959 (Mm), ENSRNOG00000062002 (Rn) |
Entrez Gene | 3738 (Hs), 16491 (Mm), 29731 (Rn) |
Human Protein Atlas | ENSG00000177272 (Hs) |
KEGG Gene | hsa:3738 (Hs), mmu:16491 (Mm), rno:29731 (Rn) |
OMIM | 176263 (Hs) |
Pharos | P22001 (Hs) |
RefSeq Nucleotide | NM_002232 (Hs), NM_008418 (Mm), NM_019270 (Rn) |
RefSeq Protein | NP_002223 (Hs), NP_032444 (Mm), NP_062143 (Rn) |
UniProtKB | P22001 (Hs), P16390 (Mm), P15384 (Rn) |
Wikipedia | KCNA3 (Hs) |
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Functional Characteristics | |
KV |
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Download all structure-activity data for this target as a CSV file
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Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific channel blocker tables | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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]. |
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Two mouse knock-out studies report effects on adipocytes [44,78]. |
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Physiological Functions Comments | ||||||||
Studies have also been carried out in macaque monkeys [58] and swine [39]. |
Phenotypes, Alleles and Disease Models | Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Gene Expression and Pathophysiology Comments | ||||||||||||
Kv1.3 -/- mouse has no immune phenotype [38]. |
Biologically Significant Variants | ||||||||||||||
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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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