K<SUB>v</SUB>11.3 | Voltage-gated potassium channels | IUPHAR/BPS Guide to PHARMACOLOGY

Kv11.3

Target id: 574

Nomenclature: Kv11.3

Family: Voltage-gated potassium channels

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Kv11.3 in GtoImmuPdb

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 1 1196 2q24.2 KCNH7 potassium voltage-gated channel subfamily H member 7
Mouse 6 1 1195 2 C1.3 Kcnh7 potassium voltage-gated channel, subfamily H (eag-related), member 7
Rat 6 1 1195 3q21 Kcnh7 potassium voltage-gated channel subfamily H member 7
Previous and Unofficial Names
erg3 | HERG3 | eag-related protein 3 | ether-a-go-go-related gene potassium channel 3 | potassium voltage-gated channel, subfamily H (eag-related), member 7 | potassium channel, voltage gated eag related subfamily H, member 7 | potassium voltage-gated channel
Database Links
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Ion Selectivity and Conductance
Species:  Rat
Macroscopic current rectification:  Ik
References:  7,11
Voltage Dependence
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -44.0 20.0 7 Xenopus laevis oocyte Rat
Inactivation  - 10.0 7
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -42.0 17.0 9,11 CHO cells. Rat
Inactivation  - -
Deactivation  -44.0 7.0 – 22.0 6,9
Voltage Dependence Comments
Kv11.2 and Kv11.3 can form heteromultimers; for voltage dependence data see [11]
Associated subunits (Human)
minK (KCNE1)

Download all structure-activity data for this target as a CSV file

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Holding voltage (mV) Reference
NS1643 Rn - - - 1x10-5 - 1
Conc range: 1x10-5 M 10 µM NS1643 produced a -15 to -20mV shift in V0.5 of channel activation [1]
Activator Comments
10µM NS1643 produced a -15 to- 20mV shift in V0.5 of channel activation [1].
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Holding voltage (mV) Reference
ErgTx-1 Rn Pore blocker 8.4 pKd - - 10
pKd 8.4 [10]
BeKm-1 Rn Pore blocker 7.9 pKd - - 10
pKd 7.9 [10]
E4031 Rn - 6.7 pKd - - 7
pKd 6.7 [7]
Tissue Distribution
Spinal cord and dorsal root ganglia (DRG), largely within GABAergic neurons, widely expressed throughout adult mouse CNS
Species:  Mouse
Technique:  Immunocytochemistry, immunohistochemistry
References:  2-4
Broadly expressed throughout the nervous system (similar to erg1), sympathetic ganglia and low levels in retina
Species:  Rat
Technique:  In situ hybridisation
References:  7,12
All Kv11 transcripts are found in pancreatic islet cells and are under differential spatial and circadian regulation
Species:  Rat
Technique:  Immunohistochemistry
References:  5
Tissue Distribution Comments
Kv11.1, Kv11.2 and Kv11.3 channels are widely expressed throughout the nervous system [7,12]. All, with the exception of Kv11.1b isoform are transiently expressed in the developing spinal cord, largely within GABAergic neurons where they regulate nascent spinal motor rhythms [3]. All are expressed in adult brain in largely overlapping distributions and largely in neuron somata [4].
Physiological Functions
Kv11.3 regulates nascent spinal motor rhythms in developing mouse spinal cord
Species:  Mouse
Tissue:  Spinal cord
References:  3
Clinically-Relevant Mutations and Pathophysiology
Disease:  Major affective disorder 1; MAFD1
Synonyms: Bipolar affective disorder
Manic depressive-psychosis
OMIM: 125480
Role: 
References:  8
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human R394H 8
Biologically Significant Variants
Type:  Splice variant
Species:  Human
Description:  Kv11.3 isoform 2
Amino acids:  732
Nucleotide accession: 
Protein accession: 
Type:  Splice variant
Species:  Human
Description:  Kv11.3 isoform 1
Amino acids:  1196
Nucleotide accession: 
Protein accession: 

References

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1. Bilet A, Bauer CK. (2012) Effects of the small molecule HERG activator NS1643 on Kv11.3 channels. PLoS ONE, 7 (11): e50886. [PMID:23226420]

2. Furlan F, Guasti L, Avossa D, Becchetti A, Cilia E, Ballerini L, Arcangeli A. (2005) Interneurons transiently express the ERG K+ channels during development of mouse spinal networks in vitro. Neuroscience, 135 (4): 1179-92. [PMID:16165280]

3. Furlan F, Taccola G, Grandolfo M, Guasti L, Arcangeli A, Nistri A, Ballerini L. (2007) ERG conductance expression modulates the excitability of ventral horn GABAergic interneurons that control rhythmic oscillations in the developing mouse spinal cord. J. Neurosci., 27 (4): 919-28. [PMID:17251434]

4. Guasti L, Cilia E, Crociani O, Hofmann G, Polvani S, Becchetti A, Wanke E, Tempia F, Arcangeli A. (2005) Expression pattern of the ether-a-go-go-related (ERG) family proteins in the adult mouse central nervous system: evidence for coassembly of different subunits. J. Comp. Neurol., 491 (2): 157-74. [PMID:16127690]

5. Mühlbauer E, Bazwinsky I, Wolgast S, Klemenz A, Peschke E. (2007) Circadian changes of ether-a-go-go-related-gene (Erg) potassium channel transcripts in the rat pancreas and beta-cell. Cell. Mol. Life Sci., 64 (6): 768-80. [PMID:17322986]

6. Schledermann W, Wulfsen I, Schwarz JR, Bauer CK. (2001) Modulation of rat erg1, erg2, erg3 and HERG K+ currents by thyrotropin-releasing hormone in anterior pituitary cells via the native signal cascade. J. Physiol. (Lond.), 532 (Pt 1): 143-63. [PMID:11283231]

7. Shi W, Wymore RS, Wang HS, Pan Z, Cohen IS, McKinnon D, Dixon JE. (1997) Identification of two nervous system-specific members of the erg potassium channel gene family. J. Neurosci., 17 (24): 9423-32. [PMID:9390998]

8. Strauss KA, Markx S, Georgi B, Paul SM, Jinks RN, Hoshi T, McDonald A, First MB, Liu W, Benkert AR et al.. (2014) A population-based study of KCNH7 p.Arg394His and bipolar spectrum disorder. Hum. Mol. Genet., 23 (23): 6395-406. [PMID:24986916]

9. Sturm P, Wimmers S, Schwarz JR, Bauer CK. (2005) Extracellular potassium effects are conserved within the rat erg K+ channel family. J. Physiol. (Lond.), 564 (Pt 2): 329-45. [PMID:15705650]

10. Wanke E, Restano-Cassulini R. (2007) Toxins interacting with ether-à-go-go-related gene voltage-dependent potassium channels. Toxicon, 49 (2): 239-48. [PMID:17097705]

11. Wimmers S, Bauer CK, Schwarz JR. (2002) Biophysical properties of heteromultimeric erg K+ channels. Pflugers Arch., 445 (3): 423-30. [PMID:12466946]

12. Wymore RS, Gintant GA, Wymore RT, Dixon JE, McKinnon D, Cohen IS. (1997) Tissue and species distribution of mRNA for the IKr-like K+ channel, erg. Circ. Res., 80 (2): 261-8. [PMID:9012748]

Contributors

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How to cite this page

Michael C. Sanguinetti, K. George Chandy, Stephan Grissmer, George A. Gutman, Michel Lazdunski, David Mckinnon, Luis A. Pardo, Gail A. Robertson, Bernardo Rudy, Walter Stühmer, Xiaoliang Wang.
Voltage-gated potassium channels: Kv11.3. Last modified on 17/02/2015. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=574.