K<SUB>v</SUB>11.2 | Voltage-gated potassium channels | IUPHAR/BPS Guide to PHARMACOLOGY

Kv11.2

Target id: 573

Nomenclature: Kv11.2

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 Kv11.2 in GtoImmuPdb

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 1 994 17q23.3 KCNH6 potassium voltage-gated channel subfamily H member 6
Mouse 6 1 950 11 E1 Kcnh6 potassium voltage-gated channel, subfamily H (eag-related), member 6
Rat 6 1 950 10q32.1 Kcnh6 potassium voltage-gated channel subfamily H member 6
Previous and Unofficial Names
erg2 | HERG2 | eag-related protein 2 | ether-a-go-go-related gene potassium channel 2 | ether-a-go-go-related protein 2 | potassium voltage-gated channel, subfamily H (eag-related), member 6 | potassium channel, voltage gated eag related subfamily H, member 6 | 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:  9,11
Voltage Dependence
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -3.5 4.0 9 Xenopus laevis oocyte Rat
Inactivation  - 100.0 9
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  -14.5 7.3 7 CHO cells Human
Inactivation  -85.2 - 7
  V0.5 (mV)  τ (msec)  Reference  Cell type  Species 
Activation  - 428.0 11 CHO cells. Rat
Inactivation  - -
Comments  Data for heteromultimers of Kv11.2 and Kv11.3 [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 Hs - 4.9 pEC50 - - 1
pEC50 4.9 [1]
Activator Comments
NS1643: Negative shift of activation curve, slows inactivation. These effects are distinct from those of the same compound on Kv11.1 [1]
Gating inhibitors
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Holding voltage (mV) Reference
γ-KTx1.7 Hs - 8.8 pKd - - 8
pKd 8.8 [8]
ErgTx-1 Rn - 8.5 pKd - - 9
pKd 8.5 [9]
BeKm-1 Rn - 8.1 pKd - - 9
pKd 8.1 [9]
ErgTx-1 Hs Inhibition 6.7 pKd - - 6
pKd 6.7 [6]
View species-specific gating inhibitor tables
Gating Inhibitor Comments
For a review of toxin sensitivity among Kv11 channels, see [10]
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
E4031 Rn - 6.9 pKd - - 9
pKd 6.9 [9]
Tissue Distribution
Transiently expressed in the developing embryonic spinal cord, largely within GABAergic neurons
Species:  Mouse
Technique:  Immunocytochemistry, immunofluorescence
References:  2
Pancreatic islet cells
Species:  Rat
Technique:  quantitative RT-PCR, immunocytochemistry, electrophysiology
References:  5
The celiac ganglia (CG), the superior mesenteric ganglia (SMG), retina
Species:  Rat
Technique:  In situ hybridisation
References:  9
Tissue Distribution Comments
Kv11.1, Kv11.2 and Kv11.3 are broadly expressed in the nervous system [9,12]. In the developing embryonic spinal cord, they regulate nascent spinal motor rhythms [3]. All are expressed in the adult brain in largely overlapping distributions and largely in neuron somata [4].
Physiological Functions
Kv11.2 (and Kv11.3) regulate nascent spinal motor rhythms in developing mouse spinal cord
Species:  Mouse
Tissue:  Organotypic slice cultures of spinal cord and dorsal root ganglia (DRG)
References:  3
All Kv11 transcripts are found in pancreatic islet cells and are under differential spatial and circadian regulation
Species:  Rat
Tissue:  Pancreatic Islet cells
References:  5
Biologically Significant Variants
Type:  Splice variant
Species:  Human
Description:  Kv11.2 isoform 2
Amino acids:  905
Nucleotide accession: 
Protein accession: 
Type:  Splice variant
Species:  Human
Description:  Kv11.2 isoform 1
Amino acids:  994
Nucleotide accession: 
Protein accession: 

References

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1. Elmedyb P, Olesen SP, Grunnet M. (2007) Activation of ERG2 potassium channels by the diphenylurea NS1643. Neuropharmacology, 53 (2): 283-94. [PMID:17610913]

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. Müller R, Thiele J, Klages U, Lingens F. (1984) Incorporation of [18O]water into 4-hydroxybenzoic acid in the reaction of 4-chlorobenzoate dehalogenase from pseudomonas spec. CBS 3. Biochem. Biophys. Res. Commun., 124 (1): 178-82. [PMID:6497878]

7. Restano-Cassulini R, Korolkova YV, Diochot S, Gurrola G, Guasti L, Possani LD, Lazdunski M, Grishin EV, Arcangeli A, Wanke E. (2006) Species diversity and peptide toxins blocking selectivity of ether-a-go-go-related gene subfamily K+ channels in the central nervous system. Mol. Pharmacol., 69 (5): 1673-83. [PMID:16497878]

8. Restano-Cassulini R, Olamendi-Portugal T, Zamudio F, Becerril B, Possani LD. (2008) Two novel ergtoxins, blockers of K+-channels, purified from the Mexican scorpion Centruroides elegans elegans. Neurochem. Res., 33 (8): 1525-33. [PMID:18338253]

9. 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]

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: Kv11.2. Last modified on 07/10/2014. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=573.