- Home
- Targets
- Ion channels
- Voltage-gated ion channels
- Potassium channels
- Inwardly rectifying potassium channels (KIR)
Inwardly rectifying potassium channels (KIR) C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Overview
Show »« Hide
More detailed introduction 
The 2TM domain family of K channels are also known as the inward-rectifier K channel family. This family includes the strong inward-rectifier K channels (Kir2.x) that are constitutively active, the G-protein-activated inward-rectifier K channels (Kir3.x) and the ATP-sensitive K channels (Kir6.x, which combine with sulphonylurea receptors (SUR1-3)). The pore-forming α subunits form tetramers, and heteromeric channels may be formed within subfamilies (e.g. Kir3.2 with Kir3.3).
Channels and Subunits
Targets of relevance to immunopharmacology are highlighted in blue
|
Kir1.1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir2.1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir2.2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir2.3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir2.4 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir3.1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir3.2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir3.3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir3.4 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir4.1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir4.2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir5.1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir6.1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir6.2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||||||||||||
|
Kir7.1 C
Show summary »« Hide summary
More detailed page
|
References
1. Abrams CJ, Davies NW, Shelton PA, Stanfield PR. (1996) The role of a single aspartate residue in ionic selectivity and block of a murine inward rectifier K+ channel Kir2.1. J Physiol (Lond.), 493 ( Pt 3): 643-9. [PMID:8799888]
2. Alagem N, Dvir M, Reuveny E. (2001) Mechanism of Ba(2+) block of a mouse inwardly rectifying K+ channel: differential contribution by two discrete residues. J Physiol (Lond.), 534 (Pt. 2): 381-93. [PMID:11454958]
3. Baukrowitz T, Schulte U, Oliver D, Herlitze S, Krauter T, Tucker SJ, Ruppersberg JP, Fakler B. (1998) PIP2 and PIP as determinants for ATP inhibition of KATP channels. Science, 282 (5391): 1141-4. [PMID:9804555]
4. Choe H, Sackin H, Palmer LG. (2000) Permeation properties of inward-rectifier potassium channels and their molecular determinants. J Gen Physiol, 115 (4): 391-404. [PMID:10736307]
5. Dascal N, Schreibmayer W, Lim NF, Wang W, Chavkin C, DiMagno L, Labarca C, Kieffer BL, Gaveriaux-Ruff C, Trollinger D et al.. (1993) Atrial G protein-activated K+ channel: expression cloning and molecular properties. Proc Natl Acad Sci USA, 90 (21): 10235-9. [PMID:8234283]
6. Döring F, Derst C, Wischmeyer E, Karschin C, Schneggenburger R, Daut J, Karschin A. (1998) The epithelial inward rectifier channel Kir7.1 displays unusual K+ permeation properties. J Neurosci, 18 (21): 8625-36. [PMID:9786970]
7. Hilgemann DW, Ball R. (1996) Regulation of cardiac Na+,Ca2+ exchange and KATP potassium channels by PIP2. Science, 273 (5277): 956-9. [PMID:8688080]
8. Ho K, Nichols CG, Lederer WJ, Lytton J, Vassilev PM, Kanazirska MV, Hebert SC. (1993) Cloning and expression of an inwardly rectifying ATP-regulated potassium channel. Nature, 362 (6415): 31-8. [PMID:7680431]
9. Huang CL, Feng S, Hilgemann DW. (1998) Direct activation of inward rectifier potassium channels by PIP2 and its stabilization by Gbetagamma. Nature, 391 (6669): 803-6. [PMID:9486652]
10. Hughes BA, Kumar G, Yuan Y, Swaminathan A, Yan D, Sharma A, Plumley L, Yang-Feng TL, Swaroop A. (2000) Cloning and functional expression of human retinal kir2.4, a pH-sensitive inwardly rectifying K(+) channel. Am J Physiol, Cell Physiol, 279 (3): C771-84. [PMID:10942728]
11. Inagaki N, Gonoi T, Clement 4th JP, Namba N, Inazawa J, Gonzalez G, Aguilar-Bryan L, Seino S, Bryan J. (1995) Reconstitution of IKATP: an inward rectifier subunit plus the sulfonylurea receptor. Science, 270 (5239): 1166-70. [PMID:7502040]
12. Inagaki N, Gonoi T, Clement JP, Wang CZ, Aguilar-Bryan L, Bryan J, Seino S. (1996) A family of sulfonylurea receptors determines the pharmacological properties of ATP-sensitive K+ channels. Neuron, 16 (5): 1011-7. [PMID:8630239]
13. Ishihara K, Hiraoka M, Ochi R. (1996) The tetravalent organic cation spermine causes the gating of the IRK1 channel expressed in murine fibroblast cells. J Physiol (Lond.), 491 ( Pt 2): 367-81. [PMID:8866861]
14. Jin W, Klem AM, Lewis JH, Lu Z. (1999) Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry, 38 (43): 14294-301. [PMID:10572004]
15. Jin W, Lu Z. (1999) Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry, 38 (43): 14286-93. [PMID:10572003]
16. Kobayashi T, Ikeda K, Kumanishi T. (2000) Inhibition by various antipsychotic drugs of the G-protein-activated inwardly rectifying K(+) (GIRK) channels expressed in xenopus oocytes. Br J Pharmacol, 129 (8): 1716-22. [PMID:10780978]
17. Kobayashi T, Washiyama K, Ikeda K. (2004) Inhibition of G protein-activated inwardly rectifying K+ channels by various antidepressant drugs. Neuropsychopharmacology, 29 (10): 1841-51. [PMID:15150531]
18. Konstas AA, Korbmacher C, Tucker SJ. (2003) Identification of domains that control the heteromeric assembly of Kir5.1/Kir4.0 potassium channels. Am J Physiol, Cell Physiol, 284 (4): C910-7. [PMID:12456399]
19. Krapivinsky G, Medina I, Eng L, Krapivinsky L, Yang Y, Clapham DE. (1998) A novel inward rectifier K+ channel with unique pore properties. Neuron, 20 (5): 995-1005. [PMID:9620703]
20. Kusaka S, Inanobe A, Fujita A, Makino Y, Tanemoto M, Matsushita K, Tano Y, Kurachi Y. (2001) Functional Kir7.1 channels localized at the root of apical processes in rat retinal pigment epithelium. J Physiol (Lond.), 531 (Pt 1): 27-36. [PMID:11179389]
21. Lopatin AN, Makhina EN, Nichols CG. (1994) Potassium channel block by cytoplasmic polyamines as the mechanism of intrinsic rectification. Nature, 372 (6504): 366-9. [PMID:7969496]
22. Makhina EN, Kelly AJ, Lopatin AN, Mercer RW, Nichols CG. (1994) Cloning and expression of a novel human brain inward rectifier potassium channel. J Biol Chem, 269 (32): 20468-74. [PMID:8051145]
23. Partiseti M, Collura V, Agnel M, Culouscou JM, Graham D. (1998) Cloning and characterization of a novel human inwardly rectifying potassium channel predominantly expressed in small intestine. FEBS Lett, 434 (1-2): 171-6. [PMID:9738472]
24. Pearson WL, Dourado M, Schreiber M, Salkoff L, Nichols CG. (1999) Expression of a functional Kir4 family inward rectifier K+ channel from a gene cloned from mouse liver. J Physiol (Lond.), 514 ( Pt 3): 639-53. [PMID:9882736]
25. Preisig-Müller R, Schlichthörl G, Goerge T, Heinen S, Brüggemann A, Rajan S, Derst C, Veh RW, Daut J. (2002) Heteromerization of Kir2.x potassium channels contributes to the phenotype of Andersen's syndrome. Proc Natl Acad Sci USA, 99 (11): 7774-9. [PMID:12032359]
26. Rapedius M, Soom M, Shumilina E, Schulze D, Schönherr R, Kirsch C, Lang F, Tucker SJ, Baukrowitz T. (2005) Long chain CoA esters as competitive antagonists of phosphatidylinositol 4,5-bisphosphate activation in Kir channels. J Biol Chem, 280 (35): 30760-7. [PMID:15980413]
27. Soom M, Schönherr R, Kubo Y, Kirsch C, Klinger R, Heinemann SH. (2001) Multiple PIP2 binding sites in Kir2.1 inwardly rectifying potassium channels. FEBS Lett, 490 (1-2): 49-53. [PMID:11172809]
28. Takahashi N, Morishige K, Jahangir A, Yamada M, Findlay I, Koyama H, Kurachi Y. (1994) Molecular cloning and functional expression of cDNA encoding a second class of inward rectifier potassium channels in the mouse brain. J Biol Chem, 269 (37): 23274-9. [PMID:8083233]
29. Takumi T, Ishii T, Horio Y, Morishige K, Takahashi N, Yamada M, Yamashita T, Kiyama H, Sohmiya K, Nakanishi S et al.. (1995) A novel ATP-dependent inward rectifier potassium channel expressed predominantly in glial cells. J Biol Chem, 270 (27): 16339-46. [PMID:7608203]
30. Tanemoto M, Fujita A, Higashi K, Kurachi Y. (2002) PSD-95 mediates formation of a functional homomeric Kir5.1 channel in the brain. Neuron, 34 (3): 387-97. [PMID:11988170]
31. Tanemoto M, Kittaka N, Inanobe A, Kurachi Y. (2000) In vivo formation of a proton-sensitive K+ channel by heteromeric subunit assembly of Kir5.1 with Kir4.1. J Physiol (Lond.), 525 Pt 3: 587-92. [PMID:10856114]
32. Tang W, Yang XC. (1994) Cloning a novel human brain inward rectifier potassium channel and its functional expression in Xenopus oocytes. FEBS Lett, 348 (3): 239-43. [PMID:8034048]
33. Yamada M, Isomoto S, Matsumoto S, Kondo C, Shindo T, Horio Y, Kurachi Y. (1997) Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K+ channel. J Physiol (Lond.), 499 ( Pt 3): 715-20. [PMID:9130167]
34. Yamashita T, Horio Y, Yamada M, Takahashi N, Kondo C, Kurachi Y. (1996) Competition between Mg2+ and spermine for a cloned IRK2 channel expressed in a human cell line. J Physiol (Lond.), 493 ( Pt 1): 143-56. [PMID:8735700]
35. Yang J, Jan YN, Jan LY. (1995) Control of rectification and permeation by residues in two distinct domains in an inward rectifier K+ channel. Neuron, 14 (5): 1047-54. [PMID:7748552]
36. Zhou H, Chepilko S, Schütt W, Choe H, Palmer LG, Sackin H. (1996) Mutations in the pore region of ROMK enhance Ba2+ block. Am J Physiol, 271 (6 Pt 1): C1949-56. [PMID:8997197]
NC-IUPHAR subcommittee and family contributors
Subcommittee members:
Paul A. Slesinger (Chairperson)
Colin G. Nichols
Lawrence G. Palmer
Henry Sackin
Stephen Tucker |
Other contributors:
John P. Adelman
David E. Clapham
Hiroshi Hibino
Atsushi Inanobe
Lily Y. Jan
Andreas Karschin
Yoshihiro Kubo
Yoshihisa Kurachi
Michel Lazdunski
Takashi Miki
Wade L. Pearson
Susumu Seino
Carol A. Vandenberg |
How to cite this family page
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Mathie AA, Peters JA, Veale EL, Striessnig J, Kelly E, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Ion channels. Br J Pharmacol. 180 Suppl 2:S145-S222.
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License