• Kir3.1

    Blocking activities of compounds on Kir3.1/Kir3.4 on the Patchliner

    Vasas et al. (2016)

Kir3.1 | Potassium Voltage-Gated Channel Subfamily J Member 3

Family:
Inward-rectifier potassium ion channel

Subgroups:
Seven families channels demonstrate robust inward rectification: Kir1.1; Kir2.1 - Kir2.4; Kir3.1 - Kir3.4, Kir4.1 - Kir4.2; Kir5.1, Kir6.1 - Kir6.2; Kir7.1

Topology:
The channel protein contains two membrane spanning alpha helices denoted as M1 and M2. Four identical subunits form a functional homotetramer, heterotetramers can combine with members of the same subfamily

Kir3.1 Background Information

Kir3.1, also colled GIRK1, is a inward rectifier potassium channel which is a mamber of the subfamily of G protein-coupled inwardly-rectifying potassium channels (GIRKs). In the heart, it forms heteromers with Kir3.4 (GIRK4). When activated by parasympathetic signals such as acetylcholine through M2 muscarinic receptors, it causes an outward current of potassium, which slows down the heart rate. Kir3.1 and Kir3.4 are as well called muscarinic potassium channels and mediate the current IKAChthe heart.

Gene:
KCNJ3

Human Protein:
UniProt P48549

Tissue:
Heart, brain, prostate

Function/ Application:
ACh-activated K+ current in the heart (IKACh)

Pathology:
QT syndrome type 13, hyperaldosteronism type 3, adenocarcinomas, diabetes mellitus, Andersen Syndrome, Leber Congenital Amaurosis 16drome, ataxia, Parkinson's disease

Interaction:
Associates with Kir3.2 (GIRK2), Kir3.3 (GIRK3), Kir3.4 (GIRK4) to form a G-protein activated heteromultimer pore-forming unit. It is not functional as homomer. It interacts with PRKACG, GNAI3, GNB3, GNB1, Adrenoceptor beta 2

Modulator:
Tertiapin-Q, Glyburide, Halothane, Flupirtine

Assays:
Patch clamp

Recommended Reviews:
Kubo et al. (2005) International Union of Pharmacology. LIV. Nomenclature and Molecular Relationships of Inwardly Rectifying Potassium Channels. Pharmacol Rev 57(4):509-526

Posters

Publications

2016 - Myrsinane, Premyrsinane, and Cyclomyrsinane Diterpenes fromEuphorbia falcata as Potassium Ion Channel Inhibitors with Selective G Protein-Activated Inwardly Rectifying Ion Channel (GIRK) Blocking Effects

icon pl  Patchliner publication in Journal of Natural Products (2016)

Authors: 
Vasas A., Forgo P., Orvos P., Tálosi L., Csorba A., Pinke G., Hohmann J.

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