Kv2 Assays
Kv2 Channel Description
The potassium channel is widely distributed in all living cells (including animal cells, plant cells, and bacterial cells), impacting various physiological activities. Voltage-gated potassium (Kv) channel is one of the most important families of potassium channels that regulate cell membrane potential or voltage changes. Currently, 12 subfamilies (about 40 members) have been identified in the Kv channel family, in which the Kv2 channel is an important Kv channel playing an important action in delayed rectifier current.
Structure of Kv2 Channel
The Kv2 channel, also known as the Shab family, shares a high level of similarity to the Kv1 channel in structure. The Kv2 channel is a homotetramer made up of four identical α subunits. Each of the subunits consists of six membrane-spanning helices S1-S6, among which S1-S4 transmembrane helices form the voltage-sensing domain (VSD) and S5-S6 contribute to the potassium ion-conducting domain (namely pore domain). The S5 transmembrane helix and S6 transmembrane helix are connected by the P loop or P domain, which contains the 'K+ channel signature sequence' (TVGYG) and is essential to the selectivity of the channel.
Fig.1 Structure of Kv channels. (Grizel, 2014)
Kv2 Channel Members
There are two identified members of the Kv2 subfamily, potassium voltage-gated channel subfamily B member 1 (Kv2.1) and potassium voltage-gated channel subfamily B member 2 (Kv2.2), both of which are abundantly expressed in the mammalian central nervous system and play important roles in the regulations of potential duration and neuronal excitability.
| Subtype | Gene | Pathways | Function |
| Kv2.1 | KCNB1 |
|
Regulates action potential duration, and tonic spiking neuronal excitability. Involved in the regulation of blood glucose and the function of smooth muscle fibers. |
| Kv2.2 | KCNB2 |
|
Mediates transmembrane potassium transport in excitable membranes, primarily in the brain and smooth muscle cells |
Assay List of Kv2 Channel
Creative Biolabs can provide a range of assays of Kv2 channels. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| S01YF-0722-KX222 | Magic™ Human KCNB1 In Vitro Electrophysiology Assay, HEK293 | HEK293 | Electrophysiology Assay |
Published Data
| Paper Title | SP6616 as a Kv2.1 inhibitor efficiently ameliorates peripheral neuropathy in diabetic mice |
| Journal | EBioMedicine |
| Published | 2020 |
| Abstract | SP6616, a Kv2.1 selective inhibitor, was administered to diabetic mice to investigate the pathological mechanism of the Kv2.1 channel in diabetic peripheral neuropathy (DPN). A series of analytical assays have been conducted to reveal the specific mechanisms Kv2.1 channel in DPN and discover potential therapeutics. |
| Result |
Polymerase chain reaction (PCR), immunohistochemistry, and western blot assays have demonstrated that the SP6616 inhibitor significantly inhibited the Kv2.1 expression compared with the increased level in diabetic mice (without change in Kv2.2 level). Further assays found that DRG neuron neurite outgrowth was enhanced by SP6616 inhibitor via inhibiting the Kv2.1 channel in diabetic mice. In addition, by inhibiting the Kv2.1 channel, SP6616 inhibitor treatment also improved peripheral neuropathy, peripheral nerve structure, and vascular function, mitochondrial dysfunction, repressed inflammation in diabetic mice.
|
Fig.2. SP6616 treatment suppressed Kv2.1 expression in DRG tissue of diabetic mice. (Zhu, 2020)
References
- Grizel, A.V.; et al. Mechanisms of activation of voltage-gated potassium channels. Acta Naturae. 2014, 6(4(23)): 10-26.
- Zhu, X., et al. SP6616 as a Kv2.1 inhibitor efficiently ameliorates peripheral neuropathy in diabetic mice. EBioMedicine. 2020, 61: 103061.
