Kv2 Related Drug Discovery Products
The channel repertoire that determines the intrinsic electrical excitability of a neuron contains a variety of channels, but voltage-dependent K+ (Kv) channels are particularly varied. Which membrane potentials Kv channels are open at depend on their biophysical characteristics. These biophysical characteristics of Kv channels as a group differ considerably more than those of other voltage-gated channels. Even though these intrinsic variations in biophysical characteristics are clearly encoded within the main structure of the specific channel subtype, posttranslational processes also have the ability to change them. Additionally, the biophysical properties can be significantly altered pharmacologically, which forms the basis for a wide range of prospective treatments.
To meet the needs of our customers, Creative Biolabs can offer Kv2 related assays and products to contribute to the success of drug discovery:
Overview of Kv2
Members of the Kv2 (KCNB) family create delayed rectifier K+ channels. Kv2.1 and Kv2.2 exhibit distinct localisation in the brain and in neurons and do not form heteromeric channels. The first member of this family, Kv2.1, is distinctive in that it was found and isolated using expression cloning. Despite this widespread neuronal expression, Kv2.1 staining is quite limited and only found on the somatic and proximal dendritic membranes of individual neurons. It is missing from axons and nerve terminals. Large clusters of Kv2.1 are seen over subsurface cisterns beneath the plasma-membrane-facing astrocytes as well as on the cell surface membrane directly facing astrocyte processes.
Many of the cells that express Kv2.1 also express Kv2.2. The two members of the mammalian Kv2 family do not appear to readily form heteromultimers in native neurons, in contrast to other Kv channels (Kv1, Kv3, and Kv4 family members), as evidenced by the different subcellular localizations of Kv2.1 and Kv2.2 expressed in the same cells. Kv2.2 is consistently present on dendrites and all the way down its length. Kv2.2 does not exhibit the proximal dendritic clustering of Kv2.1. Both cortical pyramidal neurons and olfactory bulb neurons have high levels of Kv2.2.
Kv2 Drug Discovery
Local signaling events can be affected by the localization of Kv channels to particular subcellular domains, and the localization of various Kv channels in neurons is both extremely constrained and incredibly diverse. Many new insights have been discovered regarding the factors that influence the polarized localization of Kv channels (axonal versus somatodendritic). Regarding the degree of dynamic regulation of the quantity and distribution of Kv channels in neurons, a crucial question still has to be answered. Although there are indications that the phosphorylation state affects Kv channel trafficking and localization dynamically, it is still unclear to what degree these and other signaling events contribute to the posttranslational control of Kv channel expression.
