Last update 01 Nov 2024

Kv1.5 x Kv1.3

Last update 01 Nov 2024

Basic Info

Related Targets

Kv1.5Kv1.3

Drugs associated with Kv1.5 x Kv1.3

AVE-0118

Target

Kv1.3 x Kv1.5

Mechanism

Kv1.3 blockers [+1]

Active Org.

Mosanna Therapeutics AGStartup

Originator Org.

Sanofi

Active Indication

Sleep Apnea, Obstructive

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with Kv1.5 x Kv1.3

100 Translational Medicine associated with Kv1.5 x Kv1.3

0 Patents (Medical) associated with Kv1.5 x Kv1.3

121

Literatures (Medical) associated with Kv1.5 x Kv1.3

01 Jul 2024·The Korean Journal of Physiology & Pharmacology

3,3′,4,4′-tetrachlorobiphenyl (PCB77) enhances human Kv1.3 channel currents and alters cytokine production

Article

Author: Park, Seo-In ; Jung, Yu-Jin ; Jo, Su-Hyun ; Lee, Hyo-Ji ; Kim, Jong-Hui ; Hwang, Soobeen

Polychlorinated biphenyls (PCBs) were once used throughout various industries; however, because of their persistence in the environment, exposure remains a global threat to the environment and human health. The Kv1.3 and Kv1.5 channels have been implicated in the immunotoxicity and cardiotoxicity of PCBs, respectively. We determined whether 3,3',4,4'-tetrachlorobiphenyl (PCB77), a dioxin-like PCB, alters human Kv1.3 and Kv1.5 currents using the Xenopus oocyte expression system. Exposure to 10 nM PCB77 for 15 min enhanced the Kv1.3 current by approximately 30.6%, whereas PCB77 did not affect the Kv1.5 current at concentrations up to 10 nM. This increase in the Kv1.3 current was associated with slower activation and inactivation kinetics as well as right-shifting of the steady-state activation curve. Pretreatment with PCB77 significantly suppressed tumor necrosis factor-α and interleukin-10 production in lipopolysaccharide-stimulated Raw264.7 macrophages. Overall, these data suggest that acute exposure to trace concentrations of PCB77 impairs immune function, possibly by enhancing Kv1.3 currents.

01 Oct 2023·Biophysical Reviews

Adam, amigo, brain, and K channel

Review

Author: Kodirov, Sodikdjon A

Voltage-dependent K⁺ (Kv) channels are diverse, comprising the classical Shab - Kv2, Shaker - Kv1, Shal - Kv4, and Shaw - Kv3 families. The Shaker family alone consists of Kv1.1, Kv1.2, Kv1.3, Kv1.4, Kv1.5, Kv1.6, and Kv1.7. Moreover, the Shab family comprises two functional (Kv2.1 and Kv2.2) and several "silent" alpha subunits (Kv2.3, Kv5, Kv6, Kv8, and Kv9), which do not generate K current. However, e.g., Kv8.1, via heteromerization, inhibits outward currents of the same family or even that of Shaw. This property of Kv8.1 is similar to those of designated beta subunits or non-selective auxiliary elements, including ADAM or AMIGO proteins. Kv channels and, in turn, ADAM may modulate the synaptic long-term potentiation (LTP). Prevailingly, Kv1.1 and Kv1.5 are attributed to respective brain and heart pathologies, some of which may occur simultaneously. The aforementioned channel proteins are apparently involved in several brain pathologies, including schizophrenia and seizures.

01 Mar 2023·Journal of Chemical Neuroanatomy

Domain and cell type-specific immunolocalisation of voltage-gated potassium channels in the mouse striatum

Article

Author: Monteiro, Ana Rita ; Seifi, Mohsen ; Jackson, Torquil ; Otuyemi, Babajide ; Ma, Ruolin ; Swinny, Jerome D

Diverse classes of voltage-gated potassium channels (Kv) are integral to the variety of electrical activity patterns that distinguish different classes of neurons in the brain. A feature of their heterogenous expression patterns is the highly precise manner in which specific cell types target their location within functionally specialised sub-cellular domains. Although Kv expression profiles in cortical brain regions are widely reported, their immunolocalisation in sub-cortical areas such as the striatum, and in associated diseases such as Parkinson's disease (PD), remain less well described. Therefore, the broad aims of this study were to provide a high resolution immunolocalisation analysis of various Kv subtypes within the mouse striatum and assess their potential plasticity in a model of PD. Immunohistochemistry and confocal microscopy revealed that immunoreactivity for Kv1.1, 1.2 and 1.4 overlapped to varying degrees with excitatory and inhibitory axonal marker proteins suggesting these Kv subtypes are targeted to axons innervating striatal medium spiny neurons (MSNs). Immunoreactivity for Kv1.3 strongly overlapped with signal for mitochondrial marker proteins in MSN somata and dendrites. Kv1.5 immunoreactivity was expressed in parvalbumin-immunopositive neurons whereas Kv1.6 was located in cells immunopositive for microglia. Signal for Kv2.1 was concentrated on the somatic and proximal dendritic plasma membrane of MSNs, whilst immunoreactivity for Kv4.2 was targeted to their distal dendritic regions. Finally, striatal Kv2.1 expression, at both the mRNA and protein levels, was decreased in alpha-synuclein overexpressing mice, yet increased in alpha-synuclein knockout mice, compared to wild-type counterparts. The data indicate a variety of Kv expression patterns that are distinctive to the striatum and susceptible to pathology that mirrors PD. Furthermore, these findings advance our understanding of the molecular diversity of various striatal cell types, and potentially have implications for the homeostatic changes of MSN excitability during associated medical conditions such as PD.

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