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Last update 23 Jan 2025

Kv12.2

Last update 23 Jan 2025

Basic Info

Synonyms

BEC1, Brain-specific eag-like channel 1, ELK channel 2

+ [8]

Introduction

Pore-forming (alpha) subunit of voltage-gated potassium channel. Elicits an outward current with fast inactivation. Channel properties may be modulated by cAMP and subunit assembly.

Drugs associated with Kv12.2

ASP7967

Target

Kv12.2

Mechanism

Kv12.2 blockers

Active Org.

Astellas Pharma, Inc. [+1]

Originator Org.

Okinawa Institute of Science & Technology Promotion Corp. [+1]

Active Indication-

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

EM-902

Target

Kv12.2 x Potassium channel

Mechanism

Kv12.2 blockers [+1]

Active Org.-

Originator Org.

Astellas Pharma, Inc.

Active Indication-

Inactive Indication

Alzheimer Disease [+3]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with Kv12.2

NL-OMON32022

/ CompletedNot Applicable

A double-blind, randomized, placebo-controlled study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of single ascending oral doses of ASP2905 in healthy young males, including an open-label two-period randomized crossover study to compare the pharmacokinetics under fasted and fed conditions - ASP2905 SAD/food effect study

Start Date04 May 2008

Sponsor / Collaborator

Astellas Pharma, Inc.

100 Clinical Results associated with Kv12.2

100 Translational Medicine associated with Kv12.2

0 Patents (Medical) associated with Kv12.2

Literatures (Medical) associated with Kv12.2

01 Mar 2025·Neurology Neuroimmunology & Neuroinflammation

A Systematic Review

Review

Author: Cai, Meng-Ting ; Su, Sheng-Yao ; Lai, Qi-Lun ; Shen, Chun-Hong ; Li, Er-Chuang ; Zhang, Tian-Yi ; Zhang, Yin-Xi

In dipeptidyl-peptidase-like protein 6 (DPPX) antibody-associated encephalitis, DPPX antibodies from serum and CSF target the extracellular subunit of the voltage-gated potassium channel 4.2. This targeting leads to a characteristic clinical triad comprising gastrointestinal symptoms (predominantly diarrhea), cognitive-psychiatric dysfunction, and manifestations of CNS hyperexcitability, with hyperekplexia being a more specific feature. This rare disease typically presents with a subacute or chronic course and often affects middle-aged and older individuals. Patients may have a weak association with certain hematologic malignancies, particularly lymphoma and chronic lymphocytic leukemia. Brain MRI typically shows normal findings or nonspecific white matter changes. DPPX antibody-associated encephalitis responds well to immunotherapy, and most patients ultimately present with a good prognosis. However, relapses can occur. To improve our understanding of this rare but treatable autoimmune encephalitis and avoid misdiagnosis, we conduct a systematic review and summarize the current knowledge of its clinical and paraclinical features, management, and prognosis.

01 Nov 2024·Gene

Analysis of genes differentially expressed in the cortex of mice with the Tbl1xr1 variant

Article

Author: Falize, Kim ; Boelen, Anita ; Bruinstroop, Eveline ; van Trotsenburg, Paul ; Hu, Yalan ; Hennekam, Raoul C ; Fliers, Eric ; Lauffer, Peter ; Jongejan, Aldo

Transducin β-like 1 X-linked receptor 1 (mouse Tbl1xr1) or TBL1X/Y related 1 (human TBL1XR1), part of the NCoR/SMRT corepressor complex, is involved in nuclear receptor signaling. Variants in TBL1XR1 cause a variety of neurodevelopmental disorders including Pierpont syndrome caused by the p.Tyr446Cys variant. We recently reported a mouse model carrying the Tbl1xr1^Y446C/Y446C variant as a model for Pierpont syndrome. To obtain insight into mechanisms involved in altered brain development we studied gene expression patterns in the cortex of mutant and wild type (WT) mice, using RNA-sequencing, differentially expressed gene (DEG) analysis, gene set enrichment analysis (GSEA), weighted gene correlation network analysis (WGCNA) and hub gene analysis. We validated results in mutated mouse cortex, as well as in BV2 and SK-N-AS cell lines, in both of which Tbl1xr1 was knocked down by siRNA. Two DEGs (adj.P. Val < 0.05) were found in the cortex, Mpeg1 (downregulated in mutant mice) and 2900052N01Rik (upregulated in mutant mice). GSEA, WGCNA and hub gene analysis demonstrated changes in genes involved in ion channel function and neuroinflammation in the cortex of the Tbl1xr1^Y446C/Y446C mice. The lowered expression of ion channel genes Kcnh3 and Kcnj4 mRNA was validated in the mutant mouse cortex, and increased expression of TRIM9, associated with neuroinflammation, was confirmed in the SK-N-AS cell line. Conclusively, our results show altered expression of genes involved in ion channel function and neuroinflammation in the cortex of the Tbl1xr1^Y446C/Y446C mice. These may partly explain the impaired neurodevelopment observed in individuals with Pierpont syndrome and related TBL1XR1-related disorders.

15 Jul 2024·International Journal of Cancer

Exploring the tumor genomic landscape of aggressive prostate cancer by whole‐genome sequencing of tissue or liquid biopsies

Article

Author: Kassentoft, Christine Gaasdal ; Farajzadeh, Leila ; Borre, Michael ; Sørensen, Karina Dalsgaard ; Rusan, Maria ; Nørgaard, Maibritt ; Weiss, Simone ; Pedersen, Jakob Skou ; Ulhøi, Benedicte Parm ; Lamy, Philippe ; Jensen, Jørgen Bjerggaard ; Knudsen, Michael

AbstractTreatment resistance remains a major issue in aggressive prostate cancer (PC), and novel genomic biomarkers may guide better treatment selection. Circulating tumor DNA (ctDNA) can provide minimally invasive information about tumor genomes, but the genomic landscape of aggressive PC based on whole‐genome sequencing (WGS) of ctDNA remains incompletely characterized. Thus, we here performed WGS of tumor tissue (n = 31) or plasma ctDNA (n = 10) from a total of 41 aggressive PC patients, including 11 hormone‐naïve, 15 hormone‐sensitive, and 15 castration‐resistant patients. Across all variant types, we found progressively more altered tumor genomic profiles in later stages of aggressive PC. The potential driver genes most frequently affected by single‐nucleotide variants or insertions/deletions included the known PC‐related genes TP53, CDK12, and PTEN and the novel genes COL13A1, KCNH3, and SENP3. Etiologically, aggressive PC was associated with age‐related and DNA repair‐related mutational signatures. Copy number variants most frequently affected 14q11.2 and 8p21.2, where no well‐recognized PC‐related genes are located, and also frequently affected regions near the known PC‐related genes MYC, AR, TP53, PTEN, and BRCA1. Structural variants most frequently involved not only the known PC‐related genes TMPRSS2 and ERG but also the less extensively studied gene in this context, PTPRD. Finally, clinically actionable variants were detected throughout all stages of aggressive PC and in both plasma and tissue samples, emphasizing the potential clinical applicability of WGS of minimally invasive plasma samples. Overall, our study highlights the feasibility of using liquid biopsies for comprehensive genomic characterization as an alternative to tissue biopsies in advanced/aggressive PC.

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Kv12.2

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