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KCNQ2 Identifiers Aliases KCNQ2 , BFNC, BFNS1, EBN, EBN1, EIEE7, ENB1, HNSPC, KCNA11, KV7.2, KVEBN1, potassium voltage-gated channel subfamily Q member 2, DEE7External IDs OMIM : 602235 ; MGI : 1309503 ; HomoloGene : 26174 ; GeneCards : KCNQ2 ; OMA :KCNQ2 - orthologs Wikidata
Kv 7.2 (KvLQT2) is a potassium channel protein coded for by the gene KCNQ2.
It is associated with benign familial neonatal epilepsy .
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Ligands
ICA-069673
Compound #40 (Amato 2011)
ICA-069673: channel opener at KCNQ2/Q3 , 20-fold selective over KCNQ3/Q5 , no measurable activity against a panel of cardiac ion channels (hERG , Nav1.5 , L type channels, and KCNQ1 ) and no activity on GABAA gated channels at 10 μM. A range of related benzamides exhibited activity, of which compound number 40 is shown here.[5]
ML252: channel inhibitor, IC50 = 70nM.[6]
References
^ a b c ENSG00000281151 GRCh38: Ensembl release 89: ENSG00000075043, ENSG00000281151 – Ensembl , May 2017
^ a b c GRCm38: Ensembl release 89: ENSMUSG00000016346 – Ensembl , May 2017
^ "Human PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ "Mouse PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ Amato G, JMC Lett 2011, 481, doi :10.1021/ml200053x
^ Cheung YY, Yu H, Xu K, et al. (2012). "Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor" . J. Med. Chem . 55 (15): 6975–9. doi :10.1021/jm300700v . PMC 3530927 . PMID 22793372 .
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Further reading
External links
This article incorporates text from the United States National Library of Medicine , which is in the public domain .
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