Development of a selective inhibitor for Kv1.1 channels prevalent in demyelinated nerves.

Ahmed Al-Sabi,Declan Daly, Myles Rooney,Cian Hughes,Gemma K Kinsella,Seshu K Kaza,Kieran Nolan,J Oliver Dolly

Bioorganic Chemistry（2020）

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摘要

•Compound 3 is a dimeric form of compound 1.•Compound 3 is twice as effective as compound 1 at inhibiting Kv1.1 Channels.•Compound 3 interacts with more regions/residues in Kv1.1 than compound 1.•Compound 3 is more selective for Kv1.1-enriched channels than compound 1.

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关键词

Dipyrromethane,Multiple sclerosis,Molecular modeling,Neuronal Kv1 channels,SAR analysis,Selective blocker design

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