Discovery of ‘molecular switches’ within a GIRK activator scaffold that afford selective GIRK inhibitors

This letter describes a multi-dimensional SAR campaign based on a potent, efficacious and selective GIRK1/2 activator (~10-fold versus GIRK1/4 and inactive on nonGIRK 1-containing GIRKs, GIRK 2 or GIRK2/3). Further chemical optimization through an iterative parallel synthesis effort identified multi...

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Detalhes bibliográficos
Main Authors: Wen, Wandong, Wu, Wenjun, Romaine, Ian M., Kaufmann, Kristian, Du, Yu, Sulikowski, Gary A., Weaver, C. David, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3816575/
https://ncbi.nlm.nih.gov/pubmed/23838260
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2013.06.023
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