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Discovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na(+)/H(+) Exchanger Isoform 3

[Image: see text] We present herein the design, synthesis, and optimization of gut-restricted inhibitors of Na(+)/H(+) exchanger isoform 3 (NHE3). NHE3 is predominantly expressed in the kidney and gastrointestinal tract where it acts as the major absorptive sodium transporter. We desired minimally s...

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Detalles Bibliográficos
Autores principales: Jacobs, Jeffrey W., Leadbetter, Michael R., Bell, Noah, Koo-McCoy, Samantha, Carreras, Christopher W., He, Limin, Kohler, Jill, Kozuka, Kenji, Labonté, Eric D., Navre, Marc, Spencer, Andrew G., Charmot, Dominique
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9290029/
https://www.ncbi.nlm.nih.gov/pubmed/35859876
http://dx.doi.org/10.1021/acsmedchemlett.2c00037