Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin

[Image: see text] We report the discovery of a new potent allosteric effector of sickle cell hemoglobin, GBT440 (36), that increases the affinity of hemoglobin for oxygen and consequently inhibits its polymerization when subjected to hypoxic conditions. Unlike earlier allosteric activators that bind...

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Detalles Bibliográficos
Autores principales: Metcalf, Brian, Chuang, Chihyuan, Dufu, Kobina, Patel, Mira P., Silva-Garcia, Abel, Johnson, Carl, Lu, Qing, Partridge, James R., Patskovska, Larysa, Patskovsky, Yury, Almo, Steven C., Jacobson, Matthew P., Hua, Lan, Xu, Qing, Gwaltney, Stephen L., Yee, Calvin, Harris, Jason, Morgan, Bradley P., James, Joyce, Xu, Donghong, Hutchaleelaha, Athiwat, Paulvannan, Kumar, Oksenberg, Donna, Li, Zhe
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5346980/
https://www.ncbi.nlm.nih.gov/pubmed/28337324
http://dx.doi.org/10.1021/acsmedchemlett.6b00491

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