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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2017
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5346980/
https://ncbi.nlm.nih.gov/pubmed/28337324
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00491
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