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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Bibliografische gegevens
Gepubliceerd in:ACS Med Chem Lett
Hoofdauteurs: 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
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: American Chemical Society 2017
Online toegang: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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