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

A report on the discovery of a new potent allosteric effector of sickle cell haemoglobin, GBT440, that increases the affinity of haemoglobin for oxygen and consequently inhibits its polymerisation when subjected to hypoxic conditions. GBT440 is in Phase 3 clinical trials for the treatment of sickle cell disease (NCT03036813).

[1] Metcalf et al. (2017). ACS Medical Chemistry Letters DOI:10.1021/acsmedchemlett.6b00491. Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. [link]

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