Small-molecule inhibitors in myeloproliferative neoplasms: are we aiming for the right targets?

Abstract excerpt

The ATP-binding pocket of the kinase domain of JAK2 is the major target of the present treatment of myeloproliferative neoplasms. Several inhibitors of JAK2 that are ATP competitive have been developed, but they do not discriminate between wild-type and mutant JAK2. These inhibitors have been used in myelofibrosis and, for the first time, treatment induced a reduction in spleen size and in constitutional...

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