Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372246 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Janus kinase 2 (JAK2) plays a crucial role in the pathomechanism of myeloproliferative disorders and hematologic malignancies. A somatic mutation of JAK2 (Val617Phe) was previously shown to occur in 98% of patients with polycythemia vera and 50% of patients with essential thrombocythemia and primary myelofibrosis. Thus, effective JAK2 kinase inhibitors may be of significant therapeutic importance. Here, we applied a structure-based virtual screen to identify novel JAK2 inhibitors. One JAK2 inhibitor in particular, G6, demonstrated remarkable potency as well as specificity, which makes it as a potential lead candidate against diseases related to elevated JAK2 tyrosine kinase activity.
Graphical abstractA specific and potent JAK2 inhibitor G6 was identified by structure-based virtual screening.Figure optionsDownload full-size imageDownload as PowerPoint slide