Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity
作者:Václav Němec、Prashant Khirsariya、Pavlína Janovská、Paula Martín Moyano、Lukáš Maier、Petra Procházková、Pavlína Kebková、Tomáš Gybel'、Benedict‐Tilman Berger、Apirat Chaikuad、Maria Reinecke、Bernhard Kuster、Stefan Knapp、Vítězslav Bryja、Kamil Paruch
DOI:10.1002/anie.202217532
日期:2023.3.6
and CK1ϵ in cells as well as in vivo. Our observations suggest that the central scaffold can be used more broadly in compounds targeting other protein kinases, as evidenced by the highly selective p38α inhibitor MU1299.
新发现的化学生物学探针MU1250、MU1500和MU1742,基于 1 H-吡咯并[2,3- b ]吡啶-咪唑支架,允许高度特异性靶向细胞中的亚型 CK1α、CK1δ 和 CK1ε体内。我们的观察表明,中央支架可以更广泛地用于靶向其他蛋白激酶的化合物,高选择性 p38α 抑制剂MU1299证明了这一点。