Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA.
Pharmaceutics. 2011;3(2):186-228. doi: 10.3390/pharmaceutics3020186.
Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated.
蛋白激酶 D (PKD) 属于丝氨酸/苏氨酸激酶家族，在基本细胞过程中发挥重要作用，并与多种疾病的发病机制有关。由于缺乏 PKD 特异性抑制剂，我们对 PKD 生物学功能的理解进展受到限制。苯并恶唑并氮杂卓 CID755673 最近被报道为该酶的第一个有效且激酶选择性抑制剂。为了进行结构活性分析，制备了一系列类似物，并评估了它们的体外抑制活性。
