Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.
作者： Eric F. Johnson , Kent D. Stewart , Keith W. Woods , Vincent L. Giranda , Yan Luo
DOI: 10.1021/BI7008745
关键词:
摘要: PLK1 (polo-like kinase 1) is a key mitotic and therapeutic target in the treatment of proliferative diseases. Here we investigate relative substrate specificity pharmacological relatedness PLK1, -2, -3, -4 that together comprise conserved family Ser/Thr kinases (PLK family). We report consensus sequences for PLK2, an expanded sequence which use to design optimal peptide substrate, PLKtide. inhibitory activity entire PLK across diverse set small-molecule ATP-competitive inhibitors including several clinical compounds. With respect both ATP-site specificity, highest similarity observed between PLK2 PLK3, next most similar, PLK4 least similar. Further, have identified time-dependent inhibition by two potent selective inhibitors.
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