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【摘要】The protein Kinase D(PKD) family of serine/threonine kinases plays an important role in regulating a variety of cellular processes.Dysregulation of PKD has been linked to multiple diseases including cancer and PKD actively contributes to tumor growth,metastasis,and angiogenesis,making PKD an attractive drug target for cancer.Here,we describe several studies that aim at identifying and developing potent and selective PKD small molecule inhibitors for anticancer therapy.These novel active site-directed PKD inhibitors exhibit remarkable structural diversity,high potency and selectivity, representing promising leads for further development into selective and therapeutically effective small molecule PKD inhibitors.