PIM kinases, a serine/threonine kinase family with three isoforms, has been well-known to participate in multiple physiological processes by phosphorylating various downstream targets. Accumulating evidence has recently unveiled that aberrant upregulation of PIM kinases (PIM1, PIM2, and PIM3) are closely associated with tumor cell proliferation, migration, survival, and even resistance. Inhibiting or silencing of PIM kinases has been reported have remarkable antitumor effects, such as anti-proliferation, pro-apoptosis and resensitivity, indicating the therapeutic potential of PIM kinases as potential druggable targets in many types of human cancers. More recently, several pharmacological small-molecule inhibitors have been preclinically and clinically evaluated and showed their therapeutic potential; however, none of them has been approved for clinical application so far. Thus, in this perspective, we focus on summarizing the oncogenic roles of PIM kinases, key signaling network, and pharmacological small-molecule inhibitors, which will provide a new clue on discovering more candidate antitumor drugs targeting PIM kinases in the future.

PIM 激酶是一个具有三种亚型的丝氨酸/苏氨酸激酶家族，众所周知，它通过磷酸化各种下游靶标来参与多种生理过程。最近越来越多的证据表明，PIM 激酶（PIM1、PIM2 和 PIM3）的异常上调与肿瘤细胞增殖、迁移、存活甚至耐药性密切相关。据报道，抑制或沉默 PIM 激酶具有显着的抗肿瘤作用，例如抗增殖、促凋亡和再敏感性，表明 PIM 激酶作为多种人类癌症的潜在药物靶点的治疗潜力。最近，几种药理学小分子抑制剂已经过临床前和临床评估，并显示出它们的治疗潜力；但迄今为止，尚未批准临床应用。因此，从这个角度，我们重点总结PIM激酶、关键信号网络和药理小分子抑制剂的致癌作用，这将为未来发现更多针对PIM激酶的候选抗肿瘤药物提供新线索。