激酶
可药性
个人识别码1
基诺美
小分子
丝氨酸苏氨酸激酶
AKT2型
丝氨酸
化学
基因沉默
磷酸化
癌症研究
生物
生物化学
蛋白激酶A
AKT1型
基因
蛋白激酶B
作者
Siwei Chen,Yu‐Shang Yang,Yong Yuan,Bo Liu
标识
DOI:10.1016/j.ejmech.2023.116016
摘要
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.
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