Department of Urology, Creighton University, Omaha, NE, 68178, USA.
Department of Urology, University of Florida, Jacksonville, FL, 32209, USA.
J Mol Med (Berl). 2023 Apr;101(4):341-349. doi: 10.1007/s00109-023-02298-4. Epub 2023 Feb 27.
Protein kinase D (PrKD), a novel serine-threonine kinase, belongs to a family of calcium calmodulin kinases that consists of three isoforms: PrKD1, PrKD2, and PrKD3. The PrKD isoforms play a major role in pathologic processes such as cardiac hypertrophy and cancer progression. The charter member of the family, PrKD1, is the most extensively studied isoform. PrKD play a dual role as both a proto-oncogene and a tumor suppressor depending on the cellular context. The duplicity of PrKD can be highlighted in advanced prostate cancer (PCa) where expression of PrKD1 is suppressed whereas the expressions of PrKD2 and PrKD3 are upregulated to aid in cancer progression. As understanding of the PrKD signaling pathways has been better elucidated, interest has been garnered in the development of PrKD inhibitors. The broad-spectrum kinase inhibitor staurosporine acts as a potent PrKD inhibitor and is the most well-known; however, several other novel and more specific PrKD inhibitors have been developed over the last two decades. While there is tremendous potential for PrKD inhibitors to be used in a clinical setting, none has progressed beyond preclinical trials due to a variety of challenges. In this review, we focus on PrKD signaling in PCa and the potential role of PrKD inhibitors therein, and explore the possible clinical outcomes based on known function and expression of PrKD isoforms at different stages of PCa.
蛋白激酶 D(PrKD)是一种新型丝氨酸/苏氨酸激酶,属于钙调蛋白激酶家族,该家族由三种同工型组成:PrKD1、PrKD2 和 PrKD3。PrKD 同工型在心脏肥大和癌症进展等病理过程中发挥重要作用。该家族的创始成员 PrKD1 是研究最广泛的同工型。PrKD 可以根据细胞环境发挥原癌基因和肿瘤抑制因子的双重作用。PrKD 的这种双重性在晚期前列腺癌(PCa)中表现得尤为明显,在这种癌症中,PrKD1 的表达受到抑制,而 PrKD2 和 PrKD3 的表达则上调以促进癌症进展。随着对 PrKD 信号通路的理解不断深入,人们对开发 PrKD 抑制剂产生了兴趣。广谱激酶抑制剂星形孢菌素是一种有效的 PrKD 抑制剂,也是最知名的抑制剂;然而,在过去的二十年中,已经开发出了几种其他新型且更具特异性的 PrKD 抑制剂。虽然 PrKD 抑制剂在临床环境中有很大的应用潜力,但由于各种挑战,没有一种抑制剂能超越临床前试验。在这篇综述中,我们重点关注 PrKD 在 PCa 中的信号转导以及 PrKD 抑制剂在其中的潜在作用,并根据不同阶段 PCa 中 PrKD 同工型的已知功能和表达,探讨其可能的临床结果。