针对蛋白酶卡氏蛋白酶家族中其他候选蛋白质在癌症治疗中具有巨大潜力的观点，卡氏蛋白酶B（CtsB）的重要性是异常突出的。基于其对癌症发生的作用、密切连接于调节细胞凋亡和通过其分泌或隔室亚细胞定位调节胞外和胞内功能的作用，共同突出了其与许多正常和病理调节过程的复杂分子参与。尽管其功能性质复杂，但CtsB正在成为极少数经过广泛研究以产生癌症治疗可见成果的卡氏蛋白酶之一。在本文中，我们从强调一个从基础研究向更广泛的临床和转化背景迅速转变的范例的角度，审视了科学文献对CtsB在癌症进展中表达的合理性或塑造了其重要性。通过描述CtsB特异性活性基探针的发展、这些基探针快速演变为新一代前药以及在模型系统中评估其作为抗癌药物的治疗潜力，我们详细说明了其作为诊断标记物的成熟程度。

In view of other candidate proteins from the cathepsin family of proteases holding great potential in being targeted during cancer therapy, the importance of Cathepsin B (CtsB) stands out as being truly exceptional. Based on its contribution to oncogenesis, its intimate connection with regulating apoptosis and modulating extracellular and intracellular functions through its secretion or compartmentalized subcellular localization, collectively highlight its complex molecular involvement with a myriad of normal and pathological regulatory processes. Despite its complex functional nature, CtsB is emerging as one of the few cathepsin proteases that has been extensively researched to yield tangible outcomes for cancer therapy.In this article, we review the scientific literature that has justified or shaped the importance of CtsB expression in cancer progression, from the perspective of highlighting a paradigm that is rapidly changing from basic research toward a broader clinical and translational context.In doing so, we detail its maturation as a diagnostic marker through describing the development of CtsB-specific Activity-Based Probes, the rapid evolution of these toward a new generation of Prodrugs, and the evaluation of these in model systems for their therapeutic potential as anti-cancer agents in the clinic.