人激肽释放酶相关肽酶 (KLK) 代表了 15 种丝氨酸内肽酶的亚组，参与各种生理过程和病理学，包括癌症。本综述旨在提供 KLK 家族的全面概述，重点介绍其基因组结构、表达谱和底物特异性。我们探索 KLK 在肿瘤发生中的作用，强调它们作为癌症治疗中的生物标志物和治疗靶点的潜力。 KLK 的失调活性与多种恶性肿瘤有关，使其成为癌症诊断和治疗的有希望的候选者。：了解 KLK 相关肿瘤发生机制的最新进展为开发靶向癌症治疗提供了新的前景。专家意见表明，虽然已经取得了重大进展，但还需要进一步研究以充分发挥 KLK 在临床应用中的潜力。

Human kallikrein-related peptidases (KLKs) represent a subgroup of 15 serine endopeptidases involved in various physiological processes and pathologies, including cancer.This review aims to provide a comprehensive overview of the KLK family, highlighting their genomic structure, expression profiles and substrate specificity. We explore the role of KLKs in tumorigenesis, emphasizing their potential as biomarkers and therapeutic targets in cancer treatment. The dysregulated activity of KLKs has been linked to various malignancies, making them promising candidates for cancer diagnostics and therapy.: Recent advancements in understanding the mechanistic pathways of KLK-related tumorigenesis offer new prospects for developing targeted cancer treatments. Expert opinion suggests that while significant progress has been made, further research is necessary to fully exploit KLKs' potential in clinical applications.