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Updated: Sep 5, 2025

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
Published on: November 5, 2014
PAK4 in cancer development: Emerging player and therapeutic opportunities
Yixi Yuan1, Hongyan Zhang1, Danni Li2
1Department of Cell Biology, Key Laboratory of Cell Biology, National Health Commission of the PR China, Key Laboratory of Medical Cell Biology, Ministry of Education of the PR China, China Medical University, No. 77, Puhe Road, Shenyang North New Area, Shenyang, Liaoning, 110122, China.
Abstract:
p21-activated kinase 4 (PAK4), a member of the serine-threonine kinase family, was initially identified as a protein kinase that functions downstream of the Rho GTPases cdc42 and Rac1. Recently, it has been proven that PAK4 not only regulates many cellular physiological processes, but also plays an important role in the occurrence and development of various cancers. Here, we provide a systematic overview of PAK4, including its structure, localization, expression and aberration, upstream regulators, and key functions in almost every aspect of cancer hallmarks, including cancer cell proliferation, invasion and metastasis, angiogenesis, metabolism reprogramming, and immune escape. Subsequently, we also discuss the existing small molecule PAK4 inhibitors according to their structure types and their potential applications in cancer treatment. We hope our systematic review will provide the most comprehensive description of the current advancements in PAK4 research and new enlightenment for the individualized diagnosis and treatment of cancer.
Insights
p21-activated kinase 4 (PAK4) is crucial in cancer development, regulating proliferation, metastasis, and immune escape. This review details PAK4
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- p21-activated kinase 4 (PAK4) is a serine-threonine kinase downstream of Rho GTPases.
- PAK4 regulates cellular processes and is implicated in various cancers.
Purpose of the Study:
- To provide a systematic overview of PAK4's role in cancer.
- To discuss PAK4 inhibitors for cancer treatment.
Main Methods:
- Systematic literature review of PAK4.
- Analysis of PAK4 structure, localization, expression, and function in cancer hallmarks.
- Review of small molecule PAK4 inhibitors.
Main Results:
- PAK4 is involved in cancer cell proliferation, invasion, metastasis, angiogenesis, metabolism reprogramming, and immune escape.
- Various small molecule inhibitors targeting PAK4 have been developed.
Conclusions:
- PAK4 is a significant factor in multiple cancer hallmarks.
- PAK4 inhibitors show potential for individualized cancer diagnosis and treatment.
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