p21-activated kinases and gastrointestinal cancer

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• 作者：Hong He ; Graham S. Baldwin ; ^{grahamsb@unimelb.edu.au}
• 关键词：AID ; auto-inhibitory domain ; CDK5RAP3 ; CDK5 kinase regulatory subunit-associated protein 3 ; CRC ; colorectal carcinoma ; EGFR ; epithelial growth factor receptor ; GAP ; GTPase-activating protein ; HBV ; hepatitis B virus ; HBx ; HBV X protein ; HCC ; hepatocellular
• 刊名：Biochimica et Biophysica Acta (BBA)/Molecular Cell Research
• 出版年：2013
• 出版时间：January, 2013
• 年：2013
• 卷：1833
• 期：1
• 页码：33-39
• 全文大小：353 K

文摘

p21-activated kinases (PAKs) were initially identified as effector proteins downstream from GTPases of the Rho family. To date, six members of the PAK family have been discovered in mammalian cells. PAKs play important roles in growth factor signalling, cytoskeletal remodelling, gene transcription, cell proliferation and oncogenic transformation. A large body of research has demonstrated that PAKs are up-regulated in several human cancers, and that their overexpression is linked to tumour progression and resistance to therapy. Structural and biochemical studies have revealed the mechanisms involved in PAK signalling, and opened the way to the development of PAK-targeted therapies for cancer treatment. Here we summarise recent findings from biological and clinical research on the role of PAKs in gastrointestinal cancer, and discuss the current status of PAK-targeted anticancer therapies.