Targeting integrins in hepatocellular carcinoma

Abstract

Introduction: Integrins, which are heterodimeric membrane glycoproteins, consist of a family of cell-surface receptors mediating cell–matrix and cell–cell adhesion. Analysis of tumor-associated integrins has revealed an important relationship between integrins and tumor development, bringing new insights into integrin-based cancer therapies. Hepatocellular carcinoma (HCC) is one of the most malignant tumors worldwide and integrins appeal to be a novel group of potential therapeutic targets for HCC.

Areas covered: This review summarizes the current knowledge of integrins involved in HCC and the potential of integrin-targeted drugs in HCC therapy. A brief introduction on the structure, biological function and regulatory mechanism of integrins is given. The distinct expression patterns and biological functions of HCC-associated integrins are described. Finally, the current situation of integrin-based therapies in HCC and other tumor types are extensively discussed in the light of their implications in preclinical and clinical trials.

Expert opinion: To date, increasing numbers of integrin-targeted drugs are undergoing development and they exhibit diverse effects in cancer clinical trials. Tumor heterogeneity should be emphasized in developing effective integrin-targeted drugs specific for HCC. A better understanding of how integrins cooperatively function in HCC will assist in designing more successful integrin-targeted therapeutic drugs and corresponding approaches.

Keywords::

• angiogenesis
• extracellular matrix
• hepatocellular carcinoma
• integrin

Acknowledgement

We thank Professor Y Xie and HS Xie (Department of Biology, The Hong Kong University of Science & Technology, China) for their kind help with language revision. We also thank X Yang (Institute of Genetics, Fudan University, China) for helpful discussion.

Notes

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