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As molecular indicators, biomarkers would be the ideal tools to find valid and measurable ways to determine whether a drug works and where it works.Currently, many biomarkers have been used as target for drug discovery or disease diagnosis.For example, APN, also known as CD13, which is a membrane-bound glycoprotein and widely overexpressed on tumor cells, has been found to play a crucial role in invasion into tumor cells.Therefore, anti-APN/CD13 monoclonal antibody and APN inhibitors have been used to suppress the process of tumor cell invasion.Another example of biomarker is some oligosaccharides on tumor cell surface, such as sialyl Lewis A (sLea) and sialyl Lewis X (sLex), which were associated with development and progress of many types of cancers.The development of molecular analysis probes targeted to these pathologically relevant carbohydrates will undoubtedly aid the diagnosis ,prognosis, staging, and treatment of many cancers.