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Introduction: Zhen Yongsu is a professor and chairman of the Department of Oncology, Institute of Medicinal Biotechnology of the Chinese Academy of Medical Sciences and Peking Union Medical College. He is one of the pioneers in the research on and development of antitumor drugs, especially antitumor antibiotics, in China. He has developed new models and assays for screening of antitumor drugs. As a principal investigator, he has studied and developed a series of antitumor antibiotics, including zhengguangmycin, guanghuimycin, pingyangmycin, boanmycin, and lidamycin. Among them, pingyangmycin has been widely used in clinical cancer chemotherapy in China over 26 years and listed as national essential drug. He demonstrated for the first time in China that a nucleoside transport inhibitor can be used to enhance the efficacy of antitumor drugs and pointed out that nucleoside transport can serve as a target for cancer chemotherapy. His published paper on this topic has been widely cited. Based on the study of nucleoside transport inhibitors, he has found several antitumor biochemical modulators of natural origin. In the field of biotechnology medicines, he has prepared several monoclonal antibody immunoconjugates and fusion proteins for cancer. In particular, he has made new progress in molecule downsizing of antibody-based conjugates and fusion proteins. He has published over 200 scientific articles. As chief editor, he has published three professional books, i.e., Antibody Engineering Drugs, TEA: Bioactivity and Therapeutic Potential (in English), and Antitumor Drug Research and Development. He won the second prize of the National Invention Award for the study of pingyangmycin and the Scientific Achievement Award at the National Science Congress for the study of zhengguangmycin. In addition, he won three prizes of the Science and Technology Advancement by the ministry, and the title of the National Scientist with Distinguished Contributions in 1986. He won Ho-Leung-Ho-Lee Prize for Science and Technology Advancement in 2001.