Biological pathways often have an important role in more than one process. Equally, processes that are essential for normal physiology are hijacked by diseases such as cancer. The same pathways that assist tumour growth, survival and spreading can be critically important for the recovery from injuries or other diseases. This means there are often two sides to consider in the research of these pathways. Hepatocyte growth factor (HGF) is a protein that has intrinsically a key role in pathways responsible for dynamic movement, reconstruction and survival of cells for tissue regeneration. In tumour tissues, however, these actions of HGF participate in tumour spreading, metastasis and resistance against anticancer drugs. At the forefront of Matsumoto’s research is the potential targeting of HGF and its receptor MET in regeneration and cancer, leading to drug discovery. He started bioventure to facilitate his research to clinical application. Clinical trials of HGF protein for treatment of amyotrophic lateral sclerosis/ALS and spinal cord injury are ongoing. He recently discovered artificial HGF composed of synthetic peptides. The artificial HGF can be the next generation biological drug by chemical synthesis. Peptides targeting HGF-MET pathway will be invaluable in the drug discovery for diagnosis and therapeutics of cancer.