Chemistry and biology for the small molecules targeting characteristics of cancer cells

Despite the marked progress of cancer research, cancer is the predominant cause of death in Japan, and therefore development of effective therapeutic drugs is expected. Chemical biology is a research field utilizing small molecules to investigate biological phenomena. One of the most important aims of chemical biology is to find the small molecules, and natural products are ideal screening sources due to their structural diversity. Therefore, natural product screening based on the progress of chemical biology prompted us to find small molecules targeting cancer characteristics. Another contribution of chemical biology is to facilitate the target identification of small molecule. Therefore, among a variety of methods to uncover protein function, chemical biology is a remarkable approach in which small molecules are used as probes to elucidate protein functions related to cancer development.

EGF: Epidermal growth factor; PDGF: Platelet-derived growth factor; CRPC: Castration-resistant prostate cancer; AR: Androgen receptor; FTase: Farnesyl transferase; 5-LOX: 5-Lipoxygenase; LT: Leukotriene; CysLT1: Cysteinyl leukotriene receptor 1; GPA: Glucopiericidin A; PA: Piericidin A; XN: Xanthohumol; VCP: Valosin-containing protein; ACACA: Acetyl-CoA carboxylase-α.