Novel Small Molecules in Targeted Cancer Therapy

Over the last few decades, small molecule cancer drug discovery and development have focused on personalized medicine, emphasizing molecularly targeted drugs. Because of their small size (usually ≤ 500Da), small molecules have been successfully used to target the extracellular, cell surface ligand-binding receptors and the intracellular proteins that play key roles in transducing downstream signalling for cancer cell survival, proliferation, and metastasis. Small molecule cancer drugs cover a wide range of inhibitors, including kinase inhibitors, proteasome inhibitors, matrix metalloproteinase inhibitors, etc. Research on molecularly targeted cancer drug discovery has resulted in some small molecule drugs being successfully introduced in the clinic for cancer treatment. By December 2020, 89 small-molecule targeted cancer drugs have been approved by the US FDA and the National Medical Products Administration (NMPA) of China. It provides more optional approaches for personalized medicine in different cancers treatment.

Although many small molecules cancer drugs have been developed and are currently being utilized in the clinic, many challenges remain a significant and formidable problem, such as a low response rate and drug resistance. In addition, certain small molecules bind to multiple molecular targets, including cell surface receptors and other intracellular proteins, thus increasing the risk of toxicity. Addressing these challenges will enhance our rapid progress in small molecule cancer drug development toward truly personalized medicine for cancer patients. It can be achieved by identifying novel small molecule cancer drugs and a better understanding of mechanisms underlying the effect of small molecule cancer drugs, leading to improving the efficacy of currently marketed drugs.

In this Research Topic, we welcome manuscripts that specifically focus on the basic, pre-clinical and clinical study concerning novel small molecules in targeted cancer therapy, with an emphasis on the identification of new targets and mechanisms. Authors are encouraged to submit original experimental articles, expert reviews, short communications, and clinical trial articles associated with this Research Topic. We expect submissions relating to, but not limited to, the following topics:
• Identifying novel small molecule anticancer drugs for targeted cancer therapy.
• Identifying new pharmacological activities and mechanisms of action of small molecule anticancer drugs supported by animal or clinical data.
• Exploring the molecular mechanisms and regulatory networks of novel small molecule anticancer drugs for clinical cancer therapy.
• The combination of novel small molecules with other anti-cancer strategies.

In addition, for manuscripts dealing with plant extracts or other natural substances/compounds, the composition and the stability of the study material must be described in sufficient detail. In particular, for extracts, chromatograms with characterization of the dominating compound(s) are requested. The level of purity must be proven and included.

Keywords: Small molecules, Cancer, Cell Death, Metastasis, Molecular Mechanism, Pharmacology, Targeted Therapy

Important note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.