Molecular targeted therapy for anticancer treatment

• Published in: Experimental & molecular medicine Vol. 54; no. 10; pp. 1670 - 1694
• Main Authors: Min, Hye-Young, Lee, Ho-Young
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 01.10.2022; Springer Nature B.V
• Subjects: 631/67/1059/602; 692/699/67/1059/602; Antibodies, Monoclonal - therapeutic use; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Biomedical and Life Sciences; Biomedicine; Cancer; Cancer therapies; Chemotherapy; Drug development; Drug resistance; Drug Resistance, Neoplasm; Humans; Medical Biochemistry; Molecular Medicine; Molecular Targeted Therapy; Monoclonal antibodies; Mutation; Neoplasms - drug therapy; Neoplasms - genetics; Precision Medicine; Review; Review Article; Signal transduction; Stem Cells; Therapeutic targets; Tumor cells
• ISSN: 2092-6413; 1226-3613; 2092-6413
• DOI: 10.1038/s12276-022-00864-3

Since the initial clinical approval in the late 1990s and remarkable anticancer effects for certain types of cancer, molecular targeted therapy utilizing small molecule agents or therapeutic monoclonal antibodies acting as signal transduction inhibitors has served as a fundamental backbone in precision medicine for cancer treatment. These approaches are now used clinically as first-line therapy for various types of human cancers. Compared to conventional chemotherapy, targeted therapeutic agents have efficient anticancer effects with fewer side effects. However, the emergence of drug resistance is a major drawback of molecular targeted therapy, and several strategies have been attempted to improve therapeutic efficacy by overcoming such resistance. Herein, we summarize current knowledge regarding several targeted therapeutic agents, including classification, a brief biology of target kinases, mechanisms of action, examples of clinically used targeted therapy, and perspectives for future development. Cancer: A focused approach to therapy Molecular targeted therapies have transformed cancer treatment, enabling personalized treatment of tumors in which growth is being powered by specific mutations. In contrast to traditional chemotherapies, which are toxic to both healthy and tumor cells, these targeted agents are designed to specifically block the effects of particular signaling proteins whose activity is largely restricted to cancerous tissue. Hye-Young Min and Ho-Young Lee at Seoul National University, South Korea, briefly review the history of the development of these drugs, and outline the mechanisms by which different targeted therapies work and how the acquisition of new tumor mutations can confer drug resistance. They also examine recent progress in developing agents that target proteins that have previously proven challenging therapeutic targets, such as the well-known oncogene KRAS , and explore potential opportunities for future therapeutic development.