小分子药物和靶向治疗黑色素瘤：当前策略和未来方向

Title:Small Molecule Drugs and Targeted Therapy for Melanoma: Current Strategies and Future Directions

Volume: 24 Issue: 21

关键词: 黑色素瘤，转移，小分子，靶向治疗，耐药性，MAPK通路，细胞周期控制

摘要: Malignant melanoma is the most aggressive and life-threatening skin cancer. Melanoma develops in melanocytes and is characterized by a very high tendency to spread to other parts of the body. Its pathogenesis depends on DNA mutations leading to the activation of oncogenes or to the inactivation of suppressor genes. The identification of misregulations in intracellular signal transduction pathways has provided an opportunity for the development of mutation-specific inhibitors, which specifically target the mutated signaling cascades. Over the last few years, clinical trials with MAPK pathway inhibitors have shown significant clinical activity in melanoma; however, their efficacy is limited due to the onset of acquired resistance. This has prompted a large set of preclinical studies looking at new approaches of pathway- or target-specific inhibitors. This review gives an overview of the latest developments of small molecule targeting multiple molecular pathways in both preclinical and clinical melanoma settings, with particular emphasis on additional strategies to tackle the reduced responsiveness to inhibitor treatment as possible future directions.

Cite this article as:

Small Molecule Drugs and Targeted Therapy for Melanoma: Current Strategies and Future Directions, Current Medicinal Chemistry 2017; 24 (21) . https://dx.doi.org/10.2174/0929867324666170414163937