1. Academic Validation
  2. Novel small molecule inhibitors targeting renal cell carcinoma: Status, challenges, future directions

Novel small molecule inhibitors targeting renal cell carcinoma: Status, challenges, future directions

  • Eur J Med Chem. 2024 Mar 5:267:116158. doi: 10.1016/j.ejmech.2024.116158.
Lin Xiong 1 Ya Zhang 2 Jiaxing Wang 3 Min Yu 1 Liming Huang 1 Yanpei Hou 1 Guisen Li 1 Li Wang 1 Yi Li 4
Affiliations

Affiliations

  • 1 Department of Nephrology, Sichuan Provincial People's Hospital, Sichuan Clinical Research Center for Kidney Diseases, Clinical Immunology Translational Medicine Key Laboratory of Sichuan Province, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, Sichuan, China.
  • 2 College of Life Sciences, Sichuan University, Chengdu, 610064, Sichuan, China.
  • 3 Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, 38163, Tennessee, United States.
  • 4 Department of Nephrology, Sichuan Provincial People's Hospital, Sichuan Clinical Research Center for Kidney Diseases, Clinical Immunology Translational Medicine Key Laboratory of Sichuan Province, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, Sichuan, China. Electronic address: liyisn@med.uestc.edu.cn.
Abstract

Renal cell carcinoma (RCC) is the most common renal malignancy with a rapidly increasing morbidity and mortality rate gradually. RCC has a high mortality rate and an extremely poor prognosis. Despite numerous treatment strategies, RCC is resistant to conventional radiotherapy and chemotherapy. In addition, the limited clinical efficacy and inevitable resistance of multiple agents suggest an unmet clinical need. Therefore, there is an urgent need to develop novel anti-RCC candidates. Nowadays many promising results have been achieved with the development of novel small molecule inhibitors against RCC. This paper reviews the recent research progress of novel small molecule inhibitors targeting RCC. It is focusing on the structural optimization process and conformational relationships of small molecule inhibitors, as well as the potential mechanisms and Anticancer activities for the treatment of RCC. To provide a theoretical basis for promoting the clinical translation of novel small molecule inhibitors, we discussed their application prospects and future development directions. It could be capable of improving the clinical efficacy of RCC and improving the therapy resistance for RCC.

Keywords

Drug resistance; Novel small molecule inhibitor; Renal cell carcinoma; Structure-activity relationship; Targeted therapy; Therapeutic strategy.

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