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Recent advances of small-molecule c-Src inhibitors for potential therapeutic utilities
Xia-Wen Dang1, Ji-Long Duan1, Emily Ye2
1School of Pharmacy, Key Laboratory of Elemene Class Anticancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, Zhejiang 311121, China.
Abstract:
Proto-oncogene tyrosine-protein kinase Src, also known as c-Src, belongs to the family of non-receptor tyrosine protein kinases (TKs) called Src kinases. It plays a crucial role in cell division, motility, adhesion, and survival in both normal cells and cancer cells by activating various signaling pathways mediated by multiple cytokines. Additionally, c-Src kinase has been implicated in osteoclasts and bone loss diseases mediated by inflammation and osteoporosis. In recent years, remarkable advancements have been achieved in the development of c-Src inhibitors, with several candidates progressing to the clinical stage. This review focuses on the research progress in several areas, including the mechanism of action, drug discovery, combination therapy, and clinical research. By presenting this information, we aim to provide researchers with convenient access to valuable insights and inspire new ideas to expedite future drug discovery programs.
Insights
Proto-oncogene tyrosine-protein kinase Src (c-Src) is vital in cell functions and cancer. This review details c-Src inhibitors, covering their action, discovery, combination therapy, and clinical progress.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Proto-oncogene tyrosine-protein kinase Src (c-Src) is a non-receptor tyrosine kinase crucial for cellular processes like division, motility, adhesion, and survival.
- c-Src signaling pathways are implicated in normal cell function and cancer progression, as well as in bone loss diseases such as osteoporosis.
Purpose of the Study:
- To review recent advancements in c-Src inhibitor research.
- To provide insights into the mechanism of action, drug discovery, combination therapy, and clinical research of c-Src inhibitors.
Main Methods:
- Literature review of research progress on c-Src inhibitors.
- Analysis of studies focusing on mechanism of action, drug discovery, combination therapy, and clinical trials.
Main Results:
- Significant progress has been made in developing c-Src inhibitors, with several candidates entering clinical trials.
- The review consolidates information on c-Src's role in various diseases and therapeutic strategies.
Conclusions:
- c-Src inhibitors represent a promising therapeutic avenue for cancers and inflammatory bone diseases.
- Further research and development in c-Src inhibitor programs are encouraged to expedite drug discovery.
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