期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 175, 期 -, 页码 129-148出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.04.053
关键词
Tropomyosin receptor kinase; Neoplasm; Receptor kinase inhibitor; Gene alterations
资金
- National Natural Science Foundation of China [81773559, 21807114, 21472191]
- Double First-Class University Project [CPU2018GY03]
- National Major Scientific and Technological Program for Drug Discovery Grant [2018ZX09301045002]
- International Cooperation Grant of Guangzhou of Guangzhou [201704030099]
- State Key Laboratory of Natural Medicines, China Pharmaceutical University [SKLNMZZRC201810]
- Chinese Pharmaceutical Association-Yiling Biopharmaceutical Innovation Foundation
NTRKs and their expression product tropomyosin receptor kinases (Trks) are widely distributed in mammals. While neural growth factor (NGF)-induced normal Trk activation plays a key role in nerve growth, NTRK alternations occurring in tumor cells were highly correlated to tumor progression and invasion. Recent clinical data from several pan-Trk inhibitors have demonstrated potential and broad applications in various cancers. This intrigues us to summarize the development of inhibitors targeting Trks with different mechanisms of action and their applications in cancer therapy. We believe that this perspective would be of great help in investigating novel anticancer drugs with better therapeutic index. (C) 2019 Published by Elsevier Masson SAS.
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