Title:Research Progress on Small Molecules Inhibitors Targeting TRK
Kinases
Volume: 30
Issue: 10
关键词:
Trk基因融合，Trk抑制剂，耐药性，克服耐药性，肿瘤，Trk激酶
摘要:
Background: Trk gene fusions are an important driver in the development of
cancers, including secretory breast cancer and infantile congenital sarcoma. Since the
first-generation of small molecule Trk inhibitors (Larotrectinib and Entrectinib) came to
market, research on small molecule TRK inhibitors, especially second-generation inhibitors
that break through the resistance problem, has developed rapidly. Therefore, this article
focuses on the research progress of first-generation drugs and second-generation drugs
that break through drug resistance.
Methods: We used the database to search for relevant and cutting-edge documents, and
then filtered and selected them based on the content. The appropriate articles were analyzed
and classified, and finally, the article was written according to the topics.
Results: The phenomenon of Trk protein fusion and its relation to tumors are described,
followed by an explanation of the composition and signaling pathways of Trk kinases.
The representative Trk inhibitors and the development of novel Trk inhibitors are classified
according to whether they overcome drug resistance problems.
Conclusion: This paper provides a theoretical reference for the development of novel inhibitors
by introducing and summarizing the representative and novel Trk inhibitors that
break through the drug resistance problem.
