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Discovery of Tropomyosin Receptor Kinase Inhibitors as New Generation Anticancer Agents: A Review
Ishan Panchal1,2, Rati Kailash Prasad Tripathi3, Kinjal Parmar4
1Department of Pharmaceutical Chemistry, Parul Institute of Pharmacy, Parul University, Vadodara, 391 760, Gujarat, India.
Background:
The tropomyosin receptor kinases (TRKs) are crucial for many cellular functions, such as growth, motility, differentiation, and metabolism. Abnormal TRK signalling contributes to a variety of human disorders, most evidently cancer. Comprehensive genomic studies have found numerous changes in the genes that code for TRKs like MET, HER2/ErbB2, and EGFR, among many others. Precision medicine resistance, relapse occurring because of the protein point mutations, and the existence of multiple molecular feedback loops are significant therapeutic hurdles to the long-term effectiveness of TRK inhibitors as general therapeutic agents for the treatment of cancer.
Objective:
This review is carried out to highlight the role of tropomyosin receptor kinase in cancer and the function of TRK inhibitors in the intervention of cancer.
Methods:
Literature research has been accomplished using Google Scholar and databases like ScienceDirect, WOS, PubMed, SciFinder, and Scopus.
Results:
In this review, we provide an overview of the main molecular and functional properties of TRKs and their inhibitors. It also discusses how these advancements have affected the development and use of novel treatments for malignancies and other conditions caused by activated TRKs. Several therapeutic strategies, including the discovery and development of small-molecule TRK inhibitors belonging to various chemical classes and their activity, as well as selectivity towards the receptors, have been discussed in detail.
Conclusion:
This review will help the researchers gain a fundamental understanding of TRKs, how this protein family works, and the ways to create chemical moieties, such as TRK inhibitors, which can serve as tailored therapies for cancer.
Insights
Tropomyosin receptor kinases (TRKs) are vital for cell functions but drive cancer when abnormal. TRK inhibitors offer targeted cancer therapies, though resistance remains a challenge.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Tropomyosin receptor kinases (TRKs) regulate essential cellular processes like growth and metabolism.
- Aberrant TRK signaling is implicated in various cancers, with mutations found in key genes (e.g., MET, HER2, EGFR).
- Therapeutic resistance and feedback loops pose challenges for TRK inhibitor efficacy in cancer treatment.
Approach:
- A comprehensive literature review was conducted using major scientific databases (PubMed, Scopus, Web of Science, etc.).
- The review synthesizes information on TRK molecular properties, functions, and inhibitors.
- Focus is placed on advancements impacting novel cancer treatment development.
Key Points:
- TRK inhibitors represent a targeted approach for malignancies driven by TRK activation.
- Small-molecule inhibitors across diverse chemical classes have been developed with varying selectivity and activity.
- Understanding TRK mechanisms is crucial for overcoming resistance and improving treatment outcomes.
Conclusions:
- This review provides foundational knowledge on TRKs and their inhibitors for cancer research.
- It highlights strategies for developing novel TRK-targeted chemical moieties for personalized cancer therapy.
- Further research into TRK pathways can lead to more effective and tailored cancer treatments.
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