1. Receptor tyrosine kinases and cancer: oncogenic mechanisms and therapeutic approaches
- Author
-
Victoria Wong, Shivanthy Pathmanathan, Anna Lyakisheva, Igor Stagljar, Jamie Snider, and Punit Saraon
- Subjects
0301 basic medicine ,Cancer Research ,medicine.drug_class ,TARGETED PROTEIN-DEGRADATION ,ANTITUMOR-ACTIVITY ,EGFR MUTANTS ,ACTIVATION ,GROWTH ,MET ,RESISTANCE ,INHIBITION ,DRIVEN ,CELLS ,Oncogenic Addiction ,Disease ,Tyrosine-kinase inhibitor ,Receptor tyrosine kinase ,03 medical and health sciences ,0302 clinical medicine ,Cell surface receptor ,Neoplasms ,Genetics ,medicine ,Animals ,Humans ,Molecular Targeted Therapy ,Receptor ,Protein Kinase Inhibitors ,Molecular Biology ,Rtk signaling ,biology ,fungi ,Cancer ,Oncogenes ,medicine.disease ,030104 developmental biology ,030220 oncology & carcinogenesis ,biology.protein ,Cancer research ,Tyrosine - Abstract
Receptor tyrosine kinases (RTKs) are transmembrane receptors of great clinical interest due to their role in disease, notably cancer. Since their discovery, several mechanisms of RTK dysregulation have been identified, resulting in multiple cancer types displaying 'oncogenic addiction' to RTKs. As a result, RTKs have represented a major class for targeted therapeutics over the past two decades, with numerous small molecule-based tyrosine kinase inhibitor (TKI) therapeutics having been developed and clinically approved for several cancers. However, many of the current RTK inhibitor treatments eventually result in the rapid development of acquired resistance and subsequent tumor relapse. Recent technological advances and tools are being generated for the identification of novel RTK small molecule therapeutics. These newer technologies will be important for the identification of diverse types of RTK inhibitors, targeting both the receptors themselves as well as key cellular factors that play important roles in the RTK signaling cascade.
- Published
- 2021