Recent developments in receptor tyrosine kinase inhibitors: A promising mainstay in targeted cancer therapy.
Cancer
Receptor tyrosine kinases
Targeted therapy
Therapeutic resistance
Tyrosine kinase inhibitors
Journal
Medicine in drug discovery
ISSN: 2590-0986
Titre abrégé: Med Drug Discov
Pays: Netherlands
ID NLM: 101765689
Informations de publication
Date de publication:
Sep 2024
Sep 2024
Historique:
medline:
17
9
2024
pubmed:
17
9
2024
entrez:
16
9
2024
Statut:
ppublish
Résumé
During the past two decades, significant advances have been made in the discovery and development of targeted inhibitors aimed at improving the survival rates of cancer patients. Among the multitude of potential therapeutic targets identified thus far, Receptor Tyrosine Kinases (RTKs) are of particular importance. Dysregulation of RTKs has been implicated in numerous human diseases, particularly cancer, where aberrant signaling pathways contribute to disease progression. RTKs have a profound impact on intra and intercellular communication, and they also facilitate post-translational modifications, notably phosphorylation, which intricately regulates a multitude of cellular processes. Prolonged phosphorylation or the disruption of kinase regulation may lead to significant alterations in cell signaling. The emergence of small molecule kinase inhibitors has revolutionized cancer therapy by offering a targeted and strategic approach that surpasses the efficacy of traditional chemotherapeutic drugs. Over the last two decades, a plethora of targeted inhibitors have been identified or engineered and have undergone clinical evaluation to enhance the survival rates of cancer patients. In this review, we have compared the expression of different RTKs, including Met, KDR/VEGFR2, EGFR, BRAF, BCR, and ALK across different cancer types in TCGA samples. Additionally, we have summarized the recent development of small molecule inhibitors and their potential in treating various malignancies. Lastly, we have discussed the mechanisms of acquired therapeutic resistance with a focus on kinase inhibitors in EGFR mutant and ALK-rearranged non-small cell lung cancer and BCR-ABL positive chronic myeloid leukemia.
Identifiants
pubmed: 39281823
doi: 10.1016/j.medidd.2024.100195
pmc: PMC11393807
pii:
doi:
Types de publication
Journal Article
Langues
eng