Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations

ZX Wang, QQ Li, J Cai, JZ Wu, JJ Wang… - Journal of Medicinal …, 2024 - ACS Publications
Over the past decades, the role of rearranged during transfection (RET) alterations in
tumorigenesis has been firmly established. RET kinase inhibition is an essential therapeutic …

Revisiting Aurora Kinase B: A promising therapeutic target for cancer therapy

NR Lakkaniga, Z Wang, Y Xiao… - Medicinal Research …, 2024 - Wiley Online Library
Cancer continues to be a major health concern globally, although the advent of targeted
therapy has revolutionized treatment options. Aurora Kinase B is a serine‐threonine kinase …

1-Methyl-3-((4-(quinolin-4-yloxy) phenyl) amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during transfection (RET) kinase inhibitors capable of …

Y Zhang, S Chan, R He, Y Liu, X Song, ZC Tu… - European Journal of …, 2022 - Elsevier
REarranged during Transfection (RET) is a validated target for anticancer drug discovery
and two selective RET inhibitors were approved by US FDA in 2020. However, acquired …

Discovery of 7-(1-methyl-1H-pyrazol-4-yl)-1, 6-naphthyridine derivatives as potent inhibitors of rearranged during transfection (RET) and RET solvent-front mutants for …

J Wu, H Mo, Z An, Z Tang, X Deng, H Zhou… - European Journal of …, 2024 - Elsevier
Rearranged during transfection kinase (RET) inhibition has been considered a promising
therapeutic approach for treatment of a variety of cancers. However, the clinical therapeutic …

QSAR aided design of potent c‐Met inhibitors using molecular docking, molecular dynamics simulation and binding free energy calculation

L Guo, Y Yang, J Tong, Z Chang, P Gao… - Chemistry & …, 2024 - Wiley Online Library
Mesenchymal‐epithelial transition factor (c‐Met) is a tyrosine kinase receptor. Under certain
disease conditions, the cellular transformation process may be over‐activated, resulting in …

Discovery of 9H-pyrimido [4, 5-b] indole derivatives as dual RET/TRKA inhibitors

B Acharya, D Saha, NG Garcia, D Armstrong… - Bioorganic & Medicinal …, 2024 - Elsevier
Aberrant RET kinase signaling is activated in numerous cancers including lung, thyroid,
breast, pancreatic, and prostate. Recent approvals of selective RET inhibitors, pralsetinib …

Kinase Inhibitors and Kinase-Targeted Cancer Therapies: Recent Advances and Future Perspectives

J Li, C Gong, H Zhou, J Liu, X Xia, W Ha… - International Journal of …, 2024 - mdpi.com
Over 120 small-molecule kinase inhibitors (SMKIs) have been approved worldwide for
treating various diseases, with nearly 70 FDA approvals specifically for cancer treatment …

Side Chain Investigation of Imidazopyridazine as a Hinge Binder for Targeting Actionable Mutations of RET Kinase

A Maturi, KNV Sastry, S Kumar, V Pogaku… - ACS Medicinal …, 2024 - ACS Publications
Actionable mutations of RET kinase have been identified as oncogenic drivers of solid
tumors, including thyroid cancer, metastatic colorectal cancer, and nonsmall cell lung …

Recent progress of small-molecule of RET inhibitors against Non-small cell lung cancer

J Shen, L Chen, Y Song, S Chen, W Guo, Y Li - AAPS Open, 2024 - Springer
Since the oncogenic rearranged during transfection (RET) gene fusion was discovered in
non-small cell lung cancer (NSCLC) in 2012, multiple-targeted kinase inhibitors (MKIs) …

Recent Advances on Pyrazole-Pyrimidine/Fused Pyrimidine Hybrids with Anticancer Potential (A Review)

S Wang, S Qian, S Wang, Y Zou - Russian Journal of General Chemistry, 2023 - Springer
Cancer, caused by the failure of the mechanism that controls cell growth and proliferation, is
usually associated with severe health issues. Nowadays, chemotherapy still occupies an …