Zi-Xuan Wang, Qing-Qing Li, Jiao Cai, Jia-Zhen Wu, Jing-Jing Wang, Meng-Yuan Zhang, Qing-Xin Wang, Zhen-Jiang Tong, Jin Yang, Tian-Hua Wei, Yun Zhou, Wei-Chen Dai, Ning Ding, Xue-Jiao Leng, Shan-Liang Sun, Xin Xue, Yan-Cheng Yu, Ye Yang, Nian-Guang Li, Zhi-Hao Shi
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 target in patients with RET-altered cancers. In clinical practice, initial efficacy can be achieved in patients through the utilization of multikinase inhibitors (MKIs) with RET inhibitory activity. However, the effectiveness of these MKIs is impeded by the adverse events associated with off-target effects. Recently, many RET-selective inhibitors, characterized by heightened specificity and potency, have been developed, representing a substantial breakthrough in the field of RET precision oncology...
March 14, 2024: Journal of Medicinal Chemistry