FDA-approved small molecule kinase inhibitors for cancer treatment (2001-2015): Medical indication, structural optimization, and binding mode Part I

被引：0

作者：

Wang, Ying ^{[1
]}

Nan, Xiang ^{[2
,3
]}

Duan, Yanping ^{[2
]}

Wang, Qiuxu ^{[3
]}

Liang, Zhigang ^{[3
]}

Yin, Hanrong ^{[1
]}

机构：

[1] Xi An Jiao Tong Univ, Dept Electrophysiol Diag, Hosp 3201, Hlth Sci Ctr, Hanzhong 723000, Peoples R China

[2] Shaanxi Univ Technol, Coll Chem & Environm Sci, Hanzhong 723001, Peoples R China

[3] Shenzhen Second Peoples Hosp, Dept Stomatol, Shenzhen 518035, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2024年 / 111卷

关键词：

Cancer; Protein kinases; Medical indication; Binding mode; Optimization principle; GROWTH-FACTOR RECEPTOR; CELL LUNG-CANCER; CHRONIC MYELOID-LEUKEMIA; PHENYLAMINO-PYRIMIDINE PAP; POTENT ANTITUMOR-ACTIVITY; CYCLIN-DEPENDENT KINASE; BCR-ABL INHIBITOR; TYROSINE KINASE; SELECTIVE INHIBITOR; C-MET;

D O I：

10.1016/j.bmc.2024.117870

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The dysregulation of kinases has emerged as a major class of targets for anticancer drug discovery given its node roles in the etiology of tumorigenesis, progression, invasion, and metastasis of malignancies, which is validated by the FDA approval of 28 small molecule kinase inhibitor (SMKI) drugs for cancer treatment at the end of 2015. While the preclinical and clinical data of these drugs are widely presented, it is highly essential to give an updated review on the medical indications, design principles and binding modes of these anti-tumor SMKIs approved by the FDA to offer insights for the future development of SMKIs with specific efficacy and safety.

引用

页数：37