Structure-activity relationships of Wee1 inhibitors: A review
| Autor: | Xiaojiao Luo, Xingkai Du, Feng Li, Li Rong, Yiwen Zhang, Jian Li, Jianyou Shi, Jun He |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Cell cycle checkpoint
Antineoplastic Agents Computational biology P53 Mutation 01 natural sciences 03 medical and health sciences Structure-Activity Relationship Drug Discovery Animals Humans Mitotic catastrophe Protein Kinase Inhibitors 030304 developmental biology Pharmacology 0303 health sciences biology 010405 organic chemistry Kinase Chemistry Organic Chemistry Cell Cycle Rational design General Medicine Cell cycle Protein-Tyrosine Kinases 0104 chemical sciences Wee1 Cancer cell biology.protein |
| Zdroj: | European journal of medicinal chemistry. 203 |
| ISSN: | 1768-3254 |
| Popis: | Wee1 kinase plays an important role in regulating G2/M checkpoint and S phase, and the inhibition of it will lead to mitotic catastrophe in cancer cells with p53 mutation or deletion. Therefore, the mechanism of Wee1 kinase in cancer treatment and the development of its inhibitors have become a research hotspot. However, although a variety of Wee1 inhibitors with different scaffolds and considerable activity have been successfully identified, so far no one has systematically summarized the structure-activity relationships (SARs) of Wee1 inhibitors. Previous reviews mainly focused on its mechanism and clinical application. To facilitate the rational design and development of Wee1 inhibitors in the future, this paper systematically summarizes its structural types, SARs and binding modes according to the Wee1 inhibitors reported in scientific journals, and also summarizes the regulatory effect of Wee1 kinase on cell cycle and the progress of its inhibitors in clinical application. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect