Evolution strategy of ROS1 kinase inhibitors for use in cancer therapy
| Autor: | Ruohong Yan, Tingting Zhang, Siming Liu, Jiajie Zhang, Hai-Kui Yang, Ying Jiang |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Drug Lung Neoplasms Pyridines media_common.quotation_subject Cancer therapy Molecular Dynamics Simulation Receptor tyrosine kinase 03 medical and health sciences 0302 clinical medicine Crizotinib Carcinoma Non-Small-Cell Lung Proto-Oncogene Proteins Drug Discovery ROS1 medicine Humans Lung cancer Protein Kinase Inhibitors media_common Pharmacology Binding Sites biology Kinase business.industry Protein-Tyrosine Kinases medicine.disease 030104 developmental biology Lipophilic efficiency Drug Design 030220 oncology & carcinogenesis Cancer research biology.protein Molecular Medicine business medicine.drug |
| Zdroj: | Future Medicinal Chemistry. 10:1705-1720 |
| ISSN: | 1756-8927 1756-8919 |
| DOI: | 10.4155/fmc-2018-0033 |
| Popis: | The abnormal expression of c-ros oncogene1 receptor tyrosine kinase (ROS1) has been identified as clinically actionable oncogenic driver in non-small-cell lung cancer. Since crizotinib was approved by the US FDA for the treatment of advanced ROS1-positive non-small-cell lung cancer, ROS1 kinase has become a promising therapeutic target. Under the guidance of some advanced computer-assisted technologies, such as structure-based drug design, homology modeling and lipophilic efficiency parameters, several potent and selective inhibitors against wild-type and mutant ROS1 were designed and synthesized. In this article, we will review a series of scaffolds targeting ROS1 kinase from the hit-to-drug evolution strategies of their representative compounds and it is hoped that these design strategies would facilitate medicinal chemists to optimize the process of drug design. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|