Targeting cancer epigenetic pathways with small-molecule compounds: Therapeutic efficacy and combination therapies
| Autor: | Minru Liao, Haixia Huang, Ling-Li Zheng, Qiang Xie, Shiou Zhu, Huidan Tan, Bo Liu, Yi Wang |
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| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
Antineoplastic Agents Computational biology medicine.disease_cause DNA methyltransferase Epigenesis Genetic Histones 03 medical and health sciences 0302 clinical medicine Neoplasms Antineoplastic Combined Chemotherapy Protocols medicine Animals Humans Epigenetics DNA Modification Methylases Pharmacology Histone Acetyltransferases biology Cancer medicine.disease Small molecule 030104 developmental biology Histone Treatment Outcome 030220 oncology & carcinogenesis Histone methyltransferase biology.protein Carcinogenesis |
| Zdroj: | Pharmacological research. 173 |
| ISSN: | 1096-1186 |
| Popis: | Epigenetics mainly refers to covalent modifications to DNA or histones without affecting genomes, which ultimately lead to phenotypic changes in cells or organisms. Given the abundance of regulatory targets in epigenetic pathways and their pivotal roles in tumorigenesis and drug resistance, the development of epigenetic drugs holds a great promise for the current cancer therapy. However, lack of potent, selective, and clinically tractable small-molecule compounds makes the strategy to target cancer epigenetic pathways still challenging. Therefore, this review focuses on epigenetic pathways, small molecule inhibitors targeting DNA methyltransferase (DNMT) and small molecule inhibitors targeting histone modification (the main regulatory targets are histone acetyltransferases (HAT), histone deacetylases (HDACs) and histone methyltransferases (HMTS)), as well as the combination strategies of the existing epigenetic therapeutic drugs and more new therapies to improve the efficacy, which will shed light on a new clue on discovery of more small-molecule drugs targeting cancer epigenetic pathways as promising strategies in the future. |
| Databáze: | OpenAIRE |
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