Using Chemical Epigenetics to Target Cancer
| Autor: | Tingjian Wang, Adam D. Durbin, Logan H. Sigua, Virangika K. Wimalasena, Jun Qi |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Epigenomics
Chemical biology Antineoplastic Agents Computational biology Biology Article Epigenesis Genetic 03 medical and health sciences 0302 clinical medicine Transcription (biology) Neoplasms Animals Humans Epigenetics Molecular Biology Transcription factor 030304 developmental biology 0303 health sciences Effector Cell Biology Chromatin Housekeeping gene Proteolysis Functional genomics 030217 neurology & neurosurgery Transcription Factors |
| Zdroj: | Mol Cell |
| ISSN: | 1097-2765 |
| Popis: | Transcription is epigenetically regulated by the orchestrated function of chromatin-binding proteins that tightly control the expression of master transcription factors, effectors, and supportive housekeeping genes required for establishing and propagating the normal and malignant cell state. Rapid advances in chemical biology and functional genomics have facilitated exploration of targeting epigenetic proteins, yielding effective strategies to target transcription while reducing toxicities to untransformed cells. Here, we review recent developments in conventional active site and allosteric inhibitors, peptidomimetics, and novel proteolysis-targeted chimera (PROTAC) technology that have deepened our understanding of transcriptional processes and led to promising preclinical compounds for therapeutic translation, particularly in cancer. |
| Databáze: | OpenAIRE |
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