CtBP- an emerging oncogene and novel small molecule drug target: Advances in the understanding of its oncogenic action and identification of therapeutic inhibitors
| Autor: | Benjamin L. Morris, M. Michael Dcona, Keith C. Ellis, Steven R. Grossman |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Cancer Research Epithelial-Mesenchymal Transition Protein Conformation Antineoplastic Agents Apoptosis Review Biology Bioinformatics Metastasis 03 medical and health sciences Cancer stem cell oncogene Neoplasms medicine Animals Humans Epithelial–mesenchymal transition CtBP Molecular Targeted Therapy Wnt Signaling Pathway Pharmacology Oncogene Wnt signaling pathway EMT Cancer corepressor Oncogenes medicine.disease transcriptional co-regulator DNA-Binding Proteins Alcohol Oxidoreductases 030104 developmental biology Oncology Tumor progression dehydrogenase MTOB Cancer research Neoplastic Stem Cells Molecular Medicine HIPP Protein Multimerization Corepressor C-terminal Binding Protein Glycolysis |
| Zdroj: | Cancer Biology & Therapy |
| ISSN: | 1555-8576 1538-4047 |
| Popis: | C-terminal Binding Proteins (CtBP) 1 and 2 are oncogenic transcriptional co-regulators overexpressed in many cancer types, with their expression level correlating to worse prognostic outcomes and aggressive tumor features. CtBP negatively regulates the expression of many tumor suppressor genes, while coactivating genes that promote proliferation, epithelial-mesenchymal transition, and cancer stem cell self-renewal activity. In light of this evidence, the development of novel inhibitors that mitigate CtBP function may provide clinically actionable therapeutic tools. This review article focuses on the progress made in understanding CtBP structure, role in tumor progression, and discovery and development of CtBP inhibitors that target CtBP's dehydrogenase activity and other functions, with a focus on the theory and rationale behind the designs of current inhibitors. We provide insight into the future development and use of rational combination therapy that may further augment the efficacy of CtBP inhibitors, specifically addressing metastasis and cancer stem cell populations within tumors. |
| Databáze: | OpenAIRE |
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