Emerging role of G9a in cancer stemness and promises as a therapeutic target
| العنوان: | Emerging role of G9a in cancer stemness and promises as a therapeutic target |
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| المؤلفون: | Joshua R. Haebe, Tamara Sandouka, Christopher J. Bergin, Yannick D. Benoit |
| المصدر: | Oncogenesis, Vol 10, Iss 11, Pp 1-10 (2021) Oncogenesis |
| بيانات النشر: | Springer Science and Business Media LLC, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | Cancer Research, Histone methyltransferase activity, Phenotypic screening, Review Article, Biology, 03 medical and health sciences, 0302 clinical medicine, Cancer stem cell, medicine, Epigenetics, Molecular Biology, RC254-282, 030304 developmental biology, 0303 health sciences, Cancer stem cells, Drug discovery, Neoplasms. Tumors. Oncology. Including cancer and carcinogens, Cancer, medicine.disease, 3. Good health, Chromatin, 030220 oncology & carcinogenesis, Histone methyltransferase, Cancer research |
| الوصف: | The histone methyltransferase G9a is well-documented for its implication in neoplastic growth. However, recent investigations have demonstrated a key involvement of this chromatin writer in maintaining the self-renewal and tumor-initiating capacities of cancer stem cells (CSCs). Direct inhibition of G9a’s catalytic activity was reported as a promising therapeutic target in multiple preclinical studies. Yet, none of the available pharmacological inhibitors of G9a activity have shown success at the early stages of clinical testing. Here, we discuss central findings of oncogenic expression and activation of G9a in CSCs from different origins, as well as the impact of the suppression of G9a histone methyltransferase activity in such contexts. We will explore the challenges posed by direct and systemic inhibition of G9a activity in the perspective of clinical translation of documented small molecules. Finally, we will discuss recent advances in drug discovery as viable strategies to develop context-specific drugs, selectively targeting G9a in CSC populations. |
| تدمد: | 2157-9024 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::682696d1944c10f0dd0a805f67e8f53eTest https://doi.org/10.1038/s41389-021-00370-7Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....682696d1944c10f0dd0a805f67e8f53e |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 21579024 |
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