Fine-tuning mGluRs

Osherovich, Lev

doi:10.1038/scibx.2012.3

Science-Business eXchange

2012

DOI: 10.1038/scibx.2012.3

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Fine-tuning mGluRs

Lev Osherovich¹

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2021

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Emerging role of G9a in cancer stemness and promises as a therapeutic target

et al. 2021

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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.

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Emerging role of G9a in cancer stemness and promises as a therapeutic target

et al. 2021

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Fine-tuning mGluRs

Cited by 1 publication

References 4 publications

Emerging role of G9a in cancer stemness and promises as a therapeutic target

Emerging role of G9a in cancer stemness and promises as a therapeutic target

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