Photo Credit: Dr. Microbe
The following is a summary of “Small molecule inhibitors targeting m6A regulators,” published in the May 2024 issue of Hematology by Feng et al.
N6 methyladenosine (m6A) modification is a pivotal form of epigenetic regulation within RNA, intricately entwined with fundamental physiological processes such as growth, differentiation, and DNA damage response. In the context of cancer, dysregulated m6A expression catalyzes malignant transformation, fueling tumor proliferation, metastasis, and drug resistance and impacting overall prognosis. This intimate link between m6A and oncogenesis has sparked significant interest, prompting the exploration of small molecule inhibitors targeting m6A regulators as potential therapeutics.
By targeting the epigenetic landscape, these molecules offer precise modulation of RNA modifications, disrupting critical survival mechanisms within tumor cells and presenting a promising avenue for novel cancer treatments. Despite the burgeoning interest in this field, a comprehensive review delineating the landscape of small molecules targeting m6A regulators for anti-tumor purposes is notably absent. This review endeavors to fill this gap by providing an exhaustive overview of m6A regulators, dissecting their intricate involvement in cancer pathogenesis, including proliferation, metastasis, drug resistance, and immune evasion across various malignancies.
Additionally, researchers offer a detailed examination of the development, mechanisms of action, pharmacology, and structure-activity relationships of small molecule inhibitors targeting m6A regulators. By synthesizing this wealth of knowledge, the study group aims to furnish invaluable insights for future drug design and optimization endeavors+- while also delineating prospective directions for the continued development of small molecule-based therapeutics targeting m6A in cancer.
Source: jhoonline.biomedcentral.com/articles/10.1186/s13045-024-01546-5