4.7 Article

Protein Lysine Methyltransferase SMYD2: A Promising Small Molecule Target for Cancer Therapy

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue 15, Pages 10119-10132

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.2c00325

Keywords

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Funding

  1. Science and Technology Program of Zhejiang Province (Key Innovative Team) [2018R01015]
  2. Natural Science Foundation of Zhejiang Provincial [LY19B020008]

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This article reviews the current research status of protein methyltransferase SMYD2 and the development of inhibitors. It evaluates the challenges in this field and provides insights into future directions.
In epigenetic research, the abnormality of protein methylation modification is closely related to the occurrence and development of tumors, which stimulates the interest of researchers in protein methyltransferase research and the efforts to develop corresponding specific small molecule inhibitors. Currently, the protein lysine methyltransferase SMYD2 has been identified as a promising new small molecule target for cancer therapy. But its biological functions have not been fully studied and relatively few inhibitors have been reported, thus this field needs to be further explored. This perspective provides a comprehensive and systematic review of the available resources in this field, including its research status, biological structure, related substrates and methylation mechanisms, and research status of inhibitors. In addition, this perspective elaborates in detail the current challenges in this field, our insights into what needs to be done next, rational drug design of novel SMYD2 inhibitors, and foreseeable development directions in the future.

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