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Building Blocks & Bioactive Molecules 전문제조사 ChemScene 수입/공급 업체 코아사이언스 입니다.

 

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Protein arginine methyltransferase 5 (PRMT5) is a major type II arginine methyltransferase that catalyzes the formation of symmetric dimethylarginine in a number of nuclear and cytoplasmic proteins[1]. PRMT5 plays a critical role in regulating biological processes including transcription, cell cycle progression, RNA splicing, and DNA repair. Currently, an increasing number of studies have identified the roles of PRMT5 as a tumor-promoting factor in several cancers. PRMT5 promotes the carcinogenicity of various solid tumors including colon, breast, prostate, lung, liver, bone, ovarian, gastric, and pancreatic cancers with poor clinical outcomes. In recent years, novel inhibitors of the PRMT5/MTA complex have been developed for the treatment of MTAP-deleted cancers. To date, no PRMT5 inhibitors have been approved by FDA and more than fourteen PRMT5 inhibitors have entered into clinical trials[2-10].

A series of building blocks will be used as molecular fragments in the design of PRMT5 inhibitors.

[1] Journal of Medicinal Chemistry (2022), 65, 3, 1749-1766.
[2] Journal of Medicinal Chemistry (2020), 63, 17, 9977-9989.
[3] Journal of Medicinal Chemistry (2021), 64, 7, 3911-3939.
[4] Journal of Medicinal Chemistry (2022), 65, 20, 13793-13812.
[5] Journal of Medicinal Chemistry (2023), 66, 13, 8407-8427.
[6] European Journal of Medicinal Chemistry (2019), 164, 317-333.
[7] European Journal of Medicinal Chemistry (2022), 244, 114842.
[8] Bioorganic & Medicinal Chemistry (2022), 71, 116947.
[9] ACS Medicinal Chemistry Letters (2018), 9, 7, 612-617.
[10] ACS Medicinal Chemistry Letters (2020), 11, 9, 1688-1693.

 

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