Li Hongyu, Zhang Qiong, Feng Qinglan, You Qidong, Guo Xiaoke
Jiang Su Key Laboratory of Drug Design and Optimization and Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Drug Discov Today. 2023 Apr;28(4):103513. doi: 10.1016/j.drudis.2023.103513. Epub 2023 Feb 2.
In mammals, N-methyladenosine (mA) is thought to be the most common and conserved mRNA modification. Methyltransferase-like 3 (METTL3) is the primary regulator of mA methyl-transformed modification. Small molecules targeting METTL3 could be effective therapeutics for many disorders, given that a large body of research has linked METTL3 dysregulation with a variety of diseases and altered physiological states, especially with the growth and initiation of cancer. Here, we systematically reviewed the discovery of small molecules targeting METTL3, as well as their future development, for researchers studying in the field.
在哺乳动物中，N-甲基腺苷（mA）被认为是最常见且保守的mRNA修饰。类甲基转移酶3（METTL3）是mA甲基化修饰的主要调节因子。鉴于大量研究已将METTL3失调与多种疾病及生理状态改变，尤其是与癌症的生长和发生联系起来，靶向METTL3的小分子可能是治疗多种疾病的有效药物。在此，我们为该领域的研究人员系统综述了靶向METTL3的小分子的发现及其未来发展。
