| 唐语哲,胡晓东,晁子健,等.CARM1在恶性肿瘤中的作用及靶向治疗研究进展[J].中国肿瘤,2024,33(6):498-507. |
| CARM1在恶性肿瘤中的作用及靶向治疗研究进展 |
| Research Progress on Roles of CARM1 in the Progression of Malignant Tumors and Related Strategies of Targeted Therapy |
| 投稿时间：2023-07-18 |
| DOI：10.11735/j.issn.1004-0242.2024.06.A012 |
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| 中文关键词: 蛋白精氨酸甲基化 辅激活蛋白关联精氨酸甲基转移酶1 恶性肿瘤 靶向治疗 |
| 英文关键词:protein arginine methylation coactivator-associated arginine methyltransferase 1(CARM1) malignant tumor targeted therapy |
| 基金项目:湖北省自然科学基金创新发展联合基金（2022CFD109） |
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| 中文摘要: |
| 摘 要：辅激活蛋白关联精氨酸甲基转移酶1（coactivator-associated arginine methyltransferase 1，CARM1）是一种Ⅰ型蛋白质精氨酸甲基转移酶，可以催化组蛋白和非组蛋白底物的精氨酸残基不对称二甲基化。越来越多的研究发现CARM1在多种类型的恶性肿瘤中表达水平升高并发挥促癌作用。高表达的CARM1可通过多种机制促进肿瘤的发生及进展，例如影响肿瘤免疫、肿瘤代谢、自噬等。因此，CARM1被认为是一个极具潜力的抗肿瘤靶点，已有研究尝试开发靶向CARM1的小分子抑制剂治疗恶性肿瘤。尽管目前利用CARM1抑制剂治疗恶性肿瘤还处于临床前研究阶段，但在体内外试验中已展现出很好的治疗前景。针对CARM1的靶点干预可能为肿瘤治疗提供新策略。全文主要对CARM1的分子结构、肿瘤生物学功能、分子机制以及CARM1特异性抑制剂进行综述。 |
| 英文摘要: |
| Abstract： Coactivator-associated arginine methyltransferase 1（CARM1） is a type Ⅰ protein arginine methyltransferase that catalyzes asymmetric dimethylation of arginine residues on its histone or non-histone substrates. Recent studies have proven that CARM1 is up-regulated in several types of malignant tumors with oncogenic activity. Highly expressed CARM1 promotes tumor progression through various mechanisms， including tumor immunity， tumor metabolism and autophagy. Therefore， CARM1 has been considered as apromising target for cancer therapy， and various small molecule inhibitors targeting CARM1 have been tried to treat malignant tumors. CARM1 inhibitors have shown a good therapeutic prospect in pre-clinical research，suggesting that targeting CARM1 may provide a new strategy for cancer therapy. This paper reviews current advances on roles of CARM1 in cancer progression， focusing on its molecular structure， biological function， molecular mechanism， and specific CARM1 inhibitors in cancer targeted therapy. |
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