• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

共激活因子相关精氨酸甲基转移酶1（CARM1）的苯并[d]咪唑抑制剂——从苗头化合物到先导化合物的研究

Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.

作者信息

Wan Honghe, Huynh Tram, Pang Suhong, Geng Jieping, Vaccaro Wayne, Poss Michael A, Trainor George L, Lorenzi Matthew V, Gottardis Marco, Jayaraman Lata, Purandare Ashok V

机构信息

Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, USA.

出版信息

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5063-6. doi: 10.1016/j.bmcl.2009.07.040. Epub 2009 Jul 10.

DOI:10.1016/j.bmcl.2009.07.040
PMID:19632837
Abstract

Hit to Lead optimization and SAR development led to the identification of the potent and selective benzo[d]imidazole inhibitor (17b) of Co-activator Associated Arginine Methyltransferase (CARM1).

摘要

从命中化合物到先导化合物的优化以及构效关系（SAR）研究促成了强效且具选择性的共激活因子相关精氨酸甲基转移酶（CARM1）苯并[d]咪唑抑制剂（17b）的发现。

相似文献

1
Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.共激活因子相关精氨酸甲基转移酶1（CARM1）的苯并[d]咪唑抑制剂——从苗头化合物到先导化合物的研究
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5063-6. doi: 10.1016/j.bmcl.2009.07.040. Epub 2009 Jul 10.
2
Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).共激活因子相关精氨酸甲基转移酶1（CARM1）的吡唑类抑制剂的优化
Bioorg Med Chem Lett. 2009 Jun 1;19(11):2924-7. doi: 10.1016/j.bmcl.2009.04.075. Epub 2009 Apr 22.
3
1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).1,2 - 二胺作为共激活因子相关精氨酸甲基转移酶1（CARM1）的抑制剂
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6725-32. doi: 10.1016/j.bmcl.2009.09.110. Epub 2009 Oct 2.
4
Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.通过基于结构的虚拟筛选和活性分子优化开发的强效、选择性且具有细胞活性的蛋白质精氨酸甲基转移酶5（PRMT5）抑制剂。
J Med Chem. 2017 Jul 27;60(14):6289-6304. doi: 10.1021/acs.jmedchem.7b00587. Epub 2017 Jul 12.
5
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.（2-（苯甲氧基）苯基）甲胺衍生物的开发作为 CARM1 的有效和选择性抑制剂用于治疗黑色素瘤。
J Med Chem. 2024 Apr 25;67(8):6313-6326. doi: 10.1021/acs.jmedchem.3c02265. Epub 2024 Apr 4.
6
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors.基于哌啶和噻唑的组蛋白去乙酰化酶抑制剂的设计与系列合成
Bioorg Med Chem Lett. 2008 Apr 15;18(8):2580-4. doi: 10.1016/j.bmcl.2008.03.041. Epub 2008 Mar 16.
7
Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1).共激活因子相关精氨酸甲基转移酶1（CARM1）的吡唑抑制剂。
Bioorg Med Chem Lett. 2008 Aug 1;18(15):4438-41. doi: 10.1016/j.bmcl.2008.06.026. Epub 2008 Jun 12.
8
Structural Studies Provide New Insights into the Role of Lysine Acetylation on Substrate Recognition by CARM1 and Inform the Design of Potent Peptidomimetic Inhibitors.结构研究为 CARM1 通过赖氨酸乙酰化对底物识别的作用提供了新的见解，并为设计有效的肽模拟抑制剂提供了依据。
Chembiochem. 2021 Dec 10;22(24):3469-3476. doi: 10.1002/cbic.202100506. Epub 2021 Oct 14.
9
Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays.基于虚拟筛选和生物学实验鉴定新型共激活因子相关精氨酸甲基转移酶1抑制剂
Biomed Res Int. 2016;2016:7086390. doi: 10.1155/2016/7086390. Epub 2016 Oct 27.
10
Rational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics*.选择性PRMT4抑制剂的合理设计与合成：癌症治疗药物开发的新化学类型*
ChemMedChem. 2021 Apr 8;16(7):1116-1125. doi: 10.1002/cmdc.202100018. Epub 2021 Mar 4.

引用本文的文献

1
Development of Potent and Selective Coactivator-Associated Arginine Methyltransferase 1 (CARM1) Degraders.强效和选择性共激活因子相关的精氨酸甲基转移酶 1（CARM1）降解剂的开发。
J Med Chem. 2023 Sep 28;66(18):13028-13042. doi: 10.1021/acs.jmedchem.3c00982. Epub 2023 Sep 13.
2
Chemical probes and methods for the study of protein arginine methylation.用于研究蛋白质精氨酸甲基化的化学探针和方法。
RSC Chem Biol. 2023 Jul 28;4(9):647-669. doi: 10.1039/d3cb00018d. eCollection 2023 Aug 30.
3
Discovery and biological evaluation of novel CARM1/HDAC2 dual-targeting inhibitors with anti-prostate cancer agents.
发现并评价新型 CARM1/HDAC2 双重靶向抑制剂作为抗前列腺癌药物。
J Enzyme Inhib Med Chem. 2023 Dec;38(1):2241118. doi: 10.1080/14756366.2023.2241118.
4
Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach.通过解构-重建和碎片生长方法将 I 型蛋白精氨酸甲基转移酶的非选择性抑制剂转化为蛋白精氨酸甲基转移酶 4 的有效且选择性抑制剂。
J Med Chem. 2022 Sep 8;65(17):11574-11606. doi: 10.1021/acs.jmedchem.2c00252. Epub 2022 Apr 28.
5
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.鉴定一种 CARM1 抑制剂，其在多发性骨髓瘤的临床前模型中具有强大的体外和体内活性。
Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z.
6
Recent progress in developing selective inhibitors of protein methyltransferases.蛋白质甲基转移酶选择性抑制剂开发的最新进展。
Curr Opin Chem Biol. 2017 Aug;39:100-108. doi: 10.1016/j.cbpa.2017.06.013. Epub 2017 Jun 26.
7
Inhibitors of Protein Methyltransferases and Demethylases.蛋白质甲基转移酶和去甲基酶抑制剂。
Chem Rev. 2018 Feb 14;118(3):989-1068. doi: 10.1021/acs.chemrev.6b00801. Epub 2017 Mar 24.
8
Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1).共激活因子相关精氨酸甲基转移酶1（CARM1）选择性小分子抑制剂的设计与合成
Medchemcomm. 2016 Sep 1;7(9):1793-1796. doi: 10.1039/C6MD00342G. Epub 2016 Jul 13.
9
Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays.基于虚拟筛选和生物学实验鉴定新型共激活因子相关精氨酸甲基转移酶1抑制剂
Biomed Res Int. 2016;2016:7086390. doi: 10.1155/2016/7086390. Epub 2016 Oct 27.
10
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.蛋白质精氨酸甲基转移酶4和蛋白质精氨酸甲基转移酶6强效、选择性及细胞活性双重抑制剂的发现
J Med Chem. 2016 Oct 13;59(19):9124-9139. doi: 10.1021/acs.jmedchem.6b01033. Epub 2016 Sep 15.