Optimization of N-Piperidinyl-Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8-Oxo-Guanine DNA Glycosylase 1,ChemMedChem

当前位置： X-MOL 学术 › ChemMedChem › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Optimization of N-Piperidinyl-Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8-Oxo-Guanine DNA Glycosylase 1
ChemMedChem ( IF 3.6 ) Pub Date : 2022-09-21 , DOI: 10.1002/cmdc.202200310
Olov Wallner ₁ , Armando Cázares-Körner ₁ , Emma Rose Scaletti ₂ , Geoffrey Masuyer ₂ , Tove Bekkhus ₁ , Torkild Visnes _{1,

3} , Kirill Mamonov ₁ , Florian Ortis ₁ , Thomas Lundbäck ₄ , Maria Volkova ₁ , Tobias Koolmeister ₁ , Elisée Wiita ₁ , Olga Loseva ₁ , Monica Pandey ₁ , Evert Homan ₁ , Carlos Benítez-Buelga _{1,

5} , Jonathan Davies ₂ , Martin Scobie _{1,

6} , Ulrika Warpman Berglund _{1,

6} , Christina Kalderén _{1,

6} , Pål Stenmark _{2,

7} , Thomas Helleday _{1,

8} , Maurice Michel ₁

Affiliation

8-Oxoguanine DNA glycosylase 1 (OGG1) excises oxidized guanine from DNA. Besides this role in genomic integrity maintenance, the enzyme has been implicated in transcription processes and as a target to suppress inflammation. Pharmacological modulation of OGG1 has greatly contributed to understand underlying functions of bas excision repair. Here, we report on the discovery and chemical optimization that led to widely used tool compound TH5487.

中文翻译：

N-哌啶基-苯并咪唑酮衍生物作为 8-氧代-鸟嘌呤 DNA 糖基化酶 1 强效选择性抑制剂的优化

8-氧代鸟嘌呤 DNA 糖基化酶 1 (OGG1) 从 DNA 中切除氧化鸟嘌呤。除了在基因组完整性维护中的这一作用外，该酶还参与转录过程并作为抑制炎症的靶标。OGG1 的药理学调节极大地有助于理解 bas 切除修复的潜在功能。在这里，我们报告了导致广泛使用的工具化合物 TH5487 的发现和化学优化。

更新日期：2022-09-21

点击分享查看原文

点击收藏

公开下载

阅读更多本刊最新论文本刊介绍/投稿指南11