氨酸特异性去甲基酶1 (LSD1) 抑制剂:作为新兴疗法类别的类
Stephin Baby1, Suchita Dattatray Shinde1, Neeraj Kulkarni1
1Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad, Gujarat 380054, India.
ACS chemical biology
|October 9, 2023
概括
异常的氨酸特异性去甲基酶1 (LSD1) 表达驱动疾病,使其成为关键的表观遗传标. 本综述全面整理了基于的LSD1抑制剂,包括H3和SNAIL1衍生物,用于新的治疗策略.
科学领域:
- 表观遗传学 在表观遗传学中,表观遗传学是指表观遗传学.
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
背景情况:
- lysine-specific demethylase 1 (LSD1) 的异常表达与各种疾病有关,尤其是癌症.
- LSD1已经成为治疗干预的重要表观遗传点.
- 基胺启动了LSD1抑制剂的临床实用性,为新药开发奠定了基础.
研究的目的:
- 审查和组织针对LSD1.1的基抑制剂的研究进展.
- 根据设计策略,提供/衍生LSD1抑制剂的综合分类.
- 以突出利用胺抑制剂准LSD1基质结合口袋的机会.
主要方法:
- 关于可逆和不可逆LSD1抑制剂的文献综述.
- 基于的LSD1抑制剂通过设计策略的系统组织.
- 抑制剂的分类为H3,SNAIL1衍生物和各种.
主要成果:
- 识别和分类许多可逆和不可逆的LSD1抑制剂,包括临床候选药物.
- 首次对基于的LSD1抑制剂进行全面组织.
- 通过利用LSD1基质结合口袋来突出抑制剂的潜力.
结论:
- 基于的抑制剂对LSD1向治疗来说是一个有前途的途径.
- 该分类为设计新型LSD1抑制剂提供了战略框架.
- 对/衍生抑制剂的进一步研究可能会导致对LSD1相关疾病的有效治疗.
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