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小分子可处理的PARP抑制剂:架构施工方法,机械学的见解和结构活动关系

Amandeep Thakur¹, Mandeep Rana¹, Ritika²

¹School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 110031, Taiwan.

Bioorganic chemistry

|October 2, 2023

概括

药物设计策略已经推进了多ADP-ribose) 聚合酶 (PARP) 抑制剂,重振了它们在癌症治疗中的作用. 本综述详细介绍了这些策略及其对PARP抑制剂开发的影响.

科学领域:

药用化学医学化学
药理学药理学是指药理学的学科.
在瘤学瘤学.

背景情况:

聚基聚合酶 (PARP) 在DNA修复和细胞过程中至关重要.
PARP 抑制剂已成为有前途的癌症治疗药物.
为了开发新的PARP抑制剂,已经采用了各种药物设计方法.

研究的目的:

审查PARPs的生理功能.
讨论FDA批准的PARP抑制剂的药理动力学,药理动力学和相互作用概况.
为了全面覆盖PARP抑制剂和结构-活性关系的药物设计策略.

主要方法:

对PARP抑制剂药物设计策略的文献综述.
分析PARP抑制剂的生理功能,药理动力学和药理动力学.
检查结构-活动关系和生物评估数据.

主要成果:

通过各种设计策略,已经确定了PARP抑制剂的众多有希望的支架.
结构性修改显著影响酶和细胞活动.
生物评估为物理化学性质,ADME和药理学提供了洞察力.

结论:

先进的药物设计策略对开发有效的PARP抑制剂作出了重大贡献.
PARP 抑制剂作为癌症治疗的新承诺.
了解结构-活性关系是优化PARP抑制剂疗效的关键.

关键词:

发生在BRCA突变中的突变.癌症癌症癌症癌症造成的DNA损伤是DNA损伤.分子杂交的分子杂交.在 PARP 抑制剂.脚手架跳跃跳跃跳跃的情况瘤是一个瘤.

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