以苯并咪唑为基础的小分子作为抗癌剂,靶向端粒 G-四叠体并抑制端粒酶。

IF 3.2 4区 医学 Q3 CHEMISTRY, MEDICINAL
Future medicinal chemistry Pub Date : 2024-01-01 Epub Date: 2024-09-24 DOI:10.1080/17568919.2024.2400982
Hemanathan Elango, Rabindra Nath Das, Abhijit Saha
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引用次数: 0

摘要

端粒对染色体的完整性至关重要,它与衰老和癌症的形成有关,主要是通过调节 G 型四联体结构来实现的。G 型四联体是核酸的二级结构,尤其是在富含鸟嘌呤的 DNA 和 RNA 区域。用小分子化合物靶向这些结构有望选择性地抑制细胞生长,为抗癌治疗提供了新的可能性。要研制出突破性的抗癌药物,就必须对 G-四叠体配体的多种结构形式进行全面研究。最近对使用特定苯并咪唑分子将端粒 DNA 稳定为 G-四联体结构的研究突出表明,它们能够影响癌基因的表达,并显示出对癌细胞的抗增殖特性。本综述介绍了苯并咪唑衍生物,这种衍生物旨在增强 G 型四联结构 DNA 的稳定性,从而抑制端粒酶的活性,在抗癌治疗方面具有广阔的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Benzimidazole-based small molecules as anticancer agents targeting telomeric G-quadruplex and inhibiting telomerase enzyme.

Telomeres, crucial for chromosomal integrity, have been related to aging and cancer formation, mainly through regulating G-quadruplex structures. G-quadruplexes are structural motifs that can arise as secondary structures of nucleic acids, especially in guanine-rich DNA and RNA regions. Targeting these structures by small compounds shows promise in the selective suppression of cell growth, opening up novel possibilities for anticancer treatment. A comprehensive investigation of the many structural forms of G-quadruplex ligands is required to create ground-breaking anticancer drugs. Recent research into using specific benzimidazole molecules in stabilizing telomeric DNA into G-quadruplex structures has highlighted their ability to influence oncogene expression and demonstrate antiproliferative characteristics against cancer cells. This review describes the benzimidazole derivative, designed to enhance the stability of the G-quadruplex structure DNA to suppress the activity of telomerase enzyme, exhibiting promising potential for anticancer therapy.

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来源期刊
Future medicinal chemistry
Future medicinal chemistry CHEMISTRY, MEDICINAL-
CiteScore
5.80
自引率
2.40%
发文量
118
审稿时长
4-8 weeks
期刊介绍: Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.
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