Targeting Bcl-2 with Indole Scaffolds: Emerging Drug Design Strategies for Cancer Treatment.

IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Mini reviews in medicinal chemistry Pub Date : 2024-10-08 DOI:10.2174/0113895575306176240925094457
Pouria Zarrin, Zeynep Ates-Alagoz
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Abstract

The B-cell lymphoma-2 (Bcl-2) protein family plays a crucial role as a regulator in the process of apoptosis. There is a substantial body of evidence indicating that the upregulation of antiapoptotic Bcl-2 proteins is prevalent in several cancer cell lines and original tumour tissue samples. This phenomenon plays a crucial role in enabling tumour cells to avoid apoptosis, hence facilitating the development of resistant cells against chemotherapy. Therefore, the success rate of chemotherapy for cancer can be enhanced by the down-regulation of anti-apoptotic Bcl-2 proteins. Furthermore, the indole structural design is commonly found in a variety of natural substances and biologically active compounds, particularly those that possess anti-cancer properties. Due to its distinctive physicochemical and biological characteristics, it has been highly regarded as a fundamental framework in the development and production of anti-cancer drugs. As a result, a considerable range of indole derivatives, encompassing both naturally occurring and developed compounds, have been identified as potential candidates for the treatment of cancer. Several of these derivatives have advanced to clinical trials, while others are already being used in clinical settings. This emphasizes the significant role of indole in the field of research and development of anti-cancer therapeutics. This study provides an overview of apoptosis and the structural characteristics of Bcl-2 family proteins, and mainly examines the present stage and recent developments in Bcl-2 inhibitors with an indole scaffold embedded in their structure.

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用吲哚支架靶向 Bcl-2:治疗癌症的新兴药物设计策略》。
B 细胞淋巴瘤-2(Bcl-2)蛋白家族在细胞凋亡过程中起着至关重要的调节作用。大量证据表明,在一些癌症细胞系和原始肿瘤组织样本中,抗凋亡 Bcl-2 蛋白的上调非常普遍。这一现象在使肿瘤细胞避免凋亡方面起着至关重要的作用,从而促进了抗化疗细胞的发展。因此,通过下调抗凋亡的 Bcl-2 蛋白,可以提高癌症化疗的成功率。此外,吲哚结构设计常见于各种天然物质和生物活性化合物中,尤其是那些具有抗癌特性的化合物。由于吲哚具有独特的物理化学和生物学特性,它一直被视为开发和生产抗癌药物的基本框架。因此,相当多的吲哚衍生物,包括天然存在的和已开发的化合物,已被确定为治疗癌症的潜在候选药物。其中一些衍生物已进入临床试验阶段,而另一些则已用于临床。这凸显了吲哚在抗癌疗法研发领域的重要作用。本研究概述了细胞凋亡和 Bcl-2 家族蛋白的结构特征,主要考察了在其结构中嵌入吲哚支架的 Bcl-2 抑制剂的现阶段和最新进展。
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来源期刊
CiteScore
7.80
自引率
0.00%
发文量
231
审稿时长
6 months
期刊介绍: The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. Mini-Reviews in Medicinal Chemistry covers all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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