Phytoestrogens and their synthetic analogues as substrate mimic inhibitors of CYP1B1 – An update (2020–2025)

IF 3 3区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Bioorganic & Medicinal Chemistry Pub Date : 2025-09-09 DOI:10.1016/j.bmc.2025.118385

Abanish Biswas, Venkatesan Jayaprakash

{"title":"Phytoestrogens and their synthetic analogues as substrate mimic inhibitors of CYP1B1 – An update (2020–2025)","authors":"Abanish Biswas, Venkatesan Jayaprakash","doi":"10.1016/j.bmc.2025.118385","DOIUrl":null,"url":null,"abstract":"<div><div>Cytochrome P450 enzymes (CYPs) play crucial roles in metabolizing diverse substances, including drugs, pollutants, hormones, and steroids. Among them, CYP1B1 has gained significant attention due to its involvement in cancer initiation, progression, and drug resistance. Overexpression of CYP1B1 is frequently observed in multiple cancers, including breast, lung, colorectal, and brain cancers, making it an important therapeutic target. This review is an update covering the last six years (2019–2025) to our earlier publication proposing linker-based classification. Articles published over this period broadly covers efforts taken to increase the aqueous solubility <span><math><mi>α</mi></math></span>-naphthoflavone derivatives and ability to reverse the resistance to main-stream anticancer agents. We also covered PET tracers and PROTACs designed to hit the CYP1B1 by conjugating appropriate elements to the potent CYP1B1 inhibitors reported earlier. Overall, this review highlights significant recent innovations and strategic advancements in CYP1B1 inhibitor research, offering promising directions for cancer diagnosis and treatment.</div></div>","PeriodicalId":255,"journal":{"name":"Bioorganic & Medicinal Chemistry","volume":"130 ","pages":"Article 118385"},"PeriodicalIF":3.0000,"publicationDate":"2025-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0968089625003268","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}

引用次数: 0

Abstract

Cytochrome P450 enzymes (CYPs) play crucial roles in metabolizing diverse substances, including drugs, pollutants, hormones, and steroids. Among them, CYP1B1 has gained significant attention due to its involvement in cancer initiation, progression, and drug resistance. Overexpression of CYP1B1 is frequently observed in multiple cancers, including breast, lung, colorectal, and brain cancers, making it an important therapeutic target. This review is an update covering the last six years (2019–2025) to our earlier publication proposing linker-based classification. Articles published over this period broadly covers efforts taken to increase the aqueous solubility

α

-naphthoflavone derivatives and ability to reverse the resistance to main-stream anticancer agents. We also covered PET tracers and PROTACs designed to hit the CYP1B1 by conjugating appropriate elements to the potent CYP1B1 inhibitors reported earlier. Overall, this review highlights significant recent innovations and strategic advancements in CYP1B1 inhibitor research, offering promising directions for cancer diagnosis and treatment.

Abstract Image

查看原文本刊更多论文

植物雌激素及其合成类似物作为CYP1B1底物模拟抑制剂-更新（2020-2025）

细胞色素P450酶（CYPs）在多种物质的代谢中起着至关重要的作用，包括药物、污染物、激素和类固醇。其中，CYP1B1因其参与癌症的发生、发展和耐药而备受关注。CYP1B1在乳腺癌、肺癌、结直肠癌和脑癌等多种癌症中经常观察到过表达，使其成为重要的治疗靶点。这篇综述是对我们之前提出的基于链接器的分类的出版物的更新，涵盖了过去六年（2019-2025）。在此期间发表的文章广泛涵盖了提高α-萘黄酮衍生物的水溶性和逆转对主流抗癌药物的耐药性的能力。我们还介绍了PET示踪剂和PROTACs，通过将适当的元件偶联到先前报道的强效CYP1B1抑制剂上来靶向CYP1B1。总体而言，本综述强调了CYP1B1抑制剂研究的重大创新和战略进展，为癌症诊断和治疗提供了有希望的方向。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Bioorganic & Medicinal Chemistry 医学-生化与分子生物学

CiteScore

6.80

自引率

2.90%

发文量

413

审稿时长

17 days

期刊介绍： Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.