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癌症药物研发中针对转录因子的研究

Targeting transcription factors in cancer drug discovery.

作者信息

Mitra Partha

机构信息

Institute of Health and Biomedical Innovation, the Queensland University of Technology, Brisbane 4059, Australia.

出版信息

Explor Target Antitumor Ther. 2020;1(6):401-412. doi: 10.37349/etat.2020.00025. Epub 2020 Dec 28.

DOI:10.37349/etat.2020.00025
PMID:36046384
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9402400/
Abstract

Cancer drug discovery is currently dominated by clinical trials or clinical research. Several potential drug candidates have been brought into the pipeline of drug discovery after showing very promising results at the pre-clinical level and are waiting to be tested in human clinical trials. Interestingly, among the potential drug candidates, a few of them have targeted transcription factors highlighting the fundamental undruggable nature of these molecules. However, using advanced technologies, researchers were recently successful in partly unlocking this undruggable nature, which was considered as a 'grey area' in the early days of drug discovery, and as a result, several potential candidates have emerged recently. The purpose of the review is to highlight some of the recently reported studies of targeting transcription factors in cancer and their promising outcomes.

摘要

癌症药物研发目前主要由临床试验或临床研究主导。一些潜在的候选药物在临床前阶段显示出非常有前景的结果后,已进入药物研发流程,正等待在人体临床试验中进行测试。有趣的是,在潜在的候选药物中,有一些靶向转录因子,凸显了这些分子基本的不可成药特性。然而,利用先进技术,研究人员最近成功地部分破解了这种不可成药特性,这在药物研发早期被视为一个“灰色地带”,结果最近出现了一些潜在的候选药物。本综述的目的是强调最近一些关于在癌症中靶向转录因子的研究及其有前景的成果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/543d/9402400/af06a4679a01/etat-01-100225-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/543d/9402400/f6842a17c742/etat-01-100225-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/543d/9402400/af06a4679a01/etat-01-100225-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/543d/9402400/f6842a17c742/etat-01-100225-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/543d/9402400/af06a4679a01/etat-01-100225-g002.jpg

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2
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Nat Commun. 2020 Apr 14;11(1):1833. doi: 10.1038/s41467-020-15290-0.
3
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4
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Cancers (Basel). 2023 Jun 25;15(13):3338. doi: 10.3390/cancers15133338.
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Front Chem. 2019 Dec 10;7:849. doi: 10.3389/fchem.2019.00849. eCollection 2019.
4
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