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ALDH1A inhibitors: Research advances in cancer therapeutics

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机构： [1]Department of Pulmonary and Critical Care Medicine, Molecularly Targeted Research and Development Laboratory, Institute of Respiratory Health, State Key Laboratory of Respiratory Health and Multimorbidity, Joint Research Institution of Altitude Health, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [2]West China School of Basic Medical Sciences & Forensic Medicine, Sichuan University, Chengdu, 610041, Sichuan, China [3]Department of Dermatology, West China Hospital, Sichuan University, Chengdu, 610041, China [4]Independent Researchers, New Jersey, 08009, USA [5]Department of Biology, University of California San Diego, San Diego, 92037, USA

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关键词： ALDH1A inhibitors Cancer therapy Drug design Structure-activity relationship (SAR) Drug resistance

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Aldehyde dehydrogenase 1A (ALDH1A), a cytosolic enzyme, plays a critical role in tumorigenesis, cancer progression, and therapy resistance by maintaining cancer stem cell properties across various malignancies. Dysregulation of ALDH1A is implicated in the progression of numerous human diseases, including various cancers, metabolic disorders, and neurodegenerative conditions. Consequently, ALDH1A represents a promising therapeutic target, which underscores the urgent need to develop small-molecule inhibitors targeting ALDH1A. In recent years, research groups have developed a series of highly selective and potent ALDH1A inhibitors (e.g., coumarin-based compounds, disulfiram derivatives). These inhibitors have demonstrated significant antitumor efficacy, low cytotoxicity, and favorable pharmacokinetic profiles, which highlights their broad clinical potential. This review summarizes the applications and recent advances of the ALDH1A family in the treatment of various cancers, with a particular focus on the structural optimization and structure-activity relationships (SAR) of small-molecule inhibitors, their mechanisms of action and future development directions. This work is significant for facilitating the clinical translation of novel small-molecule inhibitors and for improving strategies to overcome drug resistance.Copyright © 2025 Elsevier Masson SAS. All rights reserved.

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大类 | 2 区医学

小类 | 1 区药物化学

最新[2025]版：

大类 | 2 区医学

小类 | 1 区药物化学

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第一作者机构： [1]Department of Pulmonary and Critical Care Medicine, Molecularly Targeted Research and Development Laboratory, Institute of Respiratory Health, State Key Laboratory of Respiratory Health and Multimorbidity, Joint Research Institution of Altitude Health, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [2]West China School of Basic Medical Sciences & Forensic Medicine, Sichuan University, Chengdu, 610041, Sichuan, China

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