REVIEW article
Front. Pharmacol.
Sec. Pharmacology of Anti-Cancer Drugs
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1578342
This article is part of the Research TopicDiscovery of Small Molecule Lead Compounds: a Driving Force to Unravel New Anti-Cancer Targets and Mechanisms - Volume IIIView all 5 articles
Emerging opportunities to treat drug-resistant breast cancer: Discovery of novel small-molecule inhibitors against different targets
Provisionally accepted
- West China Hospital, Sichuan University, Chengdu, China
Select one of your emails
You have multiple emails registered with Frontiers:
Notify me on publication
Please enter your email address:
If you already have an account, please login
You don't have a Frontiers account ? You can register here
Breast cancer is now the most common malignancy among females. Numerous highly effective small-molecule inhibitors, such as tamoxifen and fulvestrant, have received clinical approval, significantly enhancing the therapeutic landscape of breast cancer. However, the emergence of drug resistance in some patients presents an unmet clinical need. Identifying resistance-related targets has been a key therapeutic strategy in combating drug-resistant tumors. Studies investigating the molecular characteristics and resistance mechanisms of breast cancer have unveiled novel targets, including cell cycle checkpoint molecules, breast cancer stem cell-related molecules, and antiapoptotic proteins. Relevant small-molecule inhibitors have shown promising potential in overcoming drug-resistant breast cancer in both preclinical and clinical trials. In this review, we evaluate the resistance mechanisms of available targeted inhibitors for breast cancer and summarize innovative targeted strategies with the potential to overcome resistance, guided by clinical research.
Keywords: breast cancer, Resistance, cell cycle checkpoint, drug design, structure-activity relationships
Received: 17 Feb 2025; Accepted: 13 Aug 2025.
Copyright: © 2025 Chen, Zhou, Meng, Lei, Wang and Wang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Yi Lei, West China Hospital, Sichuan University, Chengdu, China
Yuxi Wang, West China Hospital, Sichuan University, Chengdu, China
Yanyan Wang, West China Hospital, Sichuan University, Chengdu, China
Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.