REVIEW article
Front. Pharmacol.
Sec. Pharmacology of Anti-Cancer Drugs
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1556196
This article is part of the Research TopicReviews in Pharmacology of Anti-Cancer Drugs: 2023View all 9 articles
CXCR3 inhibitors for Therapeutic Interventions: Current status and perspectives
Provisionally accepted
- 1West China Hospital, Sichuan University, Chengdu, Sichuan Province, China
- 2State Key Laboratory of Oral Diseases, West China School of Stomatology, Sichuan University, Chengdu, Sichuan Province, China
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CXC chemokine receptor 3 (CXCR3) is a G protein-coupled chemokine receptor that plays a key role in regulating immune responses and is involved in various pathological processes, particularly in tumor development and inflammatory diseases, making it a novel target for clinical therapy. The expression of CXCR3 and its ligands-CXCL9, CXCL10, CXCL11, CXCL4, and CXCL4L1-is closely associated with the onset and progression of numerous diseases. With a deeper understanding of the mechanisms underlying CXCR3 function, significant progress has been made in the development of small molecule antagonists targeting CXCR3, some of which have entered clinical trials and demonstrated therapeutic potential. This review provides an overview of the structure and signaling pathways of CXCR3, its biological functions in cancer and inflammatory diseases, and highlights the innovative roles of CXCR3 in these diseases. Furthermore, it discusses recent advances in the development of small molecule antagonists, particularly those that have been tested in clinical settings, such as AMG 487 and ACT-777991. These studies provide a scientific foundation for the development of novel CXCR3 antagonists and may offer new directions for future clinical treatments. * CXCR3-related diseases: Includes cancers, inflammatory diseases, autoimmune disorders, neurodegenerative conditions, diabetes, cardiovascular diseases, and transplant rejection.
Keywords: CXCR3, tumor, inflammatory diseases,, CXCR3 inhibitors, molecule antagonists,, future clinical treatments
Received: 06 Jan 2025; Accepted: 23 Jun 2025.
Copyright: © 2025 Zhou, Huo, Jiang, Zhang and Du. 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:
Dan Zhou, West China Hospital, Sichuan University, Chengdu, Sichuan Province, China
Shufang Du, State Key Laboratory of Oral Diseases, West China School of Stomatology, Sichuan University, Chengdu, 610041, Sichuan Province, China
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