REVIEW article
Front. Pharmacol.
Sec. Experimental Pharmacology and Drug Discovery
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1603950
Progress in Structure-Based Drug Development Targeting Chemokine Receptors
Provisionally accepted
- 1Medical Science and Technology Innovation Center, Shandong First Medical University, Jinan, Shandong Province, China
- 2School of Clinical and Basic Medical Sciences, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, China
- 3Advanced Medical Research Institute, Shandong University, Jinan, Shandong Province, China
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As a critical subfamily of G protein-coupled receptors (GPCRs), chemokine receptors (CCRs) play pivotal regulatory roles in immune cell migration, inflammatory modulation, tissue regeneration, and tumor microenvironment (TME) remodeling. By specifically recognizing chemokine ligands, CCRs orchestrate immune cell trafficking and tissue positioning, with functional dysregulation implicated in infectious diseases, autoimmune disorders, neurodegenerative pathologies, and cancer. These receptors thus represent promising therapeutic targets. Recent breakthroughs in cryo-electron microscopy (cryo-EM) and computational chemistry have enabled high-resolution structural analysis and dynamic conformational modeling of CCRs, establishing a robust foundation for structure-based drug design (SBDD). This review synthesizes current advances in CCR biology, structural mechanisms, disease involvement, and targeted drug development, providing theoretical insights and technical frameworks for future research.
Keywords: GPCR, CCRs, cryo-EM, Drug Discovery, Structure-based drug design (SBDD)
Received: 01 Apr 2025; Accepted: 28 May 2025.
Copyright: © 2025 Wang, Qu, Xiao, Liu, Ping and Sun. 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:
Yu-Qi Ping, Medical Science and Technology Innovation Center, Shandong First Medical University, Jinan, 250117, Shandong Province, China
Jin-Peng Sun, Advanced Medical Research Institute, Shandong University, Jinan, Shandong Province, 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.