CXCR2 的作用不断扩大及其在炎症性疾病和癌症中的治疗潜力。
Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists in inflammatory diseases and cancers.
机构信息
State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China; Institute of Innovative Drug Discovery and Development, China Pharmaceutical University, Nanjing, 211198, China.
State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China; Institute of Innovative Drug Discovery and Development, China Pharmaceutical University, Nanjing, 211198, China.
出版信息
Eur J Med Chem. 2023 Mar 15;250:115175. doi: 10.1016/j.ejmech.2023.115175. Epub 2023 Feb 7.
C-X-C motif chemokine receptor 2 (CXCR2) is G protein-coupled receptor (GPCR) and plays important roles in various inflammatory diseases and cancers, including chronic obstructive pulmonary disease (COPD), atherosclerosis, asthma, and pancreatic cancer. Upregulation of CXCR2 is closely associated with the migration of neutrophils and monocytes. To date, many small-molecule CXCR2 antagonists have entered clinical trials, showing favorable safety and therapeutic effects. Hence, we provide an overview containing the discovery history, protein structure, signaling pathways, biological functions, structure-activity relationships and clinical significance of CXCR2 antagonists in inflammatory diseases and cancers. According to the latest development and recent clinical progress of CXCR2 small molecule antagonists, we speculated that CXCR2 can be used as a biomarker and a new target for diabetes and that CXCR2 antagonists may also attenuate lung injury in coronavirus disease 2019 (COVID-19).
C-X-C 基序趋化因子受体 2（CXCR2）是 G 蛋白偶联受体（GPCR），在各种炎症性疾病和癌症中发挥重要作用，包括慢性阻塞性肺疾病（COPD）、动脉粥样硬化、哮喘和胰腺癌。CXCR2 的上调与中性粒细胞和单核细胞的迁移密切相关。迄今为止，许多小分子 CXCR2 拮抗剂已进入临床试验，显示出良好的安全性和治疗效果。因此，我们提供了一份综述，其中包含 CXCR2 拮抗剂在炎症性疾病和癌症中的发现历史、蛋白质结构、信号通路、生物学功能、构效关系和临床意义。根据 CXCR2 小分子拮抗剂的最新发展和最近的临床进展，我们推测 CXCR2 可以作为糖尿病的生物标志物和新靶点，CXCR2 拮抗剂也可能减轻 2019 冠状病毒病（COVID-19）中的肺损伤。
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