Reutershan Jörg
Department of Anesthesiology and Intensive Care Medicine, University Hospital Tübingen, Hoppe-Seyler-Str. 3, 72076 Tübingen, Germany.
Drug News Perspect. 2006 Dec;19(10):615-23. doi: 10.1358/dnp.2006.19.10.1068009.
Emigration of leukocytes from the microcirculation into inflammatory tissues is one of the hallmarks of our immune system. However, excessive leukocyte recruitment can disturb the integrity of the organism and aggravate acute and chronic inflammatory diseases. Chemokines are chemoattractant peptides that are used as messengers to direct leukocytes to sites of inflammation. They mediate their effects through G-protein-coupled chemokine receptors on the surface of leukocytes and other, nonhematopoietic cells, where they induce a variety of cell responses including cell activation and transmigration. CXC chemokine receptor 2 (CXCR2) has been implicated in numerous inflammatory disorders. In many models of acute and chronic inflammatory diseases, blockade of CXCR2 substantially reduces leukocyte recruitment, tissue damage and mortality. The physiological importance of CXCR2 has led to the development of selective CXCR2 inhibitors that are now being tested in clinical trials. This review will summarize current knowledge about CXCR2 in inflammatory diseases and discuss its potential as a pharmaceutical target.
白细胞从微循环迁移至炎症组织是我们免疫系统的标志性特征之一。然而，过度的白细胞募集会破坏机体的完整性，并加重急慢性炎症性疾病。趋化因子是一类化学吸引肽，作为信使引导白细胞至炎症部位。它们通过白细胞和其他非造血细胞表面的G蛋白偶联趋化因子受体介导其作用，在这些细胞上诱导包括细胞活化和迁移在内的多种细胞反应。CXC趋化因子受体2（CXCR2）与多种炎症性疾病有关。在许多急慢性炎症性疾病模型中，阻断CXCR2可显著减少白细胞募集、组织损伤和死亡率。CXCR2的生理重要性促使了选择性CXCR2抑制剂的研发，目前这些抑制剂正在临床试验中进行测试。本综述将总结目前关于CXCR2在炎症性疾病中的知识，并讨论其作为药物靶点的潜力。
