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在研趋化因子受体抑制剂的现状。

Current status of chemokine receptor inhibitors in development.

机构信息

Dompé s.p.a, Via Campo di Pile, 67100 L'Aquila, Italy.

出版信息

Immunol Lett. 2012 Jul 30;145(1-2):68-78. doi: 10.1016/j.imlet.2012.04.003. Epub 2012 Apr 20.

Abstract

The chemokine network plays pivotal role in a large number of inflammatory, allergic and autoimmune diseases, as well as in the promotion of tumor growth and metastasis. Considerable effort has been put in the pharmaceutical industry to identify therapeutic agents that specifically target chemokine receptors. Despite the fact that several promising programs have proven unsuccessful in Phase II trials the research activity both in academia and industry is still highly intense, whereas for some of the chemokine receptors the progress is still at the preclinical stage. In this review the authors discuss possible reasons beyond successes and failures of early clinical development programs and discuss the most relevant and recent pharmacological approaches with the aim to point out new theories, open issues and expectations in this research field.

摘要

趋化因子网络在大量炎症、过敏和自身免疫性疾病中以及在促进肿瘤生长和转移中发挥关键作用。制药行业已经投入了相当大的努力来识别专门针对趋化因子受体的治疗剂。尽管有几个有前途的项目在 II 期临床试验中被证明是不成功的,但学术界和工业界的研究活动仍然非常活跃,而对于一些趋化因子受体,进展仍处于临床前阶段。在这篇综述中,作者讨论了早期临床开发项目成功和失败之外的可能原因,并讨论了最相关和最近的药理学方法,旨在指出该研究领域的新理论、未解决的问题和期望。

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