探索具有临床潜力的小分子CXCR3配体。
Towards small-molecule CXCR3 ligands with clinical potential.
作者信息
Wijtmans Maikel, Verzijl Dennis, Leurs Rob, de Esch Iwan J P, Smit Martine J
机构信息
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
出版信息
ChemMedChem. 2008 Jun;3(6):861-72. doi: 10.1002/cmdc.200700365.
The CXCR3 chemokine receptor was first discovered in 1996 and has been shown to play an important role in several diseases, most of which are related to inflammation. This review describes in detail the development of small CXCR3 ligands and their therapeutic potential. Classes of CXCR3 antagonists with strikingly variable core structures have emerged. Some of these compounds have confirmed the beneficial role of CXCR3 antagonism in animal models of disease. One of the compounds, AMG487, progressed to Phase II clinical trials but has been withdrawn because of lack of efficacy. New antagonist classes are being developed to reveal the full therapeutic potential of CXCR3.
CXCR3趋化因子受体于1996年首次被发现，已证实在多种疾病中发挥重要作用，其中大多数疾病与炎症相关。本综述详细描述了小型CXCR3配体的发展及其治疗潜力。已出现了核心结构显著不同的几类CXCR3拮抗剂。其中一些化合物已证实CXCR3拮抗作用在疾病动物模型中的有益作用。化合物之一AMG487已进入II期临床试验，但因缺乏疗效而被撤回。正在开发新的拮抗剂类别以揭示CXCR3的全部治疗潜力。
Zotero 插件