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中国临床药理学与治疗学 ›› 2022, Vol. 27 ›› Issue (6): 709-714.doi: 10.12092/j.issn.1009-2501.2022.06.015

• 综述与讲座 • 上一篇    下一篇

以αv为靶向的整合素作为肺纤维化的药物靶点

刘南玉1,岳红梅1,2,宋佩佩1,魏继芳1,魏雅倩1,谢莹莹1,王嘉琪1   

  1. 1兰州大学第一临床医学院,兰州 730000,甘肃;2兰州大学第一医院呼吸内科,兰州 730000,甘肃
  • 收稿日期:2022-04-21 修回日期:2022-05-10 出版日期:2022-06-26 发布日期:2022-07-08
  • 通讯作者: 岳红梅,女,硕士,主任医师,博士生导师,研究方向:呼吸系统疾病。 E-mail: yuehongmei18@sina.com
  • 作者简介:刘南玉,女,硕士,研究方向:特发性肺间质纤维化。 E-mail: liunanyuu@163.com
  • 基金资助:
    甘肃省科技计划项目(18YF1FA106)

Integrins targeting αv are used as drug targets for pulmonary fibrosis

LIU Nanyu1, YUE Hongmei1,2, SONG Peipei1, WEI Jifang1, WEI Yaqian1, XIE Yingying1, WANG Jiaqi1   

  1. 1The First Clinical Medical College of Lanzhou University, Lanzhou 730000, Gansu, China; 2Department of Respiratory Medicine,the First Hospital of Lanzhou University, Lanzhou 730000, Gansu, China
  • Received:2022-04-21 Revised:2022-05-10 Online:2022-06-26 Published:2022-07-08

摘要: 特发性肺纤维化是一种病因不明、预后不良的慢性进行性间质性肺疾病,尽管接受了治疗,大多数患者病情仍有可能进展或恶化。整合素是异二聚体细胞表面蛋白,是干预肺纤维化有希望的治疗靶点。αv整合素是纤维化发展的核心,因为它们激活潜伏的TGF-β,一种已知的促纤维化细胞因子。αv亚基可以与β1、β3、β5、β6或β8亚基形成异二聚体,这些整合素中的一种或多种对于肺纤维化的发展至关重要,但尚不清楚它们的相对重要性。本综述总结了肺纤维化与αv整合素相关联的知识,以及有关αv整合素抑制剂的新出现的临床前研究和临床试验。

关键词: 肺纤维化, αv整合素, TGF-β, αv整合素抑制剂

Abstract: IPF is a chronic progressive interstitial lung disease of unknown etiology and poor prognosis, and despite receive treatment, most patients consideration are likely to progress or worsen. Integrins are heterodimer cell surface proteins that are promising therapeutic targets for intervention in pulmonary fibrosis. Alphav integrins are central to the development of fibrosis because they activate latent TGF-β, a known pro-fibrosis cytokine. The alphav subunit may form heterodimers with the β1, β3, β5, β6, or β8 subunits, one or more of which are essential for the development of pulmonary fibrosis, but their relative importance is unclear. This review summarizes the knowledge of the association of pulmonary fibrosis with alpha-val-integrins, as well as emerging preclinical studies and clinical trials of alpha-fibrosis inhibitors.

Key words: pulmonary fibrosis, alphav integrin, TGF-β, alphav integrin inhibitors

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