特发性肺纤维化治疗靶点及药物研究进展
发布时间：2018-11-22 12:25
【摘要】：近年来,对特发性肺纤维化(IPF)发病机制和治疗靶点的研究成为热点。一些细胞因子与IPF关系密切,其中转化生长因子-β(TGF-β)引导成纤维细胞和巨噬细胞至损伤处,直接诱发成纤维细胞转化为肌成纤维细胞并促进胶原合成;血小板源生长因子(PDGF)和碱性纤维母细胞生长因子(b FGF)与成纤维细胞增殖有关。此外,相关蛋白如赖氨酰氧化酶相关蛋白2(LOXL2)、ανβ6整合蛋白和溶血磷脂酸1受体(LPA1)等均为新的IPF治疗靶点。目前针对IPF治疗靶点的药物相继进入临床试验,吡非尼酮(Pirfenidone)为转化生长因子-β(TGF-β)抑制剂;尼达尼布(Nintedanib)为三重酪氨酸激酶抑制剂,作用于PDGF、VEGF和FGF受体;Simtuzumab是一种人源化单克隆抗体,作用于赖氨酰氧化酶相关蛋白2(LOXL2),阻断胶原交联,正处于IPFⅡ期临床试验。STX-100是一种人源化ανβ6特异性单克隆抗体,与ανβ6整合蛋白结合,阻止后者激活TGF-β。
[Abstract]:In recent years, the research on the pathogenesis and therapeutic targets of idiopathic pulmonary fibrosis (IPF) has become a hot topic. Some cytokines are closely related to IPF, among which transforming growth factor- 尾 (TGF- 尾) guides fibroblasts and macrophages to the injured site, directly induces fibroblasts into myofibroblasts and promotes collagen synthesis. Platelet-derived growth factor (PDGF) and basic fibroblast growth factor (b FGF) are associated with fibroblast proliferation. In addition, the related proteins such as lysyl oxidase associated protein 2 (LOXL2), 伪 谓 尾 6 integrin and lysophosphatidic acid 1 receptor (LPA1) are new targets for IPF therapy. At present, the drugs targeted at the target of IPF have entered the clinical trials. Pifenidone (Pirfenidone) is a transforming growth factor- 尾 (TGF- 尾) inhibitor, and NIDNIBE (Nintedanib) is a triple tyrosine kinase inhibitor acting on PDGF,VEGF and FGF receptors. Simtuzumab is a humanized monoclonal antibody acting on lysyl oxidase associated protein 2 (LOXL2), blocking collagen crosslinking, and is in clinical trial stage 鈪，
本文编号：2349369
[Abstract]:In recent years, the research on the pathogenesis and therapeutic targets of idiopathic pulmonary fibrosis (IPF) has become a hot topic. Some cytokines are closely related to IPF, among which transforming growth factor- 尾 (TGF- 尾) guides fibroblasts and macrophages to the injured site, directly induces fibroblasts into myofibroblasts and promotes collagen synthesis. Platelet-derived growth factor (PDGF) and basic fibroblast growth factor (b FGF) are associated with fibroblast proliferation. In addition, the related proteins such as lysyl oxidase associated protein 2 (LOXL2), 伪 谓 尾 6 integrin and lysophosphatidic acid 1 receptor (LPA1) are new targets for IPF therapy. At present, the drugs targeted at the target of IPF have entered the clinical trials. Pifenidone (Pirfenidone) is a transforming growth factor- 尾 (TGF- 尾) inhibitor, and NIDNIBE (Nintedanib) is a triple tyrosine kinase inhibitor acting on PDGF,VEGF and FGF receptors. Simtuzumab is a humanized monoclonal antibody acting on lysyl oxidase associated protein 2 (LOXL2), blocking collagen crosslinking, and is in clinical trial stage 鈪，
本文编号：2349369
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