当前位置：
X-MOL 学术
›
Eur. J. Med. Chem.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-18 , DOI: 10.1016/j.ejmech.2020.112154 Hao Wang 1 , Meiling Chen 2 , Xiaohong Sang 3 , Xuefu You 3 , Yucheng Wang 3 , Ian C Paterson 4 , Wei Hong 2 , Xinyi Yang 3
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-18 , DOI: 10.1016/j.ejmech.2020.112154 Hao Wang 1 , Meiling Chen 2 , Xiaohong Sang 3 , Xuefu You 3 , Yucheng Wang 3 , Ian C Paterson 4 , Wei Hong 2 , Xinyi Yang 3
Affiliation
|
Transforming growth factor-β (TGF-β) is a member of a superfamily of pleiotropic proteins that regulate multiple cellular processes such as growth, development and differentiation. Following binding to type I and II TGF-β serine/threonine kinase receptors, TGF-β activates downstream signaling cascades involving both SMAD-dependent and -independent pathways. Aberrant TGF-β signaling is associated with a variety of diseases, such as fibrosis, cardiovascular disease and cancer. Hence, the TGF-β signaling pathway is recognized as a potential drug target. Various organic molecules have been designed and developed as TGF-β signaling pathway inhibitors and they function by either down-regulating the expression of TGF-β or by inhibiting the kinase activities of the TGF-β receptors. In this review, we discuss the current status of research regarding organic molecules as TGF-β inhibitors, focusing on the biological functions and the binding poses of compounds that are in the market or in the clinical or pre-clinical phases of development.
中文翻译：
针对TGF-β配体和受体的小分子抑制剂的开发：结构，机理，临床前研究和临床应用。
转化生长因子-β（TGF-β）是多效性蛋白超家族的成员，该家族调节多种细胞过程，例如生长，发育和分化。与I型和II型TGF-β丝氨酸/苏氨酸激酶受体结合后，TGF-β激活涉及SMAD依赖性和非依赖性途径的下游信号传导级联反应。TGF-β异常信号转导与多种疾病有关，例如纤维化，心血管疾病和癌症。因此，TGF-β信号通路被认为是潜在的药物靶标。已经设计和开发了多种有机分子作为TGF-β信号通路抑制剂，它们通过下调TGF-β的表达或抑制TGF-β受体的激酶活性发挥作用。在这篇评论中
更新日期：2020-02-20
中文翻译：
针对TGF-β配体和受体的小分子抑制剂的开发：结构，机理，临床前研究和临床应用。
转化生长因子-β（TGF-β）是多效性蛋白超家族的成员，该家族调节多种细胞过程，例如生长，发育和分化。与I型和II型TGF-β丝氨酸/苏氨酸激酶受体结合后，TGF-β激活涉及SMAD依赖性和非依赖性途径的下游信号传导级联反应。TGF-β异常信号转导与多种疾病有关，例如纤维化，心血管疾病和癌症。因此，TGF-β信号通路被认为是潜在的药物靶标。已经设计和开发了多种有机分子作为TGF-β信号通路抑制剂，它们通过下调TGF-β的表达或抑制TGF-β受体的激酶活性发挥作用。在这篇评论中
京公网安备 11010802027423号