首页> 外国专利> USE OF AN URUSHIOL COMPOUND IN PREPARATION OF PHARMACEUTICAL COMPOSITIONS FOR INHIBITING SMAD3 PHOSPHORYLATION

USE OF AN URUSHIOL COMPOUND IN PREPARATION OF PHARMACEUTICAL COMPOSITIONS FOR INHIBITING SMAD3 PHOSPHORYLATION

机译:乌舒尔油化合物在制备抑制SMAD3磷酸化的药物组合物中的用途

摘要

The invention relates to a use of an urushiol compound (code named GQ-5) in preparation of pharmaceutical compositions for inhibiting Smad3 phosphorylation. We verify that GQ-5 inhibited the interaction of Smad3 with TGF-β type I receptor (TβRI), inhibited subsequent phosphorylation of Smad3, reduced nuclear translocation of Smads complex, and suppressed the transcription of major fibrotic genes such as α-smooth muscle actin (α-SMA), collagen I and fibronectin. Therefore, GQ-5 could be a potent and selective inhibitor of TGF-β1-induced Smad3 phosphorylation, and be used to prepare pharmaceutical compositions for inhibiting Smad3 phosphorylation.
机译:本发明涉及一种漆酚醇化合物(代号GQ-5)在制备用于抑制Smad3磷酸化的药物组合物中的用途。我们证实,GQ-5抑制了Smad3与TGF-βI型受体(TβRI)的相互作用,抑制了Smad3的后续磷酸化,减少了Smads复合体的核易位,并抑制了主要纤维化基因(如α-平滑肌肌动蛋白)的转录(α-SMA),胶原蛋白I和纤连蛋白。因此,GQ-5可以是TGF-β1诱导的Smad3磷酸化的有效和选择性抑制剂,并可以用于制备抑制Smad3磷酸化的药物组合物。

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