灯盏乙素
依替巴肽
化学
药理学
血栓
体内
血小板
心肌梗塞
纤维蛋白原
心脏病学
医学
内科学
生物化学
经皮冠状动脉介入治疗
生物
生物技术
作者
Lancong Liu,Wei Ding,Lili He,Yi Yang,Fuyi Guan,Xinlin Sun,Yan Peng,Xue Chen,Wenhao Zhao,Xiao Yu,Pei Luo
标识
DOI:10.1021/acs.bioconjchem.2c00439
摘要
Myocardial ischemia/reperfusion (MI/R) injury is an unresolved clinical challenge. The blockade of binding fibrinogen by glycoprotein IIb/IIIa (GPIIb–IIIa) inhibitors has become a new therapeutic approach against MI/R injury. In this study, we modified the RGD structure to combine with scutellarin and synthesized a novel peptide, scutellarin–HomoArg–Gly–Asp–Trp–NH2 (WK001). Herein, reported experimental and docking evidence indicates that WK001 provides immediate and potent platelet inhibition, with stronger inhibition of platelet aggregation than eptifibatide and scutellarin. In particular, it is administered intravenously to prevent thrombus formation and attenuate myocardial fibrosis progression in vivo. Therefore, WK001 could be developed as an antiplatelet drug to treat thrombosis-associated diseases, such as stroke and myocardial infarction.
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