源自蛇毒蛋白的抗血栓形成剂。
Anti-thrombotic agents derived from snake venom proteins.
作者信息
Huang Tur-Fu, Hsu Chun-Chieh, Kuo Yu-Ju
机构信息
Institute of Pharmacology, College of Medicine, National Taiwan University, No.1, Sec. 1, Jen-Ai Rd, Taipei, Taiwan.
出版信息
Thromb J. 2016 Oct 4;14(Suppl 1):18. doi: 10.1186/s12959-016-0113-1. eCollection 2016.
Snake venoms affect blood coagulation and platelet function in a complex manner. However, two classes of venom proteins, snaclecs and disintegrins have been shown to specifically target receptors including GPIb, α2β1, GPVI, CLEC-2 and integrins αIIbβ3, αvβ3, α5β1 expressed on platelets, endothelial cells, phagocytes, tumor cells, thus affecting cell-matrices and cell-cell interactions. Here, we focus on disintegrins, a class of low molecular mass Arg-Gly-Asp(RGD)/Lys-Gly-Asp(KGD)-containing, cysteine-rich polypeptide derived from various viper snake venoms. This review describes the potential applications of disintegrins in field of integrin-related diseases, especially arterial thrombosis, angiogenesis, tumor progression and septic inflammation. In addition, a novel RGD-containing disintegrin TMV-7 is being developed as a safer antithrombotic agent with minimal side effects, such as thrombocytopenia and bleeding.
蛇毒以复杂的方式影响血液凝固和血小板功能。然而，两类毒液蛋白，即蛇毒凝集素和去整合素，已被证明可特异性靶向包括血小板、内皮细胞、吞噬细胞、肿瘤细胞上表达的糖蛋白Ib（GPIb）、α2β1、糖蛋白VI（GPVI）、C型凝集素样受体2（CLEC-2）以及整合素αIIbβ3、αvβ3、α5β1等受体，从而影响细胞与基质以及细胞与细胞之间的相互作用。在此，我们聚焦于去整合素，这是一类源自各种蝰蛇毒液的低分子量含精氨酸-甘氨酸-天冬氨酸（RGD）/赖氨酸-甘氨酸-天冬氨酸（KGD）、富含半胱氨酸的多肽。本综述描述了去整合素在整合素相关疾病领域的潜在应用，尤其是动脉血栓形成、血管生成、肿瘤进展和脓毒症炎症。此外，一种新型含RGD的去整合素TMV-7正在被开发为一种副作用最小（如血小板减少和出血）的更安全的抗血栓药物。
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