张麟, 郝坛义
AuthorsHTML:张麟, 郝坛义
AuthorsListE:Zhang Lin, Hao Tanyi
AuthorsHTMLE:Zhang Lin, Hao Tanyi
Unit:天津大学化工学院，天津 300350
Unit_EngLish:School of Chemical Engineering and Technology, Tianjin University, Tianjin 300350, China
Abstract_Chinese:通过荷电氨基酸残基替换LWWNSYY中的疏水性氨基酸残基W以优化其组成, 设计获得血栓抑制剂LERNSTY．研究发现, LERNSTY溶解度好, 能够有效结合胶原蛋白, K_d为(1.647±0.303)μmol/L, 有效半抑制浓度(IC₅₀)为(2.73±0.48)μg/mL, 优于LWWNSYY．因此, 通过荷电氨基酸的引入优化获得有效的血栓抑制剂LERNSTY, 将促进疗效显著而副作用小的抗血栓药物开发．
Abstract_English:A thrombus inhibitor LERNSTY was designed based on the optimization of LWWNSYY by replacing the hydrophobic amino acid residue W with charged amino acid residues. LERNSTY was found to have good solubility. It could effectively bind with collagen with a K_d of (1.647±0.303) μmol/L. An effective half inhibitory concentration (IC₅₀) of (2.73±0.48) μg/mL was obtained, which was better than that of LWWNSYY. Therefore, an effective thrombus inhibitor LERNSTY was obtained through the introduction of charged amino acid residues, which would facilitate the development of curative antithrombotic drugs with fewer side effects.
Keyword_Chinese:动脉血栓; 胶原蛋白; 血栓抑制剂; 水溶性
Keywords_English:arterial thrombosis; collagen; thrombus inhibitor; solubility

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