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论文题目: A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor
英文论文题目: A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor
第一作者: Ye, LT; Ding, K; Zhao, F; Liu, XY; Wu, YR; Liu, Y; Xue, DX; Zhou, F; Zhang, XJ; Stevens, RC; Xu, F; Zhao, SW; Tao, HC
英文第一作者: Ye, LT; Ding, K; Zhao, F; Liu, XY; Wu, YR; Liu, Y; Xue, DX; Zhou, F; Zhang, XJ; Stevens, RC; Xu, F; Zhao, SW; Tao, HC
联系作者: Zhao, SW; Tao, HC (reprint author), ShanghaiTech Univ, iHuman Inst, 2F Bldg 6,99 Haike Rd, Shanghai 201210, Peoples R China.
英文联系作者: Zhao, SW; Tao, HC (reprint author), ShanghaiTech Univ, iHuman Inst, 2F Bldg 6,99 Haike Rd, Shanghai 201210, Peoples R China.
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发表年度: 2017
卷: 8
期: 6
页码: 1332-1336
摘要: We present herein a novel dissection-then-evolution strategy for ligand optimization. Using the co-crystal structure of the smoothened receptor (SMO) as a guide, we studied the modular contribution of LY2940680 by systematically "silencing" the specific interaction between the individual residue(s) and the fragment in the ligand. Following evolution by focusing on the benzoyl part finally yielded an improved ligand 21.
英文摘要: We present herein a novel dissection-then-evolution strategy for ligand optimization. Using the co-crystal structure of the smoothened receptor (SMO) as a guide, we studied the modular contribution of LY2940680 by systematically "silencing" the specific interaction between the individual residue(s) and the fragment in the ligand. Following evolution by focusing on the benzoyl part finally yielded an improved ligand 21.
刊物名称: MEDCHEMCOMM
英文刊物名称: MEDCHEMCOMM
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学科: Biochemistry & Molecular Biology; Chemistry, Medicinal
英文学科: Biochemistry & Molecular Biology; Chemistry, Medicinal
影响因子: 2.608
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论文类别: Article
英文论文类别: Article
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