Design of MHC class II (DR4) ligands using conformationally restricted imino acids at p3 and p5
Design of MHC class II (DR4) ligands using conformationally restricted imino acids at p3 and p5
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DOI：
10.1016/0960-894x(96)00348-4
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发表时间：
1996-08-20
影响因子：
2.7
通讯作者：
Zacheis, ML
中科院分区：
文献类型：
--
作者：
Hanson, GJ;Vuletich, JL;Zacheis, ML
高效合成配体专为类风湿关节炎相关 II 类 MHC、DR4 Dw4 而设计。该设计策略利用p1和p7位置的等排替换以及在暴露于溶剂的残基p3和p5处用亚氨基酸哌啶酸(Pec)和脯氨酸进行构象限制。特别是，SC-67655, (S)-CBA-Val-Pec-Asp-Pro-Thr-NH-n-Pr (IC50 = 50 nM) 是一种有效且稳定的五肽 DR4 配体。版权所有 (C) 1996 爱思唯尔科学有限公司
High potency synthetic ligands were designed for rheumatoid arthritis linked Class II MHC, DR4 Dw4. The design strategy utilized isosteric replacements at the p1 and p7 positions and conformational restriction with imino acids pipecolic acid (Pec) and proline at the solvent exposed residues p3 and p5. In particular, SC-67655, (S)-CBA-Val-Pec-Asp-Pro-Thr-NH-n-Pr (IC50 = 50 nM) is a potent and stable pentapeptide DR4 ligand. Copyright (C) 1996 Elsevier Science Ltd