Design of MHC class II (DR4) ligands using conformationally restricted imino acids at p3 and p5

被引：22

作者：

Hanson, GJ ^{[1
]}

Vuletich, JL ^{[1
]}

Bedell, LJ ^{[1
]}

Bono, CP ^{[1
]}

Howard, SC ^{[1
]}

Welply, JK ^{[1
]}

Woulfe, SL ^{[1
]}

Zacheis, ML ^{[1
]}

机构：

[1] SEARLE RES,CHESTERFIELD,MO 63198

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 16期

关键词：

D O I：

10.1016/0960-894X(96)00348-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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

引用

页码：1931 / 1936

页数：6

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