De novo design and synthesis of a μ-conotoxin KIIIA peptidomimetic

被引：17

作者：

Brady, Ryan M. ^{[1
,2
]}

Zhang, Minmin ^{[3
]}

Gable, Robert ^{[4
]}

Norton, Raymond S. ^{[2
]}

Baell, Jonathan B. ^{[2
]}

机构：

[1] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3052, Australia

[2] Monash Univ, Monash Inst Pharmaceut Sci, Parkville, Vic 3052, Australia

[3] Univ Utah, Dept Biol, Salt Lake City, UT 84112 USA

[4] Univ Melbourne, Sch Chem, Parkville, Vic 3010, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 17期

基金：

澳大利亚研究理事会;

关键词：

Conotoxin; Peptidomimetic; Sodium channel blocker; KIIIA; Pain; SODIUM-CHANNEL BLOCKERS; NONPEPTIDE MIMETICS; BIOLOGICAL EVALUATION; III MIMETICS; SHK TOXIN; PAIN; GVIA;

D O I：

10.1016/j.bmcl.2013.06.086

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

mu-Conotoxin KIIIA blocks voltage-gated sodium channels and displays potent analgesic activity in mice models for pain. Structure-activity studies with KIIIA have shown that residues important for sodium channel activity are presented on an alpha-helix. Herein, we report the de novo design and synthesis of a three-residue (Lys7, Trp8, His12) peptidomimetic based on a novel diketopiperazine (DKP) carboxamide scaffold. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：4892 / 4895

页数：4

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