Bioconjugates to specifically render inhibitors water-soluble

被引：30

作者：

Hirsch, Anna K. H. ^{[1
]}

Diederich, Francois ^{[1
]}

Antonietti, Markus ^{[2
]}

Boerner, Hans G. ^{[2
]}

机构：

[1] ETH, Organ Chem Lab, HCI, CH-8093 Zurich, Switzerland

[2] Max Planck Inst Colloids & Interfaces, D-14476 Potsdam, Germany

来源：

SOFT MATTER | 2010年 / 6卷 / 01期

基金：

瑞士国家科学基金会;

关键词：

DEOXYXYLULOSE PHOSPHATE-PATHWAY; CATECHOL-O-METHYLTRANSFERASE; ABL TYROSINE KINASE; ISOPRENOID BIOSYNTHESIS; AQUEOUS SOLUBILITY; NONMEVALONATE PATHWAY; POLYMERIC MICELLES; CRYSTAL-STRUCTURE; RATIONAL DESIGN; DRUG;

D O I：

10.1039/b915928b

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

Polymer-peptide conjugates are utilised to render small-molecule inhibitors of the kinase IspE, a promising new antimalarial target, water-soluble. It is shown that the peptide sequence of poly( ethylene oxide)-peptide conjugates can be tailored to mediate specific interactions with the ligands, allowing the solubilisation of even highly challenging inhibitors. This strategy avoids compromising the inhibitor structure to afford water solubility and potentially enables the exploration of a greater structural space of both inhibitors and drugs.

引用

页码：88 / 91

页数：4

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