Structure-based design of agents targeting the bacterial ribosome

被引：30

作者：

Bower, J

Drysdale, M

Hebdon, R

Jordan, A

Lentzen, G

Matassova, N

Murchie, A

Powles, J

Roughley, S

机构：

[1] RiboTagets Ltd, Dept Med Chem, Cambridge CB1 6GB, England

[2] RiboTagets Ltd, Dept Bacteriol, Cambridge CB1 6GB, England

[3] RiboTagets Ltd, Dept Screening, Cambridge CB1 6GB, England

[4] RiboTagets Ltd, Dept Assay Dev, Cambridge CB1 6GB, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(03)00495-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Rational structure-based drug design has been applied to the antibiotic thiostrepton, in an attempt to overcome some of its limitations. The identification of a proposed binding fragment allowed construction of a number of key fragments, which were derivatised to generate a library of potential antibiotics. These were then evaluated to determine their ability to bind to the L11 binding domain of the prokaryotic ribosome and inhibit bacterial protein translation. (C) 200 Elsevier Ltd. All rights reserved.

引用

页码：2455 / 2458

页数：4

共 18 条

[1] The complete atomic structure of the large ribosomal subunit at 2.4 Å resolution [J].