Structure-based design of agents targeting the bacterial ribosome

Justin Bower; Martin Drysdale; Richard Hebdon; Allan Jordan; Georg Lentzen; Natalia Matassova; Alastair Murchie; Jenifer Powles; Stephen Roughley

Structure-based design of agents targeting the bacterial ribosome

Justin Bower, Martin Drysdale, Richard Hebdon, Allan Jordan, Georg Lentzen, Natalia Matassova, Alastair Murchie, Jenifer Powles, Stephen Roughley

Cancer Research UK Manchester Institute

Research output: Contribution to journal › Article › peer-review

Abstract

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.

Original language	English
Pages (from-to)	2455-8
Number of pages	4
Journal	Bioorg. Med. Chem. Lett.
Volume	13
Issue number	15
Publication status	Published - 4 Aug 2003

Keywords

Anti-Bacterial Agents
Bacteria
Drug Design
Escherichia coli
Indicators and Reagents
Methylation
Microbial Sensitivity Tests
Protein Biosynthesis
RNA, Ribosomal
Ribosomes
Structure-Activity Relationship
Thiostrepton

Cite this

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title = "Structure-based design of agents targeting the bacterial ribosome",

abstract = "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.",

keywords = "Anti-Bacterial Agents, Bacteria, Drug Design, Escherichia coli, Indicators and Reagents, Methylation, Microbial Sensitivity Tests, Protein Biosynthesis, RNA, Ribosomal, Ribosomes, Structure-Activity Relationship, Thiostrepton",

author = "Justin Bower and Martin Drysdale and Richard Hebdon and Allan Jordan and Georg Lentzen and Natalia Matassova and Alastair Murchie and Jenifer Powles and Stephen Roughley",

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TY - JOUR

T1 - Structure-based design of agents targeting the bacterial ribosome

AU - Bower, Justin

AU - Drysdale, Martin

AU - Hebdon, Richard

AU - Jordan, Allan

AU - Lentzen, Georg

AU - Matassova, Natalia

AU - Murchie, Alastair

AU - Powles, Jenifer

AU - Roughley, Stephen

PY - 2003/8/4

Y1 - 2003/8/4

N2 - 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.

AB - 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.

KW - Anti-Bacterial Agents

KW - Bacteria

KW - Drug Design

KW - Escherichia coli

KW - Indicators and Reagents

KW - Methylation

KW - Microbial Sensitivity Tests

KW - Protein Biosynthesis

KW - RNA, Ribosomal

KW - Ribosomes

KW - Structure-Activity Relationship

KW - Thiostrepton

M3 - Article

C2 - 12852942

SN - 0960-894X

VL - 13

SP - 2455

EP - 2458

JO - Bioorg. Med. Chem. Lett.

JF - Bioorg. Med. Chem. Lett.

IS - 15

ER -

Structure-based design of agents targeting the bacterial ribosome

Abstract

Keywords

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