Linked Life Data

21604761

Source:http://linkedlifedata.com/resource/pubmed/id/21604761

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
13
pubmed:dateCreated
2011-7-7
pubmed:databankReference
pubmed:abstractText
The bacterial replisome is a target for the development of new antibiotics to combat drug resistant strains. The ?(2) sliding clamp is an essential component of the replicative machinery, providing a platform for recruitment and function of other replisomal components and ensuring polymerase processivity during DNA replication and repair. A single binding region of the clamp is utilized by its binding partners, which all contain conserved binding motifs. The C-terminal Leu and Phe residues of these motifs are integral to the binding interaction. We acquired three-dimensional structural information on the binding site in ?(2) by a study of the binding of modified peptides. Development of a three-dimensional pharmacophore based on the C-terminal dipeptide of the motif enabled identification of compounds that on further development inhibited ?-?(2) interaction at low micromolar concentrations. We report the crystal structure of the complex containing one of these inhibitors, a biphenyl oxime, bound to ?(2), as a starting point for further inhibitor design.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
14
pubmed:volume
54
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4831-8
pubmed:meshHeading
pubmed:year
2011
pubmed:articleTitle
Binding inhibitors of the bacterial sliding clamp by design.
pubmed:affiliation
CSIRO Livestock Industries, St. Lucia, Queensland 4067, Australia. gene.wijffels@csiro.au
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't