Riboswitches are regions of mRNA to which a metabolite binds in the absence of proteins, resoulting in alteration of transcription, translation or splicing. The most widespread forms of riboswitches are those responsive to TPP (thiamine pyrophosphate) the active form of vitamin B1, thiamine. TPP-riboswitches have been found in all bacterial genomes examined, and are the only ones found in eukaryotes. In each case, the riboswitch appears to regulate the expression of a gene involved in synthesis or uptake of the vitamin. Riboswitches offer an attractive target for chemical intervention, and identification of novel ligands would allow a detailed study on structure–activity relationships, as well as potential leads for the development of antimicrobial compounds. To this end, we have developed a medium-throughput methodology for screening libraries of small molecules using biophysical methods.
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April 2011
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Conference Article|
March 22 2011
Identification of novel ligands for thiamine pyrophosphate (TPP) riboswitches
Elena Cressina;
Elena Cressina
*Department of Plant Sciences, University of Cambridge, Downing Street, Cambridge CB2 3EA, U.K.
†Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 3EW, U.K.
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Liuhong Chen;
Liuhong Chen
†Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 3EW, U.K.
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Michael Moulin;
Michael Moulin
1
*Department of Plant Sciences, University of Cambridge, Downing Street, Cambridge CB2 3EA, U.K.
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Finian J. Leeper;
Finian J. Leeper
†Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 3EW, U.K.
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Chris Abell;
Chris Abell
†Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 3EW, U.K.
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Alison G. Smith
Alison G. Smith
2
*Department of Plant Sciences, University of Cambridge, Downing Street, Cambridge CB2 3EA, U.K.
2To whom correspondence should be addressed (email as25@cam.ac.uk).
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Publisher: Portland Press Ltd
Received:
December 14 2010
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2011 Biochemical Society
2011
Biochem Soc Trans (2011) 39 (2): 652–657.
Article history
Received:
December 14 2010
Citation
Elena Cressina, Liuhong Chen, Michael Moulin, Finian J. Leeper, Chris Abell, Alison G. Smith; Identification of novel ligands for thiamine pyrophosphate (TPP) riboswitches. Biochem Soc Trans 1 April 2011; 39 (2): 652–657. doi: https://doi.org/10.1042/BST0390652
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