A fragment-based approach to identifying ligands for riboswitches.
Riboswitches are regions of mRNA that directly bind metabolites, leading to alteration of gene expression. We have developed fragment-based methods to screen for compounds that bind the Escherichia coli thiM riboswitch. Using complementary biophysical techniques we have identified several ligands with K(D) <100 microM. From these there is the potential to develop potent and selective modulators of riboswitch function.
Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K.
Liuhong
L
Chen
Elena
E
Cressina
Finian J
FJ
Leeper
Alison G
AG
Smith
Chris
C
Abell
D001665:Binding Sites; D004926:Escherichia coli / Q000378:metabolism*; D008024:Ligands; D012329:RNA, Bacterial / Q000378:metabolism*; D012333:RNA, Messenger / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry / Q000378:metabolism*
D008024:Ligands; D012329:RNA, Bacterial; D012333:RNA, Messenger; D054852:Small Molecule Libraries