Al. Schaefer et al., QUORUM SENSING IN VIBRIO-FISCHERI - PROBING AUTOINDUCER-LUXR INTERACTIONS WITH AUTOINDUCER ANALOGS, Journal of bacteriology, 178(10), 1996, pp. 2897-2901
The Vibrio fischeri luminescence genes are activated by the transcript
ion factor LuxR in combination with a diffusible signal compound, N-(3
-oxohexanoyl) homoserine lactone, termed the autoinducer, We have synt
hesized a set of autoinducer analogs, Many analogs with alterations in
the acyl side chain showed evidence of binding to LuxR. Some appeared
to bind with an affinity similar to that of the autoinducer, but none
showed a higher affinity, and many did not bind as tightly as the aut
oinducer. For the most part, compounds with substitutions in the homos
erine lactone ring did not show evidence of binding to LuxR, The excep
tions were compounds with a homocysteine thiolactone ring in place of
the homoserine lactone ring, Many but not all of the analogs showing e
vidence of LuxR binding had some ability to activate the luminescence
genes, None were as active as the autoinducer, While most showed littl
e ability to induce luminescence, a few analogs with rather conservati
ve substitutions had appreciable activity. Under the conditions we emp
loyed, some of the analogs showing little or no ability to induce lumi
nescence were inhibitors of the autoinducer.