Identification of small-molecule inhibitors of Trypansoma cruzi replication.
We report the outcome of a high-throughput small-molecule screen to identify novel, nontoxic, inhibitors of Trypansoma cruzi, as potential starting points for therapeutics to treat for both the acute and chronic stages of Chagas disease. Two compounds were identified that displayed nanomolar inhibition of T. cruzi and an absence of activity against host cells at the highest tested dose. These compounds have been registered with NIH Molecular Libraries Program (probes ML157 and ML158).
Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.
Andrew R
AR
Germain
Leigh C
LC
Carmody
Chris
C
Dockendorff
Cristina
C
Galan-Rodriguez
Ana
A
Rodriguez
Stephen
S
Johnston
Joshua A
JA
Bittker
Lawrence
L
MacPherson
Sivaraman
S
Dandapani
Michelle
M
Palmer
Stuart L
SL
Schreiber
Benito
B
Munoz
D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D054852:Small Molecule Libraries; D014344:Trypanocidal Agents