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Accession Number ADA566635
Title Screening for Inhibitors of Essential Leishmania Glucose Transporters.
Publication Date Jul 2012
Media Count 11p
Personal Author S. M. Landfear
Abstract The major objective of this project is to identify compounds that function as selective inhibitors of the essential glucose transporters of the parasite Leishmania mexicana. To identify such compounds, a cell growth assay was developed that can be employed in a high-throughput screen (HTS) for such inhibitors. This assay was employed in a scaling screen of the 2000 compound MicroSource Discovery Spectrum Collection and of the approx. 600,000 compound CBT library at St. Jude Children s Research Hospital with a Z-factor of 0.8. This screen yielded approx. 2800 compounds that qualified as hits in the primary screen of the library, i.e. that inhibited growth of the L. mexicana line expressing the major glucose transporter designated LmxGT2 by >65%. These 2800 primary hits were subsequently subjected to a secondary screen in which dose-response curves were performed to asses the ability of each compound to differentially inhibit growth of parasites expressing LmxGT2 versus the human glucose transporter GLUT1. This secondary screen identified 14 compounds that exhibit an IC50 of.
Keywords Cargo vehicles
Cells(Biology)
Compound libraries
Drug development
Fluorescence cell growth assay
Glucose
Growth(Physiology)
High throughput screen
Hts(High throughput screen)
Inhibitors
Leishmania
Leishmania mexicana
Leishmaniasis
Potency
Response(Biology)
Scaling factor
Selective inhibitors of essential parasite glucose transport


 
Source Agency Non Paid ADAS
NTIS Subject Category 57E - Clinical Medicine
57K - Microbiology
Corporate Author Oregon Health and Sciences Univ., Portland.
Document Type Technical report
Title Note Annual rept. 1 Jul 2011-30 Jun 2012.
NTIS Issue Number 1307
Contract Number W81XWH-09-1-0429

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