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Direct Targets Identification of a Bioactive Compound
EP22739
Poster Title: Direct Targets Identification of a Bioactive Compound
Submitted on 26 Feb 2015
Author(s): Sylvain Blanc, Paul Bradley, Marie-Edith Gourdel, Michael Cholay, Gisèle Guimèse, Mike Mckenzie, George Nasi, Jean-Christophe and Barbara Ruggiero
Affiliations: Charnwood Molecular, Hybrigenics services SAS
This poster was presented at Discovery Chemistry Congress
Poster Views: 2,799
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Poster Information
Abstract: ULTImate YChemH is a chemical biology tool for direct targets identification. This method is based on the well-established yeast two-hybrid (Y2H) technology. The small molecule of interest is used as a bait to screen highly complex protein domain libraries. The small molecule - protein interactions are detected thanks to the reconstitution of an active transcription factor from DNA Binding Domain (DBD) and Activation Domain (AD) moieties. When an interaction takes place, the bait derivative bridges the gap between the DBD and the AD. This enables the expression of the reporter gene and subsequent yeast growth on a selective medium. Positive clones are then analyzed by sequencing to identify the protein partnersSummary: Identifying protein partners of a small bioactive molecule is of great
interest in many aspects of life sciences and specifically in the drug
discovery and development process cycle. It is a support to (i) decipher
the mechanism of action after for example a “High Content” screening,
(ii) study “off-target” effects, (iii) adjust therapeutic indications and
clinical regimens of a drug and (iv) consider drug repositioning.
References: 1) C. Chidley, et al. H. Haruki, M. Gronlund Pedersen, E. Muller, K.
Johnsson, A yeast-based screen reveals that sulfazalazine inhibits
tetrahydrobiopterin biosynthesis, Nat. Chem. Biology, 2011, 7, 375-
383
2) S-M. Huang, et al. , Tankirase inhibition stabilizes axin and
antagonizes Wnt signalling, Nature, 2009, 461, 614-620.
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