Small molecule screening

Center is unique across the network in having the capability to perform NMR-based small-molecule screening and optimization. NMR-based methods are exceptionally valuable when investigating molecular targets that are not easily tractable by other methods, such as protein-protein interactions and protein targets that cannot be formatted for the classical HTS environment. 

Metz, G. Ottleben, H. Vetter, D. Small molecule screening on chemical microarrays, in Methods and Principles in Medicinal Chemistry Vol. 

Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development... 

David, G. (2005) Covell Linking tumor cell cytotoxicity to mechanism of drug action An integrated analysis of gene expression, small-molecule screening and structural databases. Proteins Structure, Function, and Bioinformatics, 59 (3), 403-433. 

Eggert, U.S. and Mitchison, T.J. 2006. Small molecule screening by imaging. Curr. Opin. Chem. Biol. 10, 232-237. 

T.J. Mitchison, Small-molecule screening and profiling by using automated microscopy, Chem. Bio. Chem., 2005, 6(1), 33. 

Gordon EJ. Small-molecule screening it takes a village. ACS Chem. Biol. 2007 2 9-16. 

Metz G, Ottleben H, Vetter D. Small molecule screening on chemical microarrays. Meth. Princ. Med. Chem. 2003 19 213-236. Ladame S. Dynamic combinatorial chemistry on the road to fulfilling the promise. Org. Biomol. Chem. 2008 6 219-226. Hioki H, Still WC. Chemical evolution a model System that selects and amplifies a receptor for the tripeptide D-Pro-L-Val-D-Val. J. Org. Chem. 1998 63 904-905. 

In many cases, small molecules are found for a TF of interest through assays developed with known protein partners. Structures of the interacting protein domains also have been invaluable for drug discovery. For several important TFs, however, the specific cellular partners with which they interact are unknown. In this case, using small molecule screens on solid supports is an extremely useful tool for dmg discovery. In one such screen, diversity-oriented synthesis (DOS (129) was used to identify a small molecule binder of Hap3p, a yeast protein... 

Zebrafish has been used historically to assess environmental toxicity and is an approved model for aquatic toxicity testing. The small size, chemical permeability, and optical transparency of the zebrafish embryo are also inducive to small molecule screening, and the zebrafish embryo has found application in the area of cardiac toxicity.44 The zebrafish is providing an excellent model to... 

Products/technologies Hand-synthesized small molecule screening libraries for lead generation offer DIVERSet 96 Program, SCREEN-Set Program, CHERRY-Pick Program, and EXPRESS-Pick Program COMBI-... 

Small molecule screening on chemical microarrays. In Bohm, H.J., and Schneider, G. (eds.) Protein-Ligand Interactions, From Molecular Recognition to Drug Design. Wiley-VCH, Weinheim, pp. 213-236. 

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