Target-based screening

N. Afeyan, S. A. Martin, G. J. Vella Multidimensional chromatography coupled with mass spectrometry for target-based screening. Mol Diversity 1997, 2, 189-196. 

Hsieh, Y.R Gordon, N. Regnier, R Afeyan, N. Martin, S.A. Vella, G. Multidimensional Chromatography Coupled with Mass Spectrometry for Target-Based Screening, J. Mol. Diversity 2, 189-196 (1997). 

Virtual target-based screening in combinatorial library design enhancing in-vitro and in-vivo hit rates (S. Lindell, Bayer CropScience, Germany)... 

Two other validated targets for antimicrobial chemotherapy will be mentioned here, both of which are defined by pathway inhibition. The earliest antibiotics, the sulfonamides, are inhibitors of the folate biosynthetic pathway (24). Sulfamethoxazole and trimethoprim, targeting dihydropteroate synthase and dihydrofolate reductase, respectively, are each susceptible to rapid emergence of resistance but have been used successfully in combination. Recently, other enzymes in the pathway have begun to engender interest for target-based screening. Fatty acid biosynthesis is another pathway that has previously been... 

Target-based screening, also called the reversed chemical genetics approach, aims to identify small-molecule modulators for a known protein of interest. The identified compounds are then employed to study protein function in cellulo or in vivo. 

Table I lists some of the anti biological and antimetabolite activities of natural products that might be included within the broader definition of "antibiotics." It is clear that in this modem era of mass screening capabilities and target-based screens, new uses for known compounds, as well as the continued discovery and development of new compounds, will continue to expand.

Vottero E, Balgi A, Woods K, Tugendreich S, Melese T, Andersen RJ, Mauk AG, Roberge M (2006) Inhibitors of human indoleamine 2,3-dioxygenase identified with a target-based screen in yeast. Biotechnol J l(3) 282-283... 

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