Screening Chemical Microarrays Methods and

Division of Hematology Oncology, Department of Internal Medicine, UC Davis Cancer Center, University of California Davis, 4501 X Street, Sacramento, CA 95817, USA 

Compounds synthesized in situ, directly on solid support Microarray formats for compounds synthesized in situ Detection methods used for screening Examples of applications 

Photolithographic Glass slide Fluorescence Protein binding 

SPOT synthesis Micro titer plate Colorimetric Label-free optical Cell signaling Enzyme specificity 

Parallel synthesis Peptide/peptoid Electrochemical applications 

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Kumaresan PR, Lam KS (2006) Screening chemical microarrays methods and applications. In Bartlett P, Entzeroth M (eds) Exploiting chemical diversity for drug discovery. RSC, UK, pp 291-312... 

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

This approach is highly efficient, as thousands to hundreds of thousands or even millions of compounds can be generated easily. In this review, we shall briefly discuss the preparation of these chemical microarrays and follow with a more detailed discussion on the various screening methods. Applications of these microarrays to various biological systems will also be described. The approaches that have been employed for preparing microarrays and the methods used to detect activity in different applications are summarized in Table 1. Schematic representations of the generation of planar chemical arrays and bead-arrays are shown in Figure 1. DNA and... 

The OBOC combinatorial library method is highly versatile and economical. It also is a form of chemical microarrays. Many investigators successfully have applied the on-bead screening methods in their research. The solution-phase and cell-based assays for OBOC libraries, however, are much less developed and have been applied successfully in only a few laboratories. A need exists to develop robust methods that allow investigators to screen routinely huge OBOC releasable peptide or chemical libraries (e.g., 200,000 compounds) with multiparametric... 

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