The evolution of microarrayed compound screening.

This review describes recent developments in the evolutionary process of microarrayed compound screening (microARCS to become a robust and efficient ultra-high-throughput screening technology. Improvements in compound spotting (including new quality-control methods), gel casting and imaging, together with software capable of automatic analysis and deconvolution of images, have helped to streamline the screening process. A variety of screening projects using cell-based and non-cell-based approaches have been successfully concluded using microARCS. Comparison of hits derived from standard microtitre-plate-based screening and from microARCS reveals excellent overlap. Furthermore, there seems to be no bias towards finding compounds within a particular range of logP values, even though compounds are solubilized from a dry state during the course of the assay.

[1]  U. Warrior,et al.  Putting Thought to Paper: A μARCS Protease Screen , 2003 .

[2]  M. Lerner,et al.  Combinatorial diffusion assay used to identify topically active melanocyte-stimulating hormone receptor antagonists. , 1995, Proceedings of the National Academy of Sciences of the United States of America.

[3]  D. Donnelly-roberts,et al.  A cell-based microarrayed compound screening format for identifying agonists of G-protein-coupled receptors. , 2003, Analytical biochemistry.

[4]  W. Patrick Walters,et al.  A guide to drug discovery: Designing screens: how to make your hits a hit , 2003, Nature Reviews Drug Discovery.

[5]  Sarah Cox,et al.  Miniaturization of Fluorescence Polarization Receptor-Binding Assays Using CyDye-Labeled Ligands , 2003, Journal of biomolecular screening.

[6]  Hua Tang,et al.  Studies on Repository Compound Stability in DMSO under Various Conditions , 2003, Journal of biomolecular screening.

[7]  J. Kofron,et al.  Application of Micro Arrayed Compound Screening (pcARCS) to Identify Inhibitors of Caspase-3 , 2002, Journal of biomolecular screening.

[8]  U. Warrior,et al.  Homogeneous Time-Resolved Fluorescence Quenching Assay (LANCE) for Caspase-3 , 2002, Journal of biomolecular screening.

[9]  Sumit K Chanda,et al.  Fulfilling the promise: drug discovery in the post-genomic era. , 2003, Drug discovery today.

[10]  Kit S. Lam,et al.  High-volume cellular screening for anticancer agents with combinatorial chemical libraries: A new methodology , 1996, Molecular Diversity.

[11]  Stephen Ashman,et al.  Single-Molecule Detection Technologies in Miniaturized High-Throughput Screening: Fluorescence Intensity Distribution Analysis , 2003, Journal of biomolecular screening.

[12]  S. Goueli,et al.  From one well to 9000: using high-density streptavidin-coated membranes for kinase detection. , 2002, BioTechniques.

[13]  U. Warrior,et al.  Use of SAM2® Biotin Capture Membrane in Microarrayed Compound Screening (μARCS) Format for Nucleic Acid Polymerization Assays , 2003, Journal of biomolecular screening.

[14]  Julie A. Wilkins,et al.  Utilization of Microarrayed Compound Screening (μARCS) to Identify Inhibitors of p56lck Tyrosine Kinase , 2004, Journal of biomolecular screening.

[15]  J. Kofron,et al.  Microarray Compound Screening (μARCS) to Identify Inhibitors of HIV Integrase , 2002 .

[16]  Bruce A. Beutel,et al.  Well-less, gel-permeation formats for ultra-HTS , 2001 .