Small molecule microarrays

For example (a) Small-Molecule Microarrays Covalent Attachment and Screening of Alcohol-Containing Small Molecules on Glass Slides, P. ). Hergenr-OTHER, K. M. Depew, S. L. Schreiber,... 

As we will soon discover, microarray-based technologies have found utility in a number of fields. While DNA arrays are the most technically mature and have the broadest application portfolio, we have witnessed the ever-increasing generation of new kinds of probe arrays antibody, antigen, enzyme, aptamer, carbohydrate, tissue, cell, and small molecule microarrays. The list undoubtedly will continue to expand. We can also describe microarrays in terms of prognostic, diagnostic, and predictive roles. A few examples that examine these applications are provided. 

Kuruvilla EG, Shamji AF, Sternson SM, et al. (2002) Dissecting glucose signalling with diversity-oriented synthesis and small-molecule microarrays. Nature 416 653-657. 

Key Words Peptide microarrays small-molecule microarrays small-molecule immobilization peptide immobilization chemoselective ligation. 

Falsey, J. R., Renil, M., Park, S., Li, S., and Lam, K. S. (2001) Peptide and small molecule microarray for high throughput cell adhesion and functional assays. Bioconjug. Chem. 12, 346-353. 

Winssinger N, Ficarro S, Schultz PG et al (2002) Profiling protein function with small molecule microarrays. Proc Natl Acad Sci USA 99 11139-11144... 

Hegenrother PJ, Depew KM, Schreiber StL (2000) Small-molecule microarrays Covalent attachment and screening of alcohol-containing small molecules on glass slides. J Am Chem Soc 122 7849-7850... 

Lue, R. Y, Zhu, Q., Li, D. (2004). Site-specific peptide immobilization strategies for the rapid detection of kinase activity on microarrays. Site-specific immobilization of biotinylated proteins for protein microarray analysis. Enzymatic profiling system in a small-molecule microarray. Intein-mediated biotinylation of proteins and its application in a protein microarray. Developing site-specific immobilization strategies of peptides in a microarray. Methods Mol. Biol. 278, 191-204. 

Small molecule or peptide substrates can also be used to profile protease and other enzyme activities. Salisbury et al. described a protease-substrate microarray in which the carboxyl end of the peptide substrates was conjugated to 7-amino-4-car-bamoylmethyl coumarin, a fluorogenic compound. The conjugate was non-fluores-cent when the electron-donating group on the coumarin was attached to the peptide. Upon proteolysis, the peptide was released and the microarray spot fluoresced. Zhu et al. demonstrated that small molecule microarrays could be used to detect enzyme activities of epoxide hydrolases and phosphatases. 

Marik J, Lam KS. Peptide and small-molecule microarrays. Methods Mol. Biol. 2005 310 217-226. 

Nenberg DS, Nghiem P, Schreiber SL, Koehler AN. A robust 106. small-molecule microarray platform for screening cell lysates. 

Duffner JL, Clemons PA, Koehler AN. A pipeline for ligand discovery using small-molecule microarrays. Curr. Opin. Chem. 

Urbina HD, Debaene F, Jost B, Bole-Feysot C, Mason DE, Kuzmic P, Harris JL, Winssinger N. Self-assembled small-molecule microarrays for protease screening and profihng. Chem-BioChem. 2006 7 1790-1797. 

Koehler AN, Shamji AF, Schreiber SL. Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis. J. Am. Chem. Soc. 2003 125 8420-8421. 

Barnes-Seeman D, Park SB, Koehler AN, Schreiber SL. Expanding the functional group compatibility of small-molecule microarrays discovery of novel calmodulin ligands. Angew. Chem. Int. Ed. Engl. 2003 42 2376-2379. 

Wang J, Uttamchandani M, Sun LP, Yao SQ. Activity-based high-throughput profiling of metalloprotease inhibitors using small molecule microarrays. Chem. Commun. (Camb). 2006 (7) 717-719. 

---