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From the third issue of 2017, Microarrays has changed its name to High-Throughput.

Open AccessArticle
Microarrays 2015, 4(1), 53-63; doi:10.3390/microarrays4010053

Screening of Small Molecule Microarrays for Ligands Targeted to the Extracellular Epitopes of Living Cells

1
Division of Hematology/Oncology, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215, USA
2
Curadel, LLC, 377 Plantation Street, Worcester, MA 01605, USA
3
Department of Cogno-Mechatronics Engineering, Pusan National University, Busan 609-735, Korea
*
Author to whom correspondence should be addressed.
Academic Editor: Ulrich Certa
Received: 3 December 2014 / Accepted: 6 February 2015 / Published: 12 February 2015
View Full-Text   |   Download PDF [1315 KB, uploaded 12 February 2015]   |  

Abstract

The screening of living cells using high-throughput microarrays is technically challenging. Great care must be taken in the chemical presentation of potential ligands and the number of collisions that cells make with them. To overcome these issues, we have developed a glass slide-based microarray system to discover small molecule ligands that preferentially bind to one cell type over another, including when the cells differ by only a single receptor. Chemical spots of 300 ± 10 µm in diameter are conjugated covalently to glass slides using an arraying robot, and novel near-infrared fluorophores with peak emission at 700 nm and 800 nm are used to label two different cell types. By carefully optimizing incubation conditions, including cell density, motion, kinetics, detection, etc. we demonstrate that cell-ligand binding occurs, and that the number of cells bound per chemical spot correlates with ligand affinity and specificity. This screening system lays the foundation for high-throughput discovery of novel ligands to the cell surface. View Full-Text
Keywords: small molecules; high-throughput screening; live cells; microarrays; cell‑based assay; drug discovery small molecules; high-throughput screening; live cells; microarrays; cell‑based assay; drug discovery
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Lee, J.H.; Bao, K.; Frangioni, J.V.; Choi, H.S. Screening of Small Molecule Microarrays for Ligands Targeted to the Extracellular Epitopes of Living Cells. Microarrays 2015, 4, 53-63.

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