Issue 50, 2018

Bead-based screening in chemical biology and drug discovery

Abstract

High-throughput screening is an important component of the drug discovery process. The screening of libraries containing hundreds of thousands of compounds requires assays amenable to miniaturisation and automization. Combinatorial chemistry holds a unique promise to deliver structurally diverse libraries for early drug discovery. Among the various library forms, the one-bead-one-compound (OBOC) library, where each bead carries many copies of a single compound, holds the greatest potential for the rapid identification of novel hits against emerging drug targets. However, this potential has not yet been fully realized due to a number of technical obstacles. In this feature article, we review the progress that has been made in bead-based library screening and its application to the discovery of bioactive compounds. We identify the key challenges of this approach and highlight key steps needed for making a greater impact in the field.

Graphical abstract: Bead-based screening in chemical biology and drug discovery

Article information

Article type
Feature Article
Submitted
27 Mas 2018
Accepted
30 Mey 2018
First published
30 Mey 2018

Chem. Commun., 2018,54, 6759-6771

Bead-based screening in chemical biology and drug discovery

V. V. Komnatnyy, T. E. Nielsen and K. Qvortrup, Chem. Commun., 2018, 54, 6759 DOI: 10.1039/C8CC02486C

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