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Light-assisted small-molecule screening against protein kinases.

ABSTRACT: High-throughput live-cell screens are intricate elements of systems biology studies and drug discovery pipelines. Here, we demonstrate an optogenetics-assisted method that avoids the need for chemical activators and reporters, reduces the number of operational steps and increases information content in a cell-based small-molecule screen against human protein kinases, including an orphan receptor tyrosine kinase. This blueprint for all-optical screening can be adapted to many drug targets and cellular processes.

SUBMITTER: Ingles-Prieto A

PROVIDER: S-EPMC4652335 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature

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Light-assisted small-molecule screening against protein kinases.

Inglés-Prieto Álvaro Á Reichhart Eva E Muellner Markus K MK Nowak Matthias M Nijman Sebastian M B SM Grusch Michael M Janovjak Harald H

Nature chemical biology 20151012 12

High-throughput live-cell screens are intricate elements of systems biology studies and drug discovery pipelines. Here, we demonstrate an optogenetics-assisted method that avoids the need for chemical activators and reporters, reduces the number of operational steps and increases information content in a cell-based small-molecule screen against human protein kinases, including an orphan receptor tyrosine kinase. This blueprint for all-optical screening can be adapted to many drug targets and cel ...[more]

PMID: 26457372

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