Pritz, Stephan, Doering, Klaus, Woelcke, Julian and Hassiepen, Ulrich (2011) Fluorescence Lifetime Assays – Current Advances and Applications in Drug Discovery. Expert Opinion on Drug Discovery, 6 (6). pp. 663-670. ISSN 1746-045X

Abstract

Importance to the field
Currently fluorescence lifetime-based biochemical assays are experiencing a new boost because of the availability of novel dyes and advances in instrumentation. The novel blue-fluorescent dyes with a significantly longer fluorescence lifetime (FLT) than probes used before and with defined mechanisms for fluorescence quenching enable a predictable development of much more robust assays. Fluorescence lifetime-based assays have been successfully introduced recently for finding and characterizing inhibitors of proteases and protein kinases, two mayor enzyme classes of high interest in drug discovery.
Areas to be covered
A comprehensive overview over the recent developments and the latest applications in the field of the fluorescence lifetime assay technology is provided. Current applications of FLT-based assays in drug discovery are reviewed.
What the reader will gain
The reader will gain a broad overview and a deeper understanding of the FLT-based assay technology that was added recently to the portfolio of assay methods established in drug discovery.
Take home message
The fluorescence lifetime technology offers an attractive alternative to existing methods for assaying proteases and protein kinases due to a straight-forward, generic, toolbox-based assay development using single-labeled substrates. Moreover, the technology enables robust identification of compound fluorescence artifacts.

Item Type:	Article
Keywords:	drug discovery, inhibitor, high throughput screening, enzyme, protease, kinase, phosphatase, assay, fluorescence lifetime, compound interference
Date Deposited:	13 Oct 2015 13:15
Last Modified:	13 Oct 2015 13:15
URI:	https://oak.novartis.com/id/eprint/4014