fulltext20 - Luminescent Lanthanide Complexes as Probes for...

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Luminescent Lanthanide Complexes as Probes for the Determination of Enzyme Activities C ORINNA M. S PANGLER ,C HRISTIAN S PANGLER , AND M ICHAEL S CH ¨ AERLING Institute of Analytical Chemistry, Chemo- and Biosensors, University of Regensburg, Regensburg, Germany The determination of enzyme activities and the screening of enzyme regulators is a major task in clinical chemistry and the development of new drugs. A broad variety of enzymatic reactions is associated with the consumption or formation of small molecules like H 2 O 2 , ATP, pyrophosphate, or phosphate. Luminescent lanthanide complexes can be applied to monitor these enzymatic con- versions and therefore can serve as probes for the determination of enzyme activities. The utility of this concept will be demonstrated by means of some selected examples including europium and terbium complexes. Accordingly, this new approach could be already implemented for the determination of glucose oxidase, catalase, and peroxidase activity. In particular, enzymes that catalyze phosphorylation or dephosphorylation reactions came to the fore of interest because of their high relevance as drug targets. These include (protein) kinases, adenylyl cyclases, phospho- diesterases, phosphatases, and ATPases. The development and design of Fuorescent lanthanide complexes should lead to probes with optimized selectivity and response times that can be applied for high-throughput screening of enzyme inhibitors and for real-time monitoring of enzyme kinet- ics. In contrast to other assays for enzyme activity determination, this method does not require the use of radioactively labelled substrates or the accomplishment of rather complex and expensive immunoassays. Key words: lanthanide complexes; probes; Fuorescence; enzyme activity Introduction The use of Fuorescent probes for the determination of enzymatic activity has attracted considerable atten- tion in scienti±c ±elds like biomedical in vivo imaging and pharmaceutical screening. There is a high de- mand for robust but inexpensive screening tools, as inhibitors of enzymes such as protein kinases or pro- teases are candidates for cancer therapy. Because of its great versatility, Fuorescence detection has become the most frequently applied method in drug screening and has clearly displaced assays using radioactively labeled substrates. In a very general perspective, luminescent methods for determination of the activity of enzymes can be classi±ed in these categories: (a) ²luorogenic enzyme substrates (b) Substrates bearing a ²¨orster resonance energy transfer (²RET) donor/acceptor system (c) Immunological assays Address for correspondence: Michael Sch¨aerling, Institute for Analyt- ical Chemistry, Chemo- and Biosensors, University of Regensburg, D- 93040 Regensburg, Germany. Voice: + 49-941-94340xx; fax: + 49-941- 9434066.
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This note was uploaded on 07/11/2010 for the course SPECTOGRAP 545 taught by Professor Gdf during the Spring '10 term at AIB College of Business.

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fulltext20 - Luminescent Lanthanide Complexes as Probes for...

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