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Title of Journal: Amino Acids

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Abbravation: Amino Acids

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Springer Vienna

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DOI

10.1007/bf01604691

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ISSN

1438-2199

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A fluorescence anisotropybased assay for determin

Authors: Christoph Hauser Robert Wodtke Reik Löser Markus Pietsch
Publish Date: 2016/02/17
Volume: 49, Issue: 3, Pages: 567-583
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Abstract

Tissue transglutaminase TGase 2 is the most abundantly expressed enzyme of the transglutaminase family and involved in a large variety of pathological processes such as neurodegenerative diseases disorders related to autoimmunity and inflammation as well as tumor growth progression and metastasis As a result TGase 2 represents an attractive target for drug discovery and development which requires assays that allow for the characterization of modulating agents and are appropriate for highthroughput screening Herein we report a fluorescence anisotropybased approach for the determination of TGase 2’s transamidase activity following the timedependent increase in fluorescence anisotropy due to the enzymecatalyzed incorporation of fluorescein‐ and rhodamine B‐conjugated cadaverines 1–3 acyl acceptor substrates into NNdimethylated casein acyl donor substrate These cadaverine derivatives 1–3 were obtained by solid‐phase synthesis To allow efficient conjugation of the rhodamine B moiety different linkers providing secondary amine functions such as sarcosyl and isonipecotyl were introduced between the cadaverine and xanthenyl entities in compounds 2 and 3 respectively with acyl acceptor 3 showing the most optimal substrate properties of the compounds investigated The assay was validated for the search of both irreversible and reversible TGase 2 inhibitors using the inactivators iodoacetamide and a recently published l‐lysinederived acrylamide and the allosteric binder GTP respectively In addition the fluorescence anisotropybased method was proven to be suitable for highthroughput screening Z′ factor of 086 and represents a nonradioactive and highly sensitive assay for determining the active TGase 2 concentration

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