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New assays and approaches for discovery and design of Sirtuin modulators.

Title data

Schutkowski, Mike ; Fischer, Frank ; Roessler, Claudia ; Steegborn, Clemens:
New assays and approaches for discovery and design of Sirtuin modulators.
In: Expert Opinion on Drug Discovery. Vol. 9 (February 2014) Issue 2 . - pp. 183-199.
ISSN 1746-045X
DOI: https://doi.org/10.1517/17460441.2014.875526

Abstract in another language

INTRODUCTION

Sirtuins are an evolutionarily conserved family of NAD(+)-dependent protein lysine deacylases. In mammals, 7 Sirtuin isoforms control various functions in metabolism, stress responses and aging processes. Sirtuins are considered attractive therapeutic targets for metabolic and aging-related diseases, such as metabolic syndrome and neurodegenerative disorders. Extensive development efforts on small-molecule Sirtuin inhibitors and activators have yielded few potent and selective compounds, partly due to shortcomings of available assays and a lack of mechanistic characterization of identified compounds.

AREAS COVERED

The authors describe the developments in analyzing Sirtuin activity and conceptual advances in the identification, improvement and design of Sirtuin-modulating compounds. They also review the application of these methods and concepts for the development and mechanistic characterization of Sirtuin modulators.

EXPERT OPINION

Novel assays and experimental approaches for studying Sirtuin activity have been instrumental for major progress in understanding functions of Sirtuins and how these enzymes can be modulated with drugs. The improved tools and mechanistic insights now enable a more efficient development of Sirtuin modulators for in vivo studies and therapeutic applications.

Further data

Item Type: Article in a journal
Refereed: Yes
Additional notes: PubMed-ID: 24382304
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry > Chair Biochemistry - Univ.-Prof. Dr. Clemens Steegborn
Faculties
Faculties > Faculty of Biology, Chemistry and Earth Sciences
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry
Result of work at the UBT: Yes
DDC Subjects: 500 Science > 540 Chemistry
Date Deposited: 20 Apr 2015 13:08
Last Modified: 20 Apr 2015 13:08
URI: https://eref.uni-bayreuth.de/id/eprint/10426