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 |