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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.
Bd. 9
(Februar 2014)
Heft 2
.
- S. 183-199.
ISSN 1746-045X
DOI: https://doi.org/10.1517/17460441.2014.875526
Abstract
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.
Weitere Angaben
| Publikationsform: | Artikel in einer Zeitschrift |
|---|---|
| Begutachteter Beitrag: | Ja |
| Zusätzliche Informationen: | PubMed-ID: 24382304 |
| Institutionen der Universität: | Fakultäten > Fakultät für Biologie, Chemie und Geowissenschaften > Fachgruppe Chemie > Lehrstuhl Biochemie > Lehrstuhl Biochemie I - Proteinbiochemie der Signaltransduktion - Univ.-Prof. Dr. Clemens Steegborn Fakultäten Fakultäten > Fakultät für Biologie, Chemie und Geowissenschaften Fakultäten > Fakultät für Biologie, Chemie und Geowissenschaften > Fachgruppe Chemie Fakultäten > Fakultät für Biologie, Chemie und Geowissenschaften > Fachgruppe Chemie > Lehrstuhl Biochemie |
| Titel an der UBT entstanden: | Ja |
| Themengebiete aus DDC: | 500 Naturwissenschaften und Mathematik > 540 Chemie |
| Eingestellt am: | 20 Apr 2015 13:08 |
| Letzte Änderung: | 20 Apr 2015 13:08 |
| URI: | https://eref.uni-bayreuth.de/id/eprint/10426 |