Angewandte Chemie (International ed.), 2013-11, Vol.52 (46), p.12081-12085
2013
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Development of an Activity-Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase-α in Brain
- Ist Teil von
- Angewandte Chemie (International ed.), 2013-11, Vol.52 (46), p.12081-12085
- Ort / Verlag
- Weinheim: WILEY-VCH Verlag
- Erscheinungsjahr
- 2013
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A model method: A strategy that combines a knowledge‐based in silico design approach and the development of novel activity‐based probes (ABPs) for the detection of endogenous diacylglycerol lipase‐α (DAGL‐α) is presented. This approach resulted in the rapid identification of new DAGL‐α inhibitors with high selectivity in the brain proteome. ABPP=activity‐based protein profiling.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1433-7851eISSN: 1521-3773DOI: 10.1002/anie.201306295Titel-ID: cdi_proquest_miscellaneous_1523401906
- Format
- –
- Schlagworte
- activity-based probe, Animals, Arachidonic Acids - metabolism, Binding Sites, Brain - enzymology, Brain - metabolism, Cell Membrane - metabolism, drug discovery, endocannabinoid, Endocannabinoids - metabolism, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - metabolism, Glycerides - metabolism, HEK293 Cells, Humans, hydrolases, Lipoprotein Lipase - antagonists & inhibitors, Lipoprotein Lipase - genetics, Lipoprotein Lipase - metabolism, Mice, Protein Binding, Protein Structure, Tertiary, Proteome, proteomics, Structure-Activity Relationship