| Autor: |
Karlsson, Olof, Karlsson, Åsa Frostell, Markova, Natalia, Marcusson, Anders, Weigelt, Johan, Zhukov, Andrei, Bomke, Jörg, Buijs, Jos, Karlsson, Robert |
| Jazyk: |
angličtina |
| Rok vydání: |
2013 |
| Předmět: |
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| Popis: |
Background: X-ray crystallography and NMR give detailed information about protein structure, while functional assays provide information on interaction dynamics. Here, three applications and their relevance to structure function studies are discussed. Identification and characterization of fragments binding to protein targetsSelectivity of inhibitor binding to Poly ADP ribose polymerases (PARPs)Kinetic analysis of drug like compounds binding to stabilized GPCRs Method: Fragment screening on Biacore 4000 system included direct and competitive assays for identification and affinity analysis of specific binders. X-ray crystallography was used for structural analysis. PARP selectivity studies were based on kinetic analysis using Biacore T200 system, while studies on stabilized GPCRs combined kinetic analysis with molecular modeling. Conclusions: Data obtained in these applications suggest an iterative workflow, where interaction analysis and structural methods are used in sequence to identify ligands and to improve the resolution in structure function studies. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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