Chemistry & biology, 2004-02, Vol.11 (2), p.211-223
2004
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- Autor(en) / Beteiligte
- Titel
- A Three-Hybrid Approach to Scanning the Proteome for Targets of Small Molecule Kinase Inhibitors
- Ist Teil von
- Chemistry & biology, 2004-02, Vol.11 (2), p.211-223
- Ort / Verlag
- United States: Elsevier Ltd
- Erscheinungsjahr
- 2004
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- In this study, we explored the application of a yeast three-hybrid (Y3H)-based compound/protein display system to scanning the proteome for targets of kinase inhibitors. Various known cyclin-dependent kinase (CDK) inhibitors, including purine and indenopyrazole analogs, were displayed in the form of methotrexate-based hybrid ligands and deployed in cDNA library or yeast cell array-based screening formats. For all inhibitors, known cell cycle CDKs as well as novel candidate CDK-like and/or CDK-unrelated kinase targets could be identified, many of which were independently confirmed using secondary enzyme assays and affinity chromatography. The Y3H system described here may prove generally useful in the discovery of candidate drug targets.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1074-5521eISSN: 1879-1301DOI: 10.1016/j.chembiol.2004.02.001Titel-ID: cdi_proquest_miscellaneous_71897662
- Format
- –
- Schlagworte
- Adenine - analogs & derivatives, Adenine - chemistry, Adenine - metabolism, Animals, Binding Sites, CDC2 Protein Kinase - antagonists & inhibitors, CDC2 Protein Kinase - chemistry, CDC2 Protein Kinase - metabolism, Cyclin-Dependent Kinases - antagonists & inhibitors, Cyclin-Dependent Kinases - chemistry, Cyclin-Dependent Kinases - metabolism, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, Ligands, Protein Array Analysis, Proteome - genetics, Saccharomyces - genetics, Two-Hybrid System Techniques