Targeting secondary protein complexes in drug discovery: studying the druggability and chemical biology of the HSP70/BAG1 complex.
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Date
2017-05-04Author
Evans, LE
Jones, K
Cheeseman, MD
Type
Journal Article
Metadata
Show full item recordAbstract
Proteins typically carry out their biological functions as multi-protein complexes, which can significantly affect the affinity of small-molecule inhibitors. HSP70 is an important target in oncology, so to study its chemical biology and the drug discovery potential of the HSP70/BAG1 complex, we designed a high-affinity non-nucleotide fluorescence polarisation probe.
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Subject
Humans
DNA-Binding Proteins
Transcription Factors
Fluorescent Dyes
Fluorescence Polarization
Molecular Structure
Structure-Activity Relationship
Dose-Response Relationship, Drug
Models, Molecular
HSP70 Heat-Shock Proteins
Small Molecule Libraries
Drug Discovery
Research team
Medicinal Chemistry 3
Language
eng
Date accepted
2017-04-14
License start date
2017-05
Citation
Chemical communications (Cambridge, England), 2017, 53 (37), pp. 5167 - 5170
Publisher
ROYAL SOC CHEMISTRY