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| | High Throughput Screening Assay for Hsp70 Inhibitors |
| Description: | Burnham Center for Chemical Genomics (BCCG) Burnham Institute for Medical Research (San Diego, CA) NIH Molecular Libraries Screening Centers Network (MLSCN) MLSCN Grant: XO1 MH079863-01 Over-expression of molecular chaperones occurs commonly in cancers and provides protection from a wide variety of cellular stresses, both endogenous and iatrogenic. Molecular chaperones also play important roles in maintaining the activity of several signal-transducing proteins and transcriptions factors involved in malignant transformation. The human genome contains nine Hsp70-family genes. These chaperones include Hsp70 and Hsc70, which are commonly over-expressed in cancers and which confer resistance to myriad cellular stresses, including cytotoxic chemotherapy. This work's aim is to identify chemical probes of Hsp70 through a fluorescence polarization (FP) assay using Fluorescein-labeled ATP. Additional TR-FRET-based assay was developed and utilized as secondary assay in hit confirmation. |
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