Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.

Article Details

Citation

Llauger-Bufi L, Felts SJ, Huezo H, Rosen N, Chiosis G

Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3975-8.

PubMed ID
14592488 [ View in PubMed
]
Abstract

Heat shock protein 90 (Hsp90) is a molecular chaperone necessary for maintaining oncogenic transformation. There is substantial interest in developing novel agents that bind to the N-terminal of the chaperone. Here we report the synthesis and characterization of two fluorescent Hsp90 inhibitors and probe their use in an Hsp90 fluorescent polarization assay.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
9-Butyl-8-(3,4,5-Trimethoxybenzyl)-9h-Purin-6-AmineHeat shock protein HSP 90-alphaEC 50 (nM)3200N/AN/ADetails