Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 4, Pages 909-912Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm049137g
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HDM2 binds to an a-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to screen chemical libraries, resulting in the discovery of a novel series of benzodiazepinedione antagonists of the HDM2-p53 interaction. The X-ray crystal structure of improved antagonists bound to HDM2 reveals their a-helix mimetic properties. These optimized molecules increase the transcription of p53 target genes and decrease proliferation of tumor cells expressing wild-type p53.
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