Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo.

doi:10.1158/1535-7163.MCT-05-0199

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Article

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo.

Molecular cancer therapeutics - 1 Jan 2006

Koblish Holly K, Zhao Shuyuan, Franks Carol F, Donatelli Robert R, Tominovich Rose M, LaFrance Louis V, Leonard Kristi A, Gushue Joan M, Parks Daniel J, Calvo Raul R, Milkiewicz Karen L, Marugán Juan José, Raboisson Pierre, Cummings Maxwell D, Grasberger Bruce L, Johnson Dana L, Lu Tianbao, Molloy Christopher J, Maroney Anna C

Abstract excerpt

The activity and stability of the p53 tumor suppressor are regulated by the human homologue of the mouse double minute 2 (Hdm2) oncoprotein. It has been hypothesized that small molecules disrupting the Hdm2:p53 complex would allow for the activation of p53 and result in growth suppression. We have identified small-molecule inhibitors of the Hdm2:p53 interaction using our proprietary ThermoFluor microcalorimetry...

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PMID: 16432175
DOI: 10.1158/1535-7163.MCT-05-0199

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