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Your search keyword '"Stuckey, Jeanne A."' showing total 10 results
Start Over Author "Stuckey, Jeanne A." Journal cancer research
10 results on '"Stuckey, Jeanne A."'

1. Abstract LB-226: Discovery of small molecule Mcl-1 and Bfl-1 inhibitors

Author

Kump, Karson J., primary, Miao, Lei, additional, Mady, Ahmed A., additional, Ansari, Nurul H., additional, Shrestha, Uttar K., additional, Yang, Yuting, additional, Pal, Mohan, additional, Liao, Chenzhong, additional, Perdih, Andrej, additional, Abulwerdi, Fardokht A., additional, Chinnaswamy, Krishnapriya, additional, Meagher, Jennifer L., additional, Carlson, Jacob M., additional, Khanna, May, additional, Stuckey, Jeanne A., additional, and Nikolovska-Coleska, Zaneta, additional

Published
2020
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2. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer

Author

Bai, Longchuan, primary, Zhou, Bing, additional, Yang, Chao-Yie, additional, Ji, Jiao, additional, McEachern, Donna, additional, Przybranowski, Sally, additional, Jiang, Hui, additional, Hu, Jiantao, additional, Xu, Fuming, additional, Zhao, Yujun, additional, Liu, Liu, additional, Fernandez-Salas, Ester, additional, Xu, Jing, additional, Dou, Yali, additional, Wen, Bo, additional, Sun, Duxin, additional, Meagher, Jennifer, additional, Stuckey, Jeanne, additional, Hayes, Daniel F., additional, Li, Shunqiang, additional, Ellis, Matthew J., additional, and Wang, Shaomeng, additional

Published
2017
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3. SAR405838: An Optimized Inhibitor of MDM2–p53 Interaction That Induces Complete and Durable Tumor Regression

Author

Wang, Shaomeng, primary, Sun, Wei, additional, Zhao, Yujun, additional, McEachern, Donna, additional, Meaux, Isabelle, additional, Barrière, Cédric, additional, Stuckey, Jeanne A., additional, Meagher, Jennifer L., additional, Bai, Longchuan, additional, Liu, Liu, additional, Hoffman-Luca, Cassandra Gianna, additional, Lu, Jianfeng, additional, Shangary, Sanjeev, additional, Yu, Shanghai, additional, Bernard, Denzil, additional, Aguilar, Angelo, additional, Dos-Santos, Odette, additional, Besret, Laurent, additional, Guerif, Stéphane, additional, Pannier, Pascal, additional, Gorge-Bernat, Dimitri, additional, and Debussche, Laurent, additional

Published
2014
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7. Abstract LB-204: Highly potent and optimized small-molecule inhibitors of MDM2 achieve complete tumor regression in animal models of solid tumors and leukemia.

Author

Wang, Shaomeng, primary, Sun, Wei, additional, Yu, Shanghai, additional, Zhao, Yu-jun, additional, Kumar, Sanjeev, additional, McEachern, Donna, additional, Liu, Liu, additional, Bernard, Denzil, additional, Sun, Duxin, additional, Zou, Peng, additional, Li, Xiaqin, additional, Yi, Han, additional, Stuckey, Jeanne, additional, Long, Jianting, additional, Malek, Sami, additional, Yang, Dajun, additional, Kang, Snmao, additional, Guo, Ming, additional, Wood, Brian, additional, Leopold, Lance, additional, Sorensen, Mel, additional, Barriere, Cedric, additional, Meaux, Isabelle, additional, Dos-Santos, Odette, additional, Carry, Jean-christophe, additional, Abecassis, Pierre-yves, additional, Charlier, Anne, additional, Ferey, Vincent, additional, Garciaecheverria, Carlos, additional, Lengauer, Christophe, additional, and Debussche, Laurent, additional

Published
2011
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8. Abstract 4521: Discovery of novel small molecule inhibitors of the antiapoptotic protein Mcl-1 through high-throughput screening approach

Author

Liu, Meilan, primary, Shen, Chenxi, additional, Larsen, Martha, additional, Yang, Chao-Yie, additional, Qiu, Su, additional, Tomita, York, additional, Krajewski, Krzysztof, additional, Roller, Peter P., additional, Stuckey, Jeanne, additional, Wang, Shaomeng, additional, and Nikolovska-Coleska, Zaneta, additional

Published
2010
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9. SM-164: A Novel, Bivalent Smac Mimetic That Induces Apoptosis and Tumor Regression by Concurrent Removal of the Blockade of cIAP-1/2 and XIAP

Author

Lu, Jianfeng, primary, Bai, Longchuan, additional, Sun, Haiying, additional, Nikolovska-Coleska, Zaneta, additional, McEachern, Donna, additional, Qiu, Su, additional, Miller, Rebecca S., additional, Yi, Han, additional, Shangary, Sanjeev, additional, Sun, Yi, additional, Meagher, Jennifer L., additional, Stuckey, Jeanne A., additional, and Wang, Shaomeng, additional

Published
2008
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10. SAR405838: An Optimized Inhibitor of MDM2-p53 Interaction That Induces Complete and Durable Tumor Regression.

Author

Shaomeng Wang, Wei Sun, Yujun Zhao, McEachern, Donna, Meaux, Isabelle, Barrière, Cédric, Stuckey, Jeanne A., Meagher, Jennifer L., Longchuan Bai, Liu Liu, Hoffman-Luca, Cassandra Gianna, Jianfeng Lu, Shangary, Sanjeev, Shanghai Yu, Bernard, Denzil, Aguilar, Angelo, Dos-Santos, Odette, Besret, Laurent, Guerif, Stéphane, and Pannier, Pascal

Subjects
*P53 protein, *PROTEIN-protein interactions, *SPONTANEOUS cancer regression, *LEUKEMIA treatment, *XENOGRAFTS, *APOPTOSIS
Abstract

Blocking the oncoprotein murine double minute 2 (MDM2)-p53 protein-protein interaction has long been considered to offer a broad cancer therapeutic strategy, despite the potential risks of selecting tumors harboring p53 mutations that escape MDM2 control. In this study, we report a novel small-molecule inhibitor of the MDM2-p53 interaction, SAR405838 (MI-77301), that has been advanced into phase I clinical trials. SAR405838 binds to MDM2 with Ki = 0.88 nmol/L and has high specificity over other proteins. A cocrystal structure of the SAR405838:MDM2 complex shows that, in addition to mimicking three key p53 amino acid residues, the inhibitor captures additional interactions not observed in the p53-MDM2 complex and induces refolding of the short, unstructured MDM2 N-terminal region to achieve its high affinity. SAR405838 effectively activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell-cycle arrest and/or apoptosis. At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer, and HCT-116 colon cancer. Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model. Mechanistically, robust transcriptional upregulation of PUMA induced by SAR405838 results in strong apoptosis in tumor tissue, leading to complete tumor regression. Our findings provide a preclinical basis upon which to evaluate SAR405838 as a therapeutic agent in patients whose tumors retain wild-type p53. [ABSTRACT FROM AUTHOR]

Published
2014
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