McEachern, Donna

Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition

Shangary, S., Qin, D., McEachern, D., Liu, M., Miller, R. S., Qiu, S., Nikolovska-Coleska, Z., Ding, K., Wang, G., Chen, J., et al. (2008) · Proceedings of the National Academy of Sciences

Cancer-related Molecular PathwaysPI3K/AKT/mTOR signaling in cancer

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A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

Bai, L., Zhou, H., Xu, R., Zhao, Y., Chinnaswamy, K., McEachern, D., Chen, J., Yang, C.-Y., Liu, Z., Wang, M., et al. (2019) · Cancer Cell

Protein Degradation and InhibitorsCytokine Signaling Pathways and Interactions

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

Wang, S., Sun, W., Zhao, Y., McEachern, D., Meaux, I., Barrière, C., Stuckey, J. A., Meagher, J. L., Bai, L., Liu, L., et al. (2014) · Cancer Research

Cancer-related Molecular PathwaysHeat shock proteins research

Cited by 328

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

Li, Y., Yang, J., Aguilar, A., McEachern, D., Przybranowski, S., Liu, L., Yang, C.-Y., Wang, M., Han, X., & Wang, S. (2019) · Journal of Medicinal Chemistry

Protein Degradation and InhibitorsCancer-related Molecular Pathways

Cited by 312

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Qin, C., Hu, Y., Zhou, B., Fernandez-Salas, E., Yang, C.-Y., Liu, L., McEachern, D., Przybranowski, S., Wang, M., Stuckey, J., et al. (2018) · Journal of Medicinal Chemistry

Protein Degradation and InhibitorsChemical Synthesis and Analysis

Cited by 281

Diastereomeric spirooxindoles as highly potent and efficacious MDM2 inhibitors

Zhao, Y., Liu, L., Sun, W., Lu, J., McEachern, D., Li, X., Yu, S., Bernard, D., Ochsenbein, P., Ferey, V., et al. (2013) · Journal of the American Chemical Society

Cancer-related Molecular PathwaysHeterocyclic Compound Synthesis and Bioactivity

Cited by 234

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

Zhou, H., Bai, L., Xu, R., Zhao, Y., Chen, J., McEachern, D., Chinnaswamy, K., Wen, B., Dai, L., Kumar, P., et al. (2019) · Journal of Medicinal Chemistry

Protein Degradation and InhibitorsCytokine Signaling Pathways and Interactions

Cited by 233

Discovery of 4-((3′ R ,4′ S ,5′ R )-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development

Aguilar, A., Lu, J., Liu, L., Du, D., Bernard, D., McEachern, D., Przybranowski, S., Li, X., Luo, R., Wen, B., et al. (2017) · Journal of Medicinal Chemistry

Cancer-related Molecular PathwaysHeterocyclic Compound Synthesis and Bioactivity

Cited by 211

Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer

Bai, L., Zhou, B., Yang, C.-Y., Ji, J., McEachern, D., Przybranowski, S., Jiang, H., Hu, J., Xu, F., Zhao, Y., et al. (2017) · Cancer Research

Protein Degradation and InhibitorsHistone Deacetylase Inhibitors Research

Cited by 199

Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction

Yu, S., Qin, D., Shangary, S., Chen, J., Wang, G., Ding, K., McEachern, D., Qiu, S., Nikolovska-Coleska, Z., Miller, R., et al. (2009) · Journal of Medicinal Chemistry

Cancer-related Molecular PathwaysPI3K/AKT/mTOR signaling in cancer

Cited by 180

Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer

Han, X., Zhao, L., Xiang, W., Qin, C., Miao, B., McEachern, D., Wang, Y., Metwally, H., Wang, L., Matvekas, A., et al. (2021) · Journal of Medicinal Chemistry

Protein Degradation and InhibitorsProstate Cancer Treatment and Research

Cited by 170

Reactivation of p53 by a specific MDM2 antagonist (MI-43) leads to p21-mediated cell cycle arrest and selective cell death in colon cancer

Shangary, S., Ding, K., Qiu, S., Nikolovska-Coleska, Z., Bauer, J. A., Liu, M., Wang, G., Lu, Y., McEachern, D., Bernard, D., et al. (2008) · Molecular Cancer Therapeutics

Cancer-related Molecular PathwaysHeat shock proteins research

Cited by 91

Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo

Hoffman-Luca, C. G., Ziazadeh, D., McEachern, D., Zhao, Y., Sun, W., Debussche, L., & Wang, S. (2015) · Clinical Cancer Research

Cancer-related Molecular PathwaysCell death mechanisms and regulation

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Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein–Protein Interaction

Aguilar, A., Zheng, K., Xu, T., Xu, S., Huang, L., Fernandez-Salas, E., Liu, L., Bernard, D., Harvey, K. P., Foster, C., et al. (2019) · Journal of Medicinal Chemistry

Computational Drug Discovery MethodsProtein Degradation and Inhibitors

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