Results 201 to 210 of about 644,957 (254)
Spirooxindole Derivatives as Emerging Scaffolds in Drug Discovery: Synthetic Strategies, Structure-Activity Relationship, and Biological Activities. [PDF]
ChemMedChemKalita RC, Bezbaruah S, Patle D.
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High-throughput strategy for targeting MDM2 in uveal melanoma to reverse radiation therapy resistance. [PDF]
Cell Death DiscovZhu Q, Gong X, Zhang S, Zhang J, Yan H.
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Activity of PROTAC MDM2 degrader in primary leukemia cells and PDX models. [PDF]
LeukemiaKandarpa M +7 more
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Resistance acquisition to MDM2 inhibitors
Biochemical Society Transactions, 2014 Various experimental strategies aim to (re)activate p53 signalling in cancer cells. The most advanced clinically are small-molecule inhibitors of the autoregulatory interaction between p53 and MDM2 (murine double minute 2). Different MDM2 inhibitors are currently under investigation in clinical trials.
Jindrich, Cinatl +3 more
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Current Pharmaceutical Design, 2012 The protein-protein interaction (PPI) between p53 and its negative regulator MDM2 comprises one of the most important and intensely studied PPI's involved in preventing the initiation of cancer. The interaction between p53 and MDM2 is conformation-based and is tightly regulated on multiple levels. Due to the Angstrom level structural insight there is a
Kareem, Khoury, Alex, Dömling
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Current Medicinal Chemistry, 2023
Abstract: Discovery of MDM2 and MDM2-p53 interaction inhibitors changed the direction of anticancer research as it is involved in about 50% of cancer cases globally. Not only the inhibition of MDM2 but also its interaction with p53 proved to be an effective strategy in anticancer drug design and development.
Suresh Thareja +2 more
exaly +3 more sources
Abstract: Discovery of MDM2 and MDM2-p53 interaction inhibitors changed the direction of anticancer research as it is involved in about 50% of cancer cases globally. Not only the inhibition of MDM2 but also its interaction with p53 proved to be an effective strategy in anticancer drug design and development.
Suresh Thareja +2 more
exaly +3 more sources
Inhibitors of MDM2 and MDMX: A Structural Perspective
Future Medicinal Chemistry, 2009 p53 is a potent tumor suppressor with a crucial role in preventing uncontrolled cell proliferation and is therefore frequently deleted or mutated in cancer. For tumors with wild-type p53, its function can be overcome by overactive cellular antagonists, such as the ubiquitin ligase murine double minute clone 2 (MDM2).
Riedinger, Christiane, McDonnell, James
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An Update on MDMX and Dual MDM2/X Inhibitors
Current Topics in Medicinal Chemistry, 2018The tumor suppressor protein p53 is inactivated in all types of human cancers, either by negative regulation, by mutation or deletion of its gene. Specifically, in tumors that retain wild-type (wt) p53 status, p53 is inactivated by interaction with negative regulators, such as MDM2 and MDMX. These two proteins are found to be overexpressed in several
Elizabeth A Lopes +2 more
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MDM2-PROTAC versus MDM2 Inhibitors: Beyond p53 Reactivation
Cancer Discovery, 2023Summary: In this issue of Cancer Discovery, Adams and colleagues present the discovery of a potent PROTAC, MDM2 degrader, which activates wild-type p53 leading to cancer cell death. Importantly, in a number of in vitro and in vivo experiments, the authors show that the depletion of MDM2 by PROTAC kills p53 ...
Sylvain Peuget, Galina Selivanova
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