Drugging the p53 pathway: understanding the route to clinical efficacy

By K. Khoo, C. Verma, David P. Lane. Nature reviews. Drug discovery, 2014

706 citations recorded by the source corpus.

View Paper: https://www.semanticscholar.org/paper/e8cb5f832dc53616c0c8d044fb1f3f1d28ca472d

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In Oncology

Citations in the corpus

The role of ubiquitination in tumorigenesis and targeted drug discovery (2020, methodology): “HLI373 is the highly water-soluble derivative of HLI98, and it has a greater potential to be a cancer therapeutic agent due to this characteristic.389 Although Mdmx (murine/human double minute X) has no ubiquitination activity, it can either bind to the N-terminus of p53 and inactivate it directly o”
OncoKB: A Precision Oncology Knowledge Base (2017, background): “…and early phase clinical trials 45,46 , the agents tested do not directly target TP53, their activity is typically not restricted to TP53 mutant models, and clinical trials testing these agents have either been aborted due to lack of efficacy or do not use TP53 status as a selection criterion 47 .”
Synthetic Lethality of Combined Bcl-2 Inhibition and p53 Activation in AML: Mechanisms and Superior Antileukemic Efficacy (2017, background): “In addition, several compounds have been reported to promote the proper folding of mutant p53 and restore its transcriptional function (Gurpinar and Vousden, 2015; Hoe et al., 2014).”
The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity. (2017, positive): “…1692–1704, August 15, 2017 ª 2017 The Autho This is an open access article under the CC BY-NC-ND license (http:// arrest and apoptosis under different stress stimuli through transcriptional and transcription-independent mechanisms (Bieging et al., 2014; Green and Kroemer, 2009; Khoo et al., 2014).”
Insights in Post-Translational Modifications: Ubiquitin and SUMO (2022, background): “Mis-regulation of these UBLs (Ubiquitin and SUMOs) are connected to diseases including cancer [94,95].”
The Cell-Cycle Arrest and Apoptotic Functions of p53 in Tumor Initiation and Progression. (2016, background): “Reactivation of p53ERTAM in MDMX-null mice induces less tissue damage and does not cause rapid death, suggesting that MDMX inhibitors may have lower systemic toxicity (Garcia et al. 2011).”
Apoptosis as anticancer mechanism: function and dysfunction of its modulators and targeted therapeutic strategies (2016, background): “Numerous findings about this subject have been shown and summarized in different reviews [159-161].”
Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. (2014, background): “The biological challenges facing clinical positioning of these compounds has been recently discussed (Khoo et al., 2014).”