ArticleACS chemical biology2018
Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors.
Article in ACS chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed.
- ZBP1 as a prognostic biomarker correlated with cell proliferation in clear cell renal cell carcinoma.Heliyon · 2024Article
- A cell-permeable probe for the labelling of a bacterial glycosyltransferase and virulence factor.RSC chemical biology · 2024Article
- Targeting p53-MDM2 interaction by small-molecule inhibitors: learning from MDM2 inhibitors in clinical trials.Journal of hematology & oncology · 2022Review
- Pilot Study to Quantify Palladium Impurities in Lead-like Compounds Following Commonly Used Purification Techniques.ACS medicinal chemistry letters · 2022Article
- Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation.ACS medicinal chemistry letters · 2021Article
- Nuisance compounds in cellular assays.Cell chemical biology · 2021Review
- Recent Synthetic Approaches towards Small Molecule Reactivators of p53.Biomolecules · 2020Review
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Targeting the protein-protein interaction between p53 and MDM2/MDMX (MDM4) represents an attractive anticancer strategy for the treatment of p53-competent tumors. Several selective and potent MDM2 inhibitors have been developed and entered the clinic; however, the repertoire of MDMX antagonists is still limited. The arylmethylidenepyrazolinone SJ-172550 has been reported as a selective MDMX antagonist; yet, uncertainties about its mechanism of action have raised doubts about its use as a chemical probe. Here, we show that, in addition to its unclear mode of action, SJ-172550 is unstable in aqueous buffers, giving rise to side products of unknown biological activity. Using an SJ-172550-derived affinity probe, we observed promiscuous binding to cellular proteins whereas cellular thermal shift assays did not reveal a stabilizing effect on MDMX. Overall, our results raise further questions about the interpretation of data using SJ-172550 and related compounds to investigate cellular phenotypes.
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Registered trials
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