ArticleACS medicinal chemistry letters2017
Artificial Macrocycles as Potent p53-MDM2 Inhibitors.
Article in ACS medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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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.
The trial behind it
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
10 citing papers in PubMed.
- DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2-p53 Inhibitor.ACS medicinal chemistry letters · 2023Article
- Conformationally Controlled spAngewandte Chemie (International ed. in English) · 2023Article
- Divergent, C-C Bond Forming Macrocyclizations Using Modular Sulfonylhydrazone and Derived Substrates.The Journal of organic chemistry · 2021Article
- Benchmark of Generic Shapes for Macrocycles.Journal of chemical information and modeling · 2020Article
- Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives.Acta pharmaceutica Sinica. B · 2020Review
- Conformation of the Macrocyclic Drug Lorlatinib in Polar and Nonpolar Environments: A MD Simulation and NMR Study.ACS omega · 2019Article
- Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.European journal of medicinal chemistry · 2019Article
- A fluorinated indole-based MDM2 antagonist selectively inhibits the growth of p53The FEBS journal · 2019Article
- Design of indole- and MCR-based macrocycles as p53-MDM2 antagonists.Beilstein journal of organic chemistry · 2019Article
- Artificial Macrocycles by Ugi Reaction and Passerini Ring Closure.The Journal of organic chemistry · 2016Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Based on a combination of an Ugi four component reaction and a ring closing metathesis, a library of novel artificial macrocyclic inhibitors of the p53-MDM2 interaction was designed and synthesized. These macrocycles, alternatively to stapled peptides, target for the first time the large hydrophobic surface area formed by Tyr67, Gln72, His73, Val93, and Lys94 yielding derivatives with affinity to MDM2 in the nanomolar range. Their binding affinity with MDM2 was evaluated using fluorescence polarization (FP) assay and
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.