Evidence map›Paper›PMID 21171592›Full record

ArticleJournal of the American Chemical Society2011

Novel pyrrolopyrimidine-based α-helix mimetics: cell-permeable inhibitors of protein−protein interactions.

Ji Hoon Lee, Qi Zhang, Sunhwan Jo, Sergio C Chai, Misook Oh, Wonpil Im, Hua Lu, Hyun-Suk Lim

Abstract read
In one paragraph

Article in Journal of the American Chemical Society, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.

0numbers the graph read from it
0cells of the map it votes in
51citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

51 citing papers in PubMed.

  1. Review
  2. Review
  3. Review
  4. Article
  5. Article
  6. Synthesis and Biological Evaluation of NovelMolecules (Basel, Switzerland) · 2023
    Article
  7. Article
  8. Article
  9. Article
  10. Article
  11. Efficient Dimerization Disruption ofJournal of medicinal chemistry · 2021
    Article
  12. Review
  13. Review
  14. Review
  15. Review
  16. Article
  17. Review
  18. Review
  19. Article
  20. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Ji Hoon LeeDepartment of Biochemistry and Molecular Biology, and Indiana University Simon Cancer Center, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
Qi Zhang
Sunhwan Jo
Sergio C Chai
Misook Oh
Wonpil Im
Hua Lu
Hyun-Suk Lim

Funding

The Role of Ribosomal Proteins in the P53-MDM2 PathwayR01CA095441 · NCI · TULANE UNIVERSITY OF LOUISIANA · PI LU, HUA · 2002 to 2021
$5.1M
Role of the AMPK-MDMX-p53 pathway in cancerR01CA127724 · NCI · TULANE UNIVERSITY OF LOUISIANA · PI LU, HUA · 2007 to 2019
$3.0M
Role of ribosomal proteins in regulating c-MycR01CA129828 · NCI · TULANE UNIVERSITY OF LOUISIANA · PI LU, HUA · 2008 to 2012
$1.5M
NCI NIH HHS CA095441NCI NIH HHS CA127724NCI NIH HHS CA129828NCI NIH HHS R01 CA095441NCI NIH HHS R01 CA127724NCI NIH HHS R01 CA129828
6 · The paper itself

Abstract

There is considerable interest in developing non-peptidic, small-molecule α-helix mimetics to disrupt α-helix-mediated protein−protein interactions. Herein, we report the design of a novel pyrrolopyrimidine-based scaffold for such α-helix mimetics with increased conformational rigidity. We also developed a facile solid-phase synthetic route that is amenable to divergent synthesis of a large library. Using a fluorescence polarization-based assay, we identified cell-permeable, dual MDMX/MDM2 inhibitors, demonstrating that the designed molecules can act as α-helix mimetics.

Indexed as

Amino Acid SequenceBiomimetic MaterialsCell Line, TumorDrug DesignHigh-Throughput Screening AssaysHumansModels, MolecularPermeabilityProtein BindingProtein Structure, SecondaryProto-Oncogene Proteins c-mdm2PyrimidinesPyrrolesTumor Suppressor Protein p53Proto-Oncogene Proteins c-mdm2PyrimidinesPyrrolespyrrolopyrimidineTumor Suppressor Protein p53

Identifiers

PMID21171592
PMCPMC3079198

What OpenQuestion holds

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Registered trials

None linked

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.