Evidence map›Paper›PMID 29111705›Full record

ArticleJournal of medicinal chemistry2017

One-Bead-Two-Compound Thioether Bridged Macrocyclic γ-AApeptide Screening Library against EphA2.

Yan Shi, Sridevi Challa, Peng Sang, Fengyu She, Chunpu Li, Geoffrey M Gray, Alekhya Nimmagadda, Peng Teng, Timothy Odom, Yan Wang and 3 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing 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

20 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Acta pharmaceutica Sinica. B · 2023
    Article
  5. Article
  6. Article
  7. Review
  8. RNA-Binding Macrocyclic Peptides.Frontiers in molecular biosciences · 2022
    Review
  9. Peptidomimetic-based antibody surrogate for HER2.Acta pharmaceutica Sinica. B · 2021
    Article
  10. Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Approaches to Manipulate Ephrin-A:EphA Forward Signaling Pathway.Pharmaceuticals (Basel, Switzerland) · 2020
    Review
  16. Article
  17. Review
  18. Inhibition of β-catenin/B cell lymphoma 9 protein-protein interaction using α-helix-mimicking sulfono-γ-AApeptide inhibitors.Proceedings of the National Academy of Sciences of the United States of America · 2019
    Article
  19. Article
  20. Article
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

13 authors.

Yan ShiDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Sridevi ChallaDepartment of Molecular Oncology, H. Lee Moffitt Cancer Center and Research Institute , 12902 Magnolia Drive, Tampa, Florida 33612, United States.
Peng SangDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Fengyu SheDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Chunpu LiDepartment of Medical Oncology, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Geoffrey M GrayDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Alekhya NimmagaddaDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Peng TengDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Timothy OdomDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
Yan WangDepartment of Medical Oncology, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Arjan van der VaartDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.ORCID 0000-0002-8950-1850
Qi LiDepartment of Medical Oncology, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Jianfeng CaiDepartment of Chemistry, University of South Florida , 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.ORCID 0000-0003-3106-3306

Funding

Requesting HPLC for the project of "Alpha-AApeptides as a Novel Class of Antimicrobial Biomaterials"R01GM112652 · NIGMS · UNIVERSITY OF SOUTH FLORIDA · PI CAI, JIANFENG · 2015 to 2019
$1.5M
NIGMS NIH HHS R01 GM112652
6 · The paper itself

Abstract

Identification of molecular ligands that recognize peptides or proteins is significant but poses a fundamental challenge in chemical biology and biomedical sciences. Development of cyclic peptidomimetic library is scarce, and thus discovery of cyclic peptidomimetic ligands for protein targets is rare. Herein we report the unprecedented one-bead-two-compound (OBTC) combinatorial library based on a novel class of the macrocyclic peptidomimetics γ-AApeptides. In the library, we utilized the coding peptide tags synthesized with Dde-protected α-amino acids, which were orthogonal to solid phase synthesis of γ-AApeptides. Employing the thioether linkage, the desired macrocyclic γ-AApeptides were found to be effective for ligand identification. Screening the library against the receptor tyrosine kinase EphA2 led to the discovery of one lead compound that tightly bound to EphA2 (K

Indexed as

Peptide LibraryCell Line, TumorCell MovementEnzyme AssaysHumansMolecular Dynamics SimulationPeptides, CyclicPeptidomimeticsProtein BindingReceptor, EphA2SulfidesPeptide LibraryPeptides, CyclicPeptidomimeticsReceptor, EphA2Sulfides

Identifiers

PMID29111705
PMCPMC5881388

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.