Evidence map›Paper›PMID 30176143›Full record

ArticleJournal of the American Chemical Society2018

Cell-Permeable Bicyclic Peptidyl Inhibitors against NEMO-IκB Kinase Interaction Directly from a Combinatorial Library.

Curran A Rhodes, Patrick G Dougherty, Jahan K Cooper, Ziqing Qian, Steffen Lindert, Qi-En Wang, Dehua Pei

Abstract read
In one paragraph

Article in Journal of the American Chemical Society, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.

0numbers the graph read from it
0cells of the map it votes in
34citing papers in PubMed
3.1field-weighted citation impact, top 6% of its field
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

34 citing papers in PubMed, 58 citations in OpenAlex.

  1. Bismuth Bicycles.Journal of peptide science : an official publication of the European Peptide Society · 2026
    Review
  2. Article
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  5. Review
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  9. Inhibition ofPNAS nexus · 2023
    Article
  10. Article
  11. Article
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  13. Article
  14. Review
  15. Article
  16. Computational Design of Structured and Functional Peptide Macrocycles.Methods in molecular biology (Clifton, N.J.) · 2022
    Article
  17. Article
  18. Designing Cell-Permeable Peptide Therapeutics That Enter the Cell by Endocytosis.ACS symposium series. American Chemical Society · 2022
    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

7 authors at 2 institutions in 1 country.

Curran A RhodesDepartment of Chemistry and Biochemistry , The Ohio State University , 100 West 18th Avenue , Columbus , Ohio 43210 , United States.
Patrick G DoughertyDepartment of Chemistry and Biochemistry , The Ohio State University , 100 West 18th Avenue , Columbus , Ohio 43210 , United States.
Jahan K CooperDepartment of Chemistry and Biochemistry , The Ohio State University , 100 West 18th Avenue , Columbus , Ohio 43210 , United States.
Ziqing QianDepartment of Chemistry and Biochemistry , The Ohio State University , 100 West 18th Avenue , Columbus , Ohio 43210 , United States.
Steffen LindertDepartment of Chemistry and Biochemistry , The Ohio State University , 100 West 18th Avenue , Columbus , Ohio 43210 , United States.ORCID 0000-0002-3976-3473
Qi-En WangDepartment of Radiology, James Cancer Hospital and Solove Research Institute , The Ohio State University Wexner Medical Center , Columbus , Ohio 43210 , United States.
Dehua PeiDepartment of Chemistry and Biochemistry , The Ohio State University , 100 West 18th Avenue , Columbus , Ohio 43210 , United States.ORCID 0000-0002-2057-6934
The Ohio State University · USThe Ohio State University Comprehensive Cancer Center – Arthur G. James Cancer Hospital and Richard J. Solove Research Institute · US

Funding

Development of Cell-Permeable Peptides and ProteinsR35GM122459 · NIGMS · OHIO STATE UNIVERSITY · PI Dehua Pei · 2017 to 2026
$5.1M
CHEMISTRY/BIOLOGY TRAINING GRANTT32GM008512 · NIGMS · OHIO STATE UNIVERSITY · PI PEI, DEHUA · 1996 to 2016
$3.9M
Averting recurrent and resistant ovarian tumorsR01CA211175 · NCI · OHIO STATE UNIVERSITY · PI WANG, QIEN · 2017 to 2021
$2.3M
Molecular models to characterize actions of calcium sensitizing drugsR01HL137015 · NHLBI · OHIO STATE UNIVERSITY · PI LINDERT, STEFFEN · 2018 to 2022
$1.8M
Cyclic Cell-Penetrating PeptidesR01GM110208 · NIGMS · OHIO STATE UNIVERSITY · PI PEI, DEHUA · 2014 to 2016
$980k
Rational Drug Design for Chronic Neuronal DamageR03AG054904 · NIA · OHIO STATE UNIVERSITY · PI LINDERT, STEFFEN · 2017 to 2018
$155k
NCI NIH HHS R01 CA211175NHLBI NIH HHS R01 HL137015NIA NIH HHS R03 AG054904NIGMS NIH HHS R01 GM110208NIGMS NIH HHS R35 GM122459
6 · The paper itself

Abstract

Macrocyclic peptides are capable of binding to flat protein surfaces such as the interfaces of protein-protein interactions with antibody-like affinity and specificity, but generally lack cell permeability in order to access intracellular targets. In this work, we designed and synthesized a large combinatorial library of cell-permeable bicyclic peptides, in which the first ring consisted of randomized peptide sequences for potential binding to a target of interest, while the second ring featured a family of different cell-penetrating motifs, for both cell penetration and target binding. The library was screened against the IκB kinase α/β (IKKα/β)-binding domain of NF-κB essential modulator (NEMO), resulting in the discovery of several cell-permeable bicyclic peptides, which inhibited the NEMO-IKKβ interaction with low μM IC

Indexed as

Peptide LibraryAmino Acid SequenceAntineoplastic AgentsBiological TransportCell Line, TumorHEK293 CellsHumansI-kappa B KinaseMolecular Docking SimulationPeptides, CyclicProtein BindingSignal TransductionAntineoplastic AgentsI-kappa B KinaseIKBKG protein, humanPeptide LibraryPeptides, Cyclic

Identifiers

PMID30176143
PMCPMC6231237
OpenAlexW2890017736

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

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.