Evidence map›Paper›PMID 25162754›Full record

ArticleJournal of medicinal chemistry2014

Structure-based optimization of a peptidyl inhibitor against calcineurin-nuclear factor of activated T cell (NFAT) interaction.

Ziqing Qian, Patrick G Dougherty, Tao Liu, Shameema Oottikkal, Patrick G Hogan, Christopher M Hadad, Dehua Pei

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
0.3field-weighted citation impact, top 39% 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

10 citing papers in PubMed, 12 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Designing Cell-Permeable Peptide Therapeutics That Enter the Cell by Endocytosis.ACS symposium series. American Chemical Society · 2022
    Article
  6. A Review of Calcineurin Biophysics with Implications for Cardiac Physiology.International journal of molecular sciences · 2021
    Review
  7. Article
  8. Targeting the NFAT:AP-1 transcriptional complex on DNA with a small-molecule inhibitor.Proceedings of the National Academy of Sciences of the United States of America · 2019
    Article
  9. Article
  10. 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

7 authors at 2 institutions in 1 country.

Ziqing QianDepartment of Chemistry and Biochemistry, The Ohio State University , 484 West 12th Avenue, Columbus, Ohio 43210, United States.
Patrick G Dougherty
Tao Liu
Shameema Oottikkal
Patrick G Hogan
Christopher M Hadad
Dehua Pei
The Ohio State University · USLa Jolla Institute for Immunology · US

Funding

Recognition and Catalysis of Phosphotyrosyl ProteinsR01GM062820 · NIGMS · OHIO STATE UNIVERSITY · PI PEI, DEHUA · 2003 to 2015
$3.2M
Substrate Profiling of Protein Tyrosine PhosphatasesR01CA132855 · NCI · OHIO STATE UNIVERSITY · PI PEI, DEHUA · 2009 to 2013
$1.3M
NCI NIH HHS CA132855NCI NIH HHS R01 CA132855NIGMS NIH HHS GM062820NIGMS NIH HHS R01 GM062820
6 · The paper itself

Abstract

Calcineurin inhibitors such as cyclosporine A and FK506 are effective immunosuppressants but produce severe side effects. Rational modification of a previously reported peptide inhibitor, GPHPVIVITGPHEE (KD ∼ 500 nM), by replacing the two valine residues with tert-leucine and the C-terminal proline with a cis-proline analogue, gave an improved inhibitor ZIZIT-cisPro, which binds to calcineurin with a KD value of 2.6 nM and is more resistant to proteolysis.

Indexed as

Active Transport, Cell NucleusAmino Acid SequenceAmino Acid SubstitutionBinding SitesCalcineurinCalcineurin InhibitorsCell NucleusDrug StabilityHeLa CellsHumansModels, MolecularNFATC Transcription FactorsPeptidesProtein BindingProtein ConformationStructure-Activity RelationshipCalcineurinCalcineurin InhibitorsNFATC Transcription FactorsPeptides

Identifiers

PMID25162754
PMCPMC4174996
OpenAlexW2326350727

What OpenQuestion holds

Textmetadata
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.