Evidence map›Paper›PMID 31009996›Full record

ArticleMolecules (Basel, Switzerland)2019

A Stapled Peptide Mimic of the Pseudosubstrate Inhibitor PKI Inhibits Protein Kinase A.

Jascha T Manschwetus, George N Bendzunas, Ameya J Limaye, Matthias J Knape, Friedrich W Herberg, Eileen J Kennedy

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
0.7field-weighted citation impact, top 31% 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

11 citing papers in PubMed, 15 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Article
  6. Article
  7. Biochemical Analysis of AKAP-Anchored PKA Signaling Complexes.Methods in molecular biology (Clifton, N.J.) · 2022
    Article
  8. GPharmacological reviews · 2021
    Review
  9. Protein kinase A inhibitor proteins (PKIs) divert GPCR-Gαs-cAMP signaling toward EPAC and ERK activation and are involved in tumor growth.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020
    Article
  10. Review
  11. 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

6 authors at 2 institutions in 2 countries.

Jascha T ManschwetusDepartment of Biochemistry, Institute for Biology, University of Kassel, Heinrich-Plett-Str. 40, 34132 Kassel, Germany. j.manschwetus@uni-kassel.de.ORCID 0000-0003-3136-9153
George N BendzunasDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, 240 W. Green St, Athens, GA 30602, USA. georgenb@uga.edu.
Ameya J LimayeDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, 240 W. Green St, Athens, GA 30602, USA. ameya.limaye@uga.edu.
Matthias J KnapeDepartment of Biochemistry, Institute for Biology, University of Kassel, Heinrich-Plett-Str. 40, 34132 Kassel, Germany. maknape@googlemail.com.ORCID 0000-0002-0474-9997
Friedrich W HerbergDepartment of Biochemistry, Institute for Biology, University of Kassel, Heinrich-Plett-Str. 40, 34132 Kassel, Germany. herberg@uni-kassel.de.
Eileen J KennedyDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, 240 W. Green St, Athens, GA 30602, USA. ekennedy@uga.edu.ORCID 0000-0001-5610-1677
University of Georgia · USUniversity of Kassel · DE

Funding

Deutsche Forschungsgemeinschaft He1818/10National Institutes of Health CA154600National Institutes of Health CA188439Otto-Braun Fund Predoctoral FellowshipPhosMOrg FutureU.S. Department of Defense W81XWH-17-1-0290
6 · The paper itself

Abstract

Kinases regulate multiple and diverse signaling pathways and misregulation is implicated in a multitude of diseases. Although significant efforts have been put forth to develop kinase-specific inhibitors, specificity remains a challenge. As an alternative to catalytic inhibition, allosteric inhibitors can target areas on the surface of an enzyme, thereby providing additional target diversity. Using cAMP-dependent protein kinase A (PKA) as a model system, we sought to develop a hydrocarbon-stapled peptide targeting the pseudosubstrate domain of the kinase. A library of peptides was designed from a Protein Kinase Inhibitor (PKI), a naturally encoded protein that serves as a pseudosubstrate inhibitor for PKA. The binding properties of these peptide analogs were characterized by fluorescence polarization and surface plasmon resonance, and two compounds were identified with K

Indexed as

Binding SitesCell LineCyclic AMP-Dependent Protein KinasesDose-Response Relationship, DrugHumansKineticsMolecular Docking SimulationMolecular Dynamics SimulationPeptidesProtein BindingProtein Kinase InhibitorsStructure-Activity RelationshipSubstrate SpecificitySurface Plasmon ResonanceCyclic AMP-Dependent Protein KinasesPeptidesProtein Kinase InhibitorsIP20kinase inhibitorPKAPKIpseudosubstratestapled peptide

Identifiers

PMID31009996
PMCPMC6514771
OpenAlexW2935897823

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.