Evidence map›Paper›PMID 39137166›Full record

ArticleACS chemical biology2024

Targeted Degradation of Protein Kinase A via a Stapled Peptide PROTAC.

Matthew K Whittaker, George N Bendzunas, Mahsa Shirani, Timothy J LeClair, Bassem Shebl, Taylor C Dill, Philip Coffino, Sanford M Simon, Eileen J Kennedy

Abstract readLetter
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS chemical biology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Review
  2. Article
  3. 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

9 authors.

Matthew K WhittakerDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia 30602, United States.ORCID 0000-0002-1846-6402
George N BendzunasDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia 30602, United States.
Mahsa ShiraniLaboratory of Cellular Biophysics, The Rockefeller University, New York, New York 10065, United States.
Timothy J LeClairDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia 30602, United States.
Bassem SheblLaboratory of Cellular Biophysics, The Rockefeller University, New York, New York 10065, United States.
Taylor C DillDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia 30602, United States.
Philip CoffinoLaboratory of Cellular Biophysics, The Rockefeller University, New York, New York 10065, United States.
Sanford M SimonLaboratory of Cellular Biophysics, The Rockefeller University, New York, New York 10065, United States.
Eileen J KennedyDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia 30602, United States.ORCID 0000-0001-5610-1677

Funding

Project 4: ImmunovirotherapyP50CA210964 · NCI · MAYO CLINIC ROCHESTER · PI Zongming Eric Chen · 2018 to 2026
$20.5M
What differences between the chimeric fusion oncoprotein DNAJB1-PRKACA and native kinase PRKACA lead to transformation in the childhood cancer, fibrolamellar hepatocellular carcinoma?U54CA243126 · NCI · ROCKEFELLER UNIVERSITY · PI SIMON, SANFORD M · 2019 to 2023
$5.4M
Targeting WASF3 to suppress metastasisR01GM134168 · NIGMS · UNIVERSITY OF GEORGIA · PI KENNEDY, EILEEN J · 2019 to 2022
$1.2M
NCI NIH HHS P50 CA210964NCI NIH HHS U54 CA243126NIGMS NIH HHS R01 GM134168
6 · The paper itself

Abstract

Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules that bind and recruit an E3 ubiquitin ligase to a targeted protein of interest, often through the utilization of a small molecule inhibitor. To expand the possible range of kinase targets that can be degraded by PROTACs, we sought to develop a PROTAC utilizing a hydrocarbon-stapled peptide as the targeting agent to bind the surface of a target protein of interest. In this study, we describe the development of a proteolysis-targeting chimera, dubbed

Indexed as

Cyclic AMP-Dependent Protein KinasesPeptidesProteolysisHumansPhosphorylationProteasome Endopeptidase ComplexUbiquitin-Protein LigasesCyclic AMP-Dependent Protein KinasesPeptidesProteasome Endopeptidase ComplexUbiquitin-Protein Ligases

Identifiers

PMID39137166
PMCPMC11420944

What Socratic 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 Socratic graph.