Evidence map›Paper›PMID 33200929›Full record

ArticleJournal of medicinal chemistry2020

Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.

Huiyu Ren, Nicole A Bakas, Mitchell Vamos, Apirat Chaikuad, Allison S Limpert, Carina D Wimer, Sonja N Brun, Lester J Lambert, Lutz Tautz, Maria Celeridad and 4 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.

0numbers the graph read from it
0cells of the map it votes in
30citing papers in PubMed
4.7field-weighted citation impact, top 4% 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

30 citing papers in PubMed, 67 citations in OpenAlex.

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  15. Autophagy and cancer therapy.Cancer letters · 2024
    Review
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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

14 authors at 3 institutions in 2 countries.

Huiyu RenCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Nicole A BakasCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Mitchell VamosCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Apirat ChaikuadStructural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe-University Frankfurt, Frankfurt 60438, Germany.ORCID 0000-0003-1120-2209
Allison S LimpertCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Carina D WimerCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Sonja N BrunMolecular and Cell Biology Laboratory, The Salk Institute for Biological Studies, La Jolla, San Diego, California 92037, United States.
Lester J LambertCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Lutz TautzCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Maria CeleridadCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Douglas J ShefflerCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.
Stefan KnappStructural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe-University Frankfurt, Frankfurt 60438, Germany.ORCID 0000-0001-5995-6494
Reuben J ShawMolecular and Cell Biology Laboratory, The Salk Institute for Biological Studies, La Jolla, San Diego, California 92037, United States.
Nicholas D P CosfordCancer Molecules & Structures Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.ORCID 0000-0001-7228-4709
Sanford Burnham Prebys Medical Discovery Institute · USGoethe University Frankfurt · DESalk Institute for Biological Studies · US

Funding

Tumor Microenvironment and Cancer ImmunologyP30CA030199 · NCI · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI Michael Jackson · 1985 to 2026
$107.2M
Viral Vector Core (VVC)P30CA014195 · NCI · SALK INSTITUTE FOR BIOLOGICAL STUDIES · PI Ye Zheng · 1985 to 2026
$82.8M
Decoding And Targeting The LKB1-AMPK Signaling Pathway In CancerR35CA220538 · NCI · SALK INSTITUTE FOR BIOLOGICAL STUDIES · PI Reuben Shaw · 2017 to 2026
$11.3M
Cancer Targets and Drug DiscoveryT32CA211036 · NCI · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI COSFORD, NICHOLAS DAVID · 2018 to 2022
$1.2M
NCI NIH HHS P30 CA014195NCI NIH HHS P30 CA030199NCI NIH HHS R35 CA220538NCI NIH HHS T32 CA211036Wellcome Trust
6 · The paper itself

Abstract

Inhibition of autophagy, the major cellular recycling pathway in mammalian cells, is a promising strategy for the treatment of triple-negative breast cancer (TNBC). We previously reported SBI-0206965, a small molecule inhibitor of unc-51-like autophagy activating kinase 1 (ULK1), which is a key regulator of autophagy initiation. Herein, we describe the design, synthesis, and characterization of new dual inhibitors of ULK1 and ULK2 (ULK1/2). One inhibitor, SBP-7455 (compound

Indexed as

AnimalsAntineoplastic AgentsApoptosisAutophagyAutophagy-Related Protein-1 HomologCell Line, TumorCell ProliferationCell SurvivalDrug Screening Assays, AntitumorDrug SynergismFemaleHEK293 CellsHumansIntracellular Signaling Peptides and ProteinsMice, Inbred C57BLPhthalazinesAntineoplastic AgentsAutophagy-Related Protein-1 HomologIntracellular Signaling Peptides and ProteinsolaparibPhthalazinesPiperazinesPoly(ADP-ribose) Polymerase InhibitorsProtein Kinase InhibitorsProtein Serine-Threonine KinasesPyrimidinesULK1 protein, humanUlk2 protein, human

Identifiers

PMID33200929
PMCPMC8064294
OpenAlexW3101755431

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.