Evidence map›Paper›PMID 29289448›Full record

ArticleBioorganic & medicinal chemistry2018

Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.

Andrii Monastyrskyi, Napon Nilchan, Victor Quereda, Yoshihiko Noguchi, Claudia Ruiz, Wayne Grant, Michael Cameron, Derek Duckett, William Roush

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing 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

14 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
  4. Inhibition of Casein Kinase 1International journal of molecular sciences · 2025
    Article
  5. Review
  6. Article
  7. Article
  8. Article
  9. "Dual Anta-Inhibitors" of the APharmaceuticals (Basel, Switzerland) · 2023
    Article
  10. Review
  11. Review
  12. Article
  13. Article
  14. The nucleolus, an ally, and an enemy of cancer cells.Histochemistry and cell biology · 2018
    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.

Andrii MonastyrskyiDepartment of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Napon NilchanDepartment of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Victor QueredaDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Yoshihiko NoguchiDepartment of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Claudia RuizDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Wayne GrantDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Michael CameronDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Derek DuckettDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
William RoushDepartment of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States. Electronic address: roush@scripps.edu.

Funding

Targeting Casein Kinase 1d/e (CK1d/1e) in Cancer TherapeuticsR01CA175094 · NCI · SCRIPPS FLORIDA · PI ROUSH, WILLIAM R · 2014 to 2016
$1.5M
Development of Casein Kinase 1d and 1e Inhibitors for Treatment of Brain CancerF32CA200105 · NCI · SCRIPPS FLORIDA · PI MONASTYRSKYI, ANDRII · 2016 to 2017
$111k
NCI NIH HHS F32 CA200105NCI NIH HHS R01 CA175094
6 · The paper itself

Abstract

Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.

Indexed as

AnimalsBinding SitesCasein Kinase 1 epsilonCasein Kinase IdeltaCatalytic DomainCell Line, TumorFemaleHalf-LifeHumansMaleMiceMice, Inbred C57BLMicrosomes, LiverMolecular Docking SimulationPermeabilityProtein Kinase InhibitorsCasein Kinase 1 epsilonCasein Kinase IdeltaProtein Kinase InhibitorsBreast cancerCasein kinase 1 delta and epsilonInhibitorKinaseStructure-activity relationship

Identifiers

PMID29289448
PMCPMC5803353

What Socratic 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 Socratic graph.