Evidence map›Paper›PMID 32530623›Full record

ArticleJournal of medicinal chemistry2020

Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6

Fleur M Ferguson, Yan Liu, Wayne Harshbarger, Ling Huang, Jinhua Wang, Xianming Deng, Stephen J Capuzzi, Eugene N Muratov, Alexander Tropsha, Senthil Muthuswamy and 2 more

Erratum issuedOpen 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. An erratum has been issued. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.9field-weighted citation impact, top 14% 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

12 citing papers in PubMed, 21 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7International journal of molecular sciences · 2024
    Article
  5. Review
  6. Article
  7. Review
  8. Article
  9. Article
  10. Structural Basis of Inhibition of DCLK1 by Ruxolitinib.International journal of molecular sciences · 2021
    Article
  11. Article
  12. Review
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

12 authors at 4 institutions in 1 country.

Fleur M FergusonDepartment of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States.ORCID 0000-0003-4091-7617
Yan LiuDepartments of Radiation Oncology and Biochemistry, The University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390, United States.
Wayne HarshbargerDepartments of Radiation Oncology and Biochemistry, The University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390, United States.
Ling HuangCancer Research Institute and Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts 02215, United States.
Jinhua WangDepartment of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States.
Xianming DengDepartment of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States.ORCID 0000-0002-9354-5864
Stephen J CapuzziUNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0003-0001-8211
Eugene N MuratovUNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0003-4616-7036
Alexander TropshaUNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0003-3802-8896
Senthil MuthuswamyCancer Research Institute and Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts 02215, United States.
Kenneth D WestoverDepartments of Radiation Oncology and Biochemistry, The University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390, United States.ORCID 0000-0003-3653-5923
Nathanael S GrayDepartment of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States.ORCID 0000-0001-5354-7403
Harvard University · USThe University of Texas Southwestern Medical Center · USUniversity of North Carolina at Chapel Hill · USBeth Israel Deaconess Medical Center · US

Funding

Tissue and Pathology ResourcesP50CA127003 · NCI · DANA-FARBER CANCER INST · PI BASS, ADAM JOEL · 2007 to 2023
$33.2M
Development of covalent PIP4K2 inhibitors for the treatment of p53 deficient lung tumorsR01CA197329 · NCI · DANA-FARBER CANCER INST · PI GRAY, NATHANAEL SCHIANDER · 2015 to 2019
$2.7M
Drug Repurposing for Cancer Therapy: From Man to Molecules to ManU01CA207160 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI TROPSHA, ALEXANDER · 2016 to 2018
$1.2M
NCI NIH HHS P50 CA127003NCI NIH HHS R01 CA197329NCI NIH HHS U01 CA207160
6 · The paper itself

Abstract

Doublecortin-like kinase 1 (DCLK1) is a serine/threonine kinase that is overexpressed in gastrointestinal cancers, including esophageal, gastric, colorectal, and pancreatic cancers. DCLK1 is also used as a marker of tuft cells, which regulate type II immunity in the gut. However, the substrates and functions of DCLK1 are understudied. We recently described the first selective DCLK1/2 inhibitor, DCLK1-IN-1, developed to aid the functional characterization of this important kinase. Here we describe the synthesis and structure-activity relationships of 5,11-dihydro-6

Indexed as

BenzodiazepinesEnzyme AssaysMolecular StructureProtein Kinase InhibitorsProtein Serine-Threonine KinasesPyrimidinesStructure-Activity RelationshipBenzodiazepinesProtein Kinase InhibitorsProtein Serine-Threonine KinasesPyrimidines

Identifiers

PMID32530623
PMCPMC8270059
OpenAlexW3034990744

What OpenQuestion 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 OpenQuestion graph.