Evidence map›Paper›PMID 38556760›Full record

ArticleJournal of medicinal chemistry2024

Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors.

Deyu Kong, Qiang Tian, Zhilong Chen, Hongchao Zheng, Michael A Stashko, Dan Yan, H Shelton Earp, Stephen V Frye, Deborah DeRyckere, Dmitri Kireev and 2 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
2.4field-weighted citation impact, top 11% 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

6 citing papers in PubMed, 10 citations in OpenAlex.

  1. [Role of Receptor Tyrosine Kinase AXL in Cancer Targeted Therapy Drug Resistance].Zhongguo fei ai za zhi = Chinese journal of lung cancer · 2026
    Review
  2. Article
  3. Recent advances in TAM mechanisms in lung diseases.Journal of translational medicine · 2025
    Review
  4. Discovery of Novel TYRO3/MERTK Dual Inhibitors.Journal of medicinal chemistry · 2025
    Article
  5. Article
  6. 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

12 authors at 2 institutions in 1 country.

Deyu KongCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.
Qiang TianCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.
Zhilong ChenCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.ORCID 0000-0001-6312-4914
Hongchao ZhengCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.
Michael A StashkoCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.
Dan YanAflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta and Department of Pediatrics, School of Medicine, Emory University, Atlanta, Georgia 30322, United States.
H Shelton EarpDepartment of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Stephen V FryeCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.ORCID 0000-0002-2415-2215
Deborah DeRyckereAflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta and Department of Pediatrics, School of Medicine, Emory University, Atlanta, Georgia 30322, United States.
Dmitri KireevCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.ORCID 0000-0001-8479-8555
Douglas K GrahamAflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta and Department of Pediatrics, School of Medicine, Emory University, Atlanta, Georgia 30322, United States.
Xiaodong WangCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, Chapel Hill, North Carolina 27599-7355, United States.ORCID 0000-0003-3293-7538
University of North Carolina at Chapel Hill · USEmory University · US

Funding

MERTK/AXL dual inhibitors provide novel treatment for cancer by targeting tumor cells and activating anti-tumor immunityR01CA249190 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI GRAHAM, DOUGLAS K, WANG, XIAODONG · 2020 to 2024
$2.5M
NCI NIH HHS R01 CA249190
6 · The paper itself

Abstract

MERTK and AXL are members of the TAM (TYRO3, AXL, MERTK) family of receptor tyrosine kinases that are aberrantly expressed and have been implicated as therapeutic targets in a wide variety of human tumors. Dual MERTK and AXL inhibition could provide antitumor action mediated by both direct tumor cell killing and modulation of the innate immune response in some tumors such as nonsmall cell lung cancer. We utilized our knowledge of MERTK inhibitors and a structure-based drug design approach to discover a novel class of macrocyclic dual MERTK/AXL inhibitors. The lead compound

Indexed as

Carcinoma, Non-Small-Cell LungLung NeoplasmsAxl Receptor Tyrosine KinaseCell Line, Tumorc-Mer Tyrosine KinaseHumansProto-Oncogene ProteinsAxl Receptor Tyrosine Kinasec-Mer Tyrosine KinaseMERTK protein, humanProto-Oncogene Proteins

Identifiers

PMID38556760
PMCPMC11627231
OpenAlexW4393363878

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.