Evidence map›Paper›PMID 30188734›Full record

ArticleJournal of medicinal chemistry2019

Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.

Wei Yan, Naga Rajiv Lakkaniga, Francesca Carlomagno, Massimo Santoro, Neil Q McDonald, Fengping Lv, Naresh Gunaganti, Brendan Frett, Hong-Yu Li

Erratum issuedAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. 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 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing 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

24 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Article
  6. Pyrazolo[1,5-Molecules (Basel, Switzerland) · 2024
    Review
  7. Review
  8. Article
  9. Review
  10. Review
  11. Article
  12. Article
  13. Article
  14. Article
  15. Review
  16. Review
  17. In Pursuit of an Allosteric Human Tropomyosin Kinase A (ACS medicinal chemistry letters · 2021
    Article
  18. Article
  19. Review
  20. Azaindole therapeutic agents.Bioorganic & medicinal chemistry · 2020
    Article
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

9 authors.

Wei YanDepartment of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.
Naga Rajiv LakkanigaDepartment of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.
Francesca CarlomagnoDipartimento di Medicina Molecolare e Biotecnologie Mediche , Università Federico II , Via S Pansini 5 , 80131 Naples , Italy.
Massimo SantoroDipartimento di Medicina Molecolare e Biotecnologie Mediche , Università Federico II , Via S Pansini 5 , 80131 Naples , Italy.
Neil Q McDonaldSignaling and Structural Biology Laboratory , The Francis Crick Institute , London NW1 1AT , U.K.
Fengping LvDepartment of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.
Naresh GunagantiDepartment of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.ORCID 0000-0001-8149-9795
Brendan FrettDepartment of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.
Hong-Yu LiDepartment of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.ORCID 0000-0001-9212-2010

Funding

Selective RET Kinase and Its Mutant Inhibitors for the Treatment of Medullary Thyroid CancerR01CA197178 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI LI, HONG-YU, MCDONALD, NEIL · 2015 to 2019
$1.5M
Discovery and Development of a Selective pan-FLT3-ITD Kinase Inhibitor Clinical Candidate for the Treatment of FLT3-ITD-Driven AMLR01CA194094 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI LI, HONG-YU, SHAH, NEIL P · 2015 to 2018
$1.5M
NCI NIH HHS R01 CA194094NCI NIH HHS R01 CA197178
6 · The paper itself

Abstract

The use of kinase-directed precision medicine has been heavily pursued since the discovery and development of imatinib. Annually, it is estimated that around ∼20 000 new cases of tropomyosin receptor kinase (TRK) cancers are diagnosed, with the majority of cases exhibiting a TRK genomic rearrangement. In this Perspective, we discuss current development and clinical applications for TRK precision medicine by providing the following: (1) the biological background and significance of the TRK kinase family, (2) a compilation of known TRK inhibitors and analysis of their cocrystal structures, (3) an overview of TRK clinical trials, and (4) future perspectives for drug discovery and development of TRK inhibitors.

Indexed as

AnimalsAntineoplastic AgentsCatalytic DomainCell Line, TumorDrug DiscoveryHumansMice, Inbred BALB CNeoplasmsPrecision MedicineProtein Kinase InhibitorsRats, Sprague-DawleyReceptor, trkAReceptor, trkBReceptor, trkCAntineoplastic AgentsProtein Kinase InhibitorsReceptor, trkAReceptor, trkBReceptor, trkC

Identifiers

PMID30188734
PMCPMC7875308

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Registered trials

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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.