Evidence map›Paper›PMID 35081714›Full record

ArticleJournal of medicinal chemistry2022

Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.

Lingtian Zhang, Marialuisa Moccia, David C Briggs, Jaideep B Bharate, Naga Rajiv Lakkaniga, Phillip Knowles, Wei Yan, Phuc Tran, Anupreet Kharbanda, Xiuqi Wang and 6 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
1.7field-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

5 citing papers in PubMed, 16 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Article
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

16 authors at 5 institutions in 3 countries.

Lingtian ZhangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.
Marialuisa MocciaDipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II", 80131 Napoli, Italia.
David C BriggsSignalling and Structural Biology Laboratory, The Francis Crick Institute, London NW1 1AT, U.K.ORCID 0000-0002-9793-7339
Jaideep B BharateDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.ORCID 0000-0003-3269-6228
Naga Rajiv LakkanigaDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, California 92037, United States.
Phillip KnowlesSignalling and Structural Biology Laboratory, The Francis Crick Institute, London NW1 1AT, U.K.
Wei YanDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.ORCID 0000-0003-1535-3100
Phuc TranDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.
Anupreet KharbandaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.
Xiuqi WangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.ORCID 0000-0002-8514-0410
Yuet-Kin LeungDepartment of Pharmacology & Toxicology, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.
Brendan FrettDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205, United States.ORCID 0000-0003-2429-8895
Massimo SantoroDipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II", 80131 Napoli, Italia.
Neil Q McDonaldSignalling and Structural Biology Laboratory, The Francis Crick Institute, London NW1 1AT, U.K.ORCID 0000-0003-0975-6325
Francesca CarlomagnoDipartimento di Medicina Molecolare e Biotecnologie Mediche, Università di Napoli "Federico II", 80131 Napoli, Italia.ORCID 0000-0002-1483-4677
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
University of Arkansas for Medical Sciences · USThe Francis Crick Institute · GBUniversity of Naples Federico II · ITInstitute for Experimental Endocrinology and Oncology · ITScripps Research Institute · US

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
Synactix Pharmaceuticals I-Corps ApplicationR41CA195826 · NCI · SYNACTIX PHARMACEUTICALS, INC. · PI FRETT, BRENDAN ANDREW, LI, HONG-YU · 2015 to 2016
$340k
NCI NIH HHS R01 CA197178NCI NIH HHS R41 CA195826Wellcome Trust FC001115
6 · The paper itself

Abstract

Mutations of the rearranged during transfection (RET) kinase are frequently reported in cancer, which make it as an attractive therapeutic target. Herein, we discovered a series of N-trisubstituted pyrimidine derivatives as potent inhibitors for both wild-type (

Indexed as

MutationAdenocarcinoma of LungApoptosisCell ProliferationHumansLung NeoplasmsProtein Kinase InhibitorsProto-Oncogene Proteins c-retPyrimidinesStructure-Activity RelationshipTumor Cells, CulturedWound HealingProtein Kinase InhibitorsProto-Oncogene Proteins c-retPyrimidinesRET protein, human

Identifiers

PMID35081714
PMCPMC10536133
OpenAlexW4210311274

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.