Evidence map›Paper›PMID 39723919›Full record

ArticleJournal of medicinal chemistry2025

Targeting Oncogenic RET Kinase by Simultaneously Inhibiting Kinase Activity and Degrading the Protein.

Yafeng Wang, Xueqing Hu, Shriya Pandey, Ujjwol Khatri, Tao Shen, Vivek Subbiah, Blaine H M Mooers, Ting Chao, Shaohui Wang, Huaxuan Yu and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. 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

13 authors.

Yafeng WangDepartment of Chemistry, University of South Florida, Tampa, Florida 33620, United States.
Xueqing HuPeggy and Charles Stephenson Cancer Center and Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma 73104, United States.
Shriya PandeyPeggy and Charles Stephenson Cancer Center and Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma 73104, United States.
Ujjwol KhatriPeggy and Charles Stephenson Cancer Center and Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma 73104, United States.
Tao ShenPeggy and Charles Stephenson Cancer Center and Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma 73104, United States.
Vivek SubbiahEarly-Phase Drug Development, Sarah Cannon Research Institute, Nashville, Tennessee 37203, United States.
Blaine H M MooersPeggy and Charles Stephenson Cancer Center and Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma 73104, United States.ORCID 0000-0001-8181-8987
Ting ChaoDepartment of Chemistry, University of South Florida, Tampa, Florida 33620, United States.
Shaohui WangDepartment of Molecular Medicine, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612, United States.
Huaxuan YuDepartment of Chemistry, University of South Florida, Tampa, Florida 33620, United States.
Xingmin SunDepartment of Molecular Medicine, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612, United States.
Jie WuPeggy and Charles Stephenson Cancer Center and Department of Pathology, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma 73104, United States.
Jianfeng CaiDepartment of Chemistry, University of South Florida, Tampa, Florida 33620, United States.ORCID 0000-0003-3106-3306

Funding

Tissue Pathology Shared ResourceP30CA225520 · NCI · UNIVERSITY OF OKLAHOMA HLTH SCIENCES CTR · PI Wade Williams · 2018 to 2026
$27.1M
TUMOR RESISTANCE MECHANISMS TO ANTI-VEGF THERAPY IN PROSTATE CANCER (Sukyung Woo)P20GM103639 · NIGMS · UNIVERSITY OF OKLAHOMA HLTH SCIENCES CTR · PI DHANASEKARAN, DANNY N. · 2012 to 2022
$21.3M
Supplement for Google cloud build-outR24GM137786 · NIGMS · UNIV OF ARKANSAS FOR MED SCIS · PI Alan Tackett · 2020 to 2026
$15.4M
Protein Production and Characterization CoreP30GM145423 · NIGMS · UNIVERSITY OF OKLAHOMA · PI ANN H WEST · 2022 to 2026
$6.9M
Blocking tumor progression in therapy-responsive RET aberration-associated cancerR01CA242845 · NCI · UNIVERSITY OF OKLAHOMA HLTH SCIENCES CTR · PI AHNERT, JORDI RODON, MOOERS, BLAINE H. M. · 2020 to 2024
$1.9M
Novel polymer biomaterials combating C. difficile infectionR01AI149852 · NIAID · UNIVERSITY OF SOUTH FLORIDA · PI CAI, JIANFENG, SUN, XINGMIN · 2019 to 2023
$1.9M
Targeting Wnt signaling pathwayR01GM150196 · NIGMS · UNIVERSITY OF SOUTH FLORIDA · PI Jianfeng Cai · 2023 to 2026
$1.7M
NCI NIH HHS P30 CA225520NCI NIH HHS R01 CA242845NIAID NIH HHS R01 AI149852NIGMS NIH HHS P20 GM103639NIGMS NIH HHS P30 GM145423NIGMS NIH HHS R01 GM150196NIGMS NIH HHS R24 GM137786
6 · The paper itself

Abstract

The rearranged-during-transfection (RET) kinase is a validated target for the treatment of RET-altered cancers. Currently approved RET-selective kinase inhibitors, selpercatinib (LOXO-292) and pralsetinib (BLU-667), increase the oncogenic RET protein level upon treatment, which may affect their efficacy. We seek to reduce the oncogenic RET protein level and RET kinase activity simultaneously. Here, we report the development of proteolysis targeting chimera (PROTAC) degraders of oncogenic RET protein. Compound

Indexed as

Protein Kinase InhibitorsProto-Oncogene Proteins c-retAnimalsAntineoplastic AgentsCell Line, TumorFemaleHumansMiceMice, NudeProteolysisPyrazolesXenograft Model Antitumor AssaysAntineoplastic AgentsProtein Kinase InhibitorsProto-Oncogene Proteins c-retPyrazolesRET protein, human

Identifiers

PMID39723919
PMCPMC12874623

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.