Evidence map›Paper›PMID 41294372›Full record

ArticleJournal of medicinal chemistry2025

Discovery and Development of a Small-Molecule Inhibitor Targeting the GAS41 YEATS Domain in Nonsmall Cell Lung Cancer.

Dymytrii Listunov, Alyssa Winkler, Joshua Ray, Brian M Linhares, Bradley Clegg, Sidney Weaver, EunGi Kim, Sergei Zari, Se Ra Park, Sergey N Zolov and 6 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. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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.

Dymytrii ListunovDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Alyssa WinklerDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Joshua RayDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Brian M LinharesDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Bradley CleggDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Sidney WeaverDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0001-7446-9870
EunGi KimDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Sergei ZariDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Se Ra ParkDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Sergey N ZolovDepartment of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, United States.
Sergei ChuikovDepartment of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, United States.
Liang ZhaoDepartment of Molecular & Integrative Physiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Yatrik M ShahDepartment of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, United States.
Venkateshwar G KeshamouniDepartment of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, United States.
Jolanta GrembeckaDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0002-6180-9095
Tomasz CierpickiDepartment of Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.ORCID 0000-0003-2058-0658

Funding

Control of iron absorption by intestinal HIF2 in iron and hematological disordersR01DK095201 · NIDDK · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SHAH, YATRIK M · 2012 to 2025
$5.7M
The role of HIF2alpha in colon carcinogenesisR01CA148828 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SHAH, YATRIK M · 2010 to 2025
$5.2M
Development of ASH1L inhibitors for acute leukemiaR01CA244254 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI GREMBECKA, JOLANTA · 2020 to 2024
$2.8M
Targeting Menin in Acute Leukemia with Upregulated HOX GenesR01CA272561 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Jolanta Grembecka · 2023 to 2026
$2.5M
Targeting PRC1 in leukemiaR01CA282082 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Tomasz Cierpicki · 2023 to 2026
$2.5M
Targeting Fibroblast Discoidin Domain Receptor 2 for Immunotherapy to Pulmonary FibrosisR01HL156998 · NHLBI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI KESHAMOUNI, VENKATESHWAR G, KIM, KEVIN KEEWOUN · 2022 to 2025
$2.4M
Understanding the mechanisms of iron addiction in colon cancerR01CA245546 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI SHAH, YATRIK M · 2020 to 2024
$2.3M
Targeting epigenetic reader GAS41R01CA240514 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI CIERPICKI, TOMASZ · 2020 to 2023
$2.0M
Screening for inhibitors of NSD3 as a treatment for lung cancerR01CA276074 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Jolanta Grembecka · 2023 to 2026
$2.0M
Development of chemical probe targeting NSD3 SET domain in breast cancerR01CA285304 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Tomasz Cierpicki · 2024 to 2026
$1.7M
CSRD VA I01 CX002233NCI NIH HHS R01 CA148828NCI NIH HHS R01 CA240514NCI NIH HHS R01 CA244254NCI NIH HHS R01 CA245546NCI NIH HHS R01 CA272561NCI NIH HHS R01 CA276074NCI NIH HHS R01 CA282082NCI NIH HHS R01 CA285304NHLBI NIH HHS R01 HL156998NIDDK NIH HHS R01 DK095201
6 · The paper itself

Abstract

GAS41 is frequently overexpressed in Non-Small Cell Lung Cancer (NSCLC). GAS41 contains a YEATS domain, which recognizes acetylated lysine residues on histones to recruit protein complexes and facilitate transcription. Suppression of GAS41 in NSCLC models inhibits cellular proliferation and markedly reduces tumor growth in mouse xenografts, justifying the development of small-molecule inhibitors. We have employed structure-based design and medicinal chemistry optimization to discover

Indexed as

Antineoplastic AgentsCarcinoma, Non-Small-Cell LungLung NeoplasmsSmall Molecule LibrariesAnimalsCell Line, TumorCell ProliferationDrug DiscoveryHumansMiceProtein DomainsStructure-Activity RelationshipAntineoplastic AgentsSmall Molecule Libraries

Identifiers

PMID41294372
PMCPMC12880737

What OpenQuestion holds

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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.