Evidence map›Paper›PMID 42885518›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2026

Optimisation and mechanistic characterization of a selective benzoxazine-based MAP4K4 inhibitor in pancreatic cancer cells.

Yi-Wen Wu, Chun-Lin Yang, Yu-Ting Fang-Chin, Yun-Hsuan Yeh, Bor-Jiun Chen, Tzu-Ying Sung, Jung-Chun Chu, Tony Eight Lin, Shih-Chung Yen, Jui-Hua Hsieh and 5 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2026. 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

15 authors.

Yi-Wen WuGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Chun-Lin YangGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Yu-Ting Fang-ChinGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Yun-Hsuan YehGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Bor-Jiun ChenGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Tzu-Ying SungGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Jung-Chun ChuGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Tony Eight LinGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Shih-Chung YenWarshel Institute for Computational Biology, School of Medicine, The Chinese University of Hong Kong (Shenzhen), Shenzhen, Guangdong, China.
Jui-Hua HsiehDivision of Translational Toxicology, National Institute of Environmental Health Sciences, National Institutes of Health, Durham, NC, USA.
Sing-Han HuangDepartment of Digital Biology, Graphen Drugomics Inc., New York, NY, USA.
Cheng-Ying ChuCRISPR Gene Targeting Core, Taipei Medical University, Taipei, Taiwan.
Kai-Chien YangDepartment and Graduate Institute of Pharmacology, National Taiwan University College of Medicine, Taipei, Taiwan.
Kai-Cheng HsuGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.
Shiow-Lin PanGraduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Pancreatic ductal adenocarcinoma (PDAC) remains a lethal malignancy with limited targeted therapeutic options. Mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) has been implicated in PDAC progression, but the development of effective MAP4K4 inhibitors requires further improvement in potency, selectivity, and mechanistic characterisation. We previously identified F389-0746 as a selective benzoxazine-based MAP4K4 inhibitor with anti-cancer activity in pancreatic cancer. Here, we used the F389-0746 scaffold to guide the selection and evaluation of benzoxazine-based analogs, followed by biochemical, structural, selectivity, and cellular characterisation of the most potent analogue. Among the identified analogs, F389-0736 showed the strongest MAP4K4 inhibitory activity, with an IC

Indexed as

Antineoplastic AgentsBenzoxazinesIntracellular Signaling Peptides and ProteinsPancreatic NeoplasmsProtein Kinase InhibitorsProtein Serine-Threonine KinasesApoptosisCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMolecular StructureStructure-Activity RelationshipTumor Cells, CulturedAntineoplastic AgentsBenzoxazinesIntracellular Signaling Peptides and ProteinsMAP4K4 protein, humanProtein Kinase InhibitorsProtein Serine-Threonine Kinasesbenzoxazine-based inhibitorMAP4K4pancreatic cancerstructure-activity relationship

Identifiers

PMID42885518
PMCPMC13678883

What OpenQuestion holds

Textmetadata
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.