Evidence map›Paper›PMID 40478495›Full record

ArticleMolecular biomedicine2025

The EZH2 selective inhibitor ZLD1039 attenuates UUO-induced renal fibrosis by suppressing YAP activation.

Qingling Xia, Fujiang Xu, Lidan Zhang, Wenfei Ding, Jiang Liu, Jing Liu, Minhao Chen, Santao Ou, Yong Xu, Li Wen

Abstract read
In one paragraph

Article in Molecular biomedicine, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

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

10 authors.

Qingling Xia *Department of Nephrology, Sichuan Clinical Research Center for Nephropathy and Metabolic Vascular Diseases Key Laboratory of Sichuan Province, The Affiliated Hospital of Southwest Medical University, Luzhou, China.
Fujiang Xu *Department of Oncology, The Affiliated Hospital of Southwest Medical University, Luzhou, China.
Lidan ZhangLaboratory of Anesthesia & Critical Care Medicine, Translational Neuroscience Center, West China Hospital of Sichuan University, Chengdu, China.
Wenfei DingDepartment of Nephrology, Sichuan Clinical Research Center for Nephropathy and Metabolic Vascular Diseases Key Laboratory of Sichuan Province, The Affiliated Hospital of Southwest Medical University, Luzhou, China.
Jiang LiuDepartment of Nephrology, Sichuan Clinical Research Center for Nephropathy and Metabolic Vascular Diseases Key Laboratory of Sichuan Province, The Affiliated Hospital of Southwest Medical University, Luzhou, China.
Jing LiuDepartment of Urology, The Affiliated Hospital of Southwest Medical University, Luzhou, China.
Minhao ChenClinical Medical College, Southwest Medical University, Luzhou, China.
Santao OuDepartment of Nephrology, Sichuan Clinical Research Center for Nephropathy and Metabolic Vascular Diseases Key Laboratory of Sichuan Province, The Affiliated Hospital of Southwest Medical University, Luzhou, China. ousantao@163.com.
Yong XuDepartment of Endocrinology and Metabolism, The Affiliated Hospital of Southwest Medical University, Luzhou, China. xywyll@swmu.edu.cn.
Li WenDepartment of Nephrology, Sichuan Clinical Research Center for Nephropathy and Metabolic Vascular Diseases Key Laboratory of Sichuan Province, The Affiliated Hospital of Southwest Medical University, Luzhou, China. wenlixnydfy@163.com.

Funding

China Postdoctoral Science Foundation 2023M742905Luzhou Science and Technology Bureau 2023JYJ018Luzhou Science and Technology Program 2023JYJ008Natural Science Foundation of Sichuan Province 2023NSFSC1530School-Level Scientific Research Project of the Southwest Medical University 2022ZD005
6 · The paper itself

Abstract

Renal fibrosis is a manifestation of the progression of chronic kidney disease (CKD) and chronic inflammation is a main driver in the development of renal fibrosis. Yes-associated protein (YAP), acting as a transcriptional co-activator within the Hippo signaling pathway, has been implicated in renal fibrosis. Enhancer of zeste homolog 2 (EZH2) exhibits high expression level in renal fibrosis induced by unilateral ureteral obstruction (UUO), yet the interplay between YAP and EZH2 in renal fibrosis remains to be elucidated. ZLD1039, a selective inhibitor of EZH2, has demonstrated protective effects against cancer and acute kidney injury (AKI). In this study, we conducted a systemic pharmacological investigation to determine if ZLD1039 treatment mitigates UUO-induced renal inflammation and fibrosis through modulation of the Hippo-YAP pathway. Our results revealed that UUO triggered renal inflammation and collagen deposition, with significant activation of YAP. Notably, ZLD1039 treatment effectively alleviated renal inflammation and fibrosis, while inhibiting the expression and nuclear translocation of YAP. Mechanically, we observed a notable down-regulation of large tumor suppressor homolog 1 (LATS1) in parallel with the up-regulation of EZH2. Furthermore, inhibition of EZH2 by ZLD1039 was linked to the up-regulation of LATS1 expression and YAP inactivation. Similarly, in vitro pharmacological inhibition of EZH2 by ZLD1039 resulted in elevated LATS1 expression and diminished YAP activation. Collectively, our findings suggest that ZLD1039, a selective inhibitor of EZH2, likely attenuates renal inflammation and fibrosis probably by up-regulating LATS1 and inhibiting YAP activation. This mechanistic link between EZH2 and YAP provides a fresh perspective on treating renal fibrosis.

Indexed as

Adaptor Proteins, Signal TransducingEnhancer of Zeste Homolog 2 ProteinKidneyKidney DiseasesUreteral ObstructionAnimalsCell Cycle ProteinsFibrosisMaleMiceMice, Inbred C57BLProtein Serine-Threonine KinasesSignal TransductionTranscription FactorsYAP-Signaling ProteinsAdaptor Proteins, Signal TransducingCell Cycle ProteinsEnhancer of Zeste Homolog 2 ProteinProtein Serine-Threonine KinasesTranscription FactorsYap1 protein, mouseYAP-Signaling ProteinsEnhancer of zeste homolog 2InflammationLarge tumor suppressor 1Renal fibrosisYes-associated protein 1

Identifiers

PMID40478495
PMCPMC12144025

What Socratic 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 Socratic graph.