PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter

Abstract Ten–eleven translocation protein 1 (TET1) functions as an epigenetic regulatory molecule, mediating the majority of DNA demethylation, and plays a role in the development of different types of cancers by regulating the expression of proto‐oncogenes and oncogenes. Here it is found that TET1...

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Main Authors: Wenzheng Liu, Yiyang Kuai, Da Wang, Junsheng Chen, Fei Xiong, Guanhua Wu, Qi Wang, Wenhua Huang, Yongqiang Qi, Bing Wang, Yongjun Chen
Format: Article
Language:English
Published: Wiley 2024-12-01
Series:Advanced Science
Subjects:
Online Access:https://doi.org/10.1002/advs.202407323
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author Wenzheng Liu
Yiyang Kuai
Da Wang
Junsheng Chen
Fei Xiong
Guanhua Wu
Qi Wang
Wenhua Huang
Yongqiang Qi
Bing Wang
Yongjun Chen
author_facet Wenzheng Liu
Yiyang Kuai
Da Wang
Junsheng Chen
Fei Xiong
Guanhua Wu
Qi Wang
Wenhua Huang
Yongqiang Qi
Bing Wang
Yongjun Chen
author_sort Wenzheng Liu
collection DOAJ
description Abstract Ten–eleven translocation protein 1 (TET1) functions as an epigenetic regulatory molecule, mediating the majority of DNA demethylation, and plays a role in the development of different types of cancers by regulating the expression of proto‐oncogenes and oncogenes. Here it is found that TET1 is highly expressed in cholangiocarcinoma (CCA) and is associated with a poor prognosis. In addition, TET1 promotes claudin‐3 (CLDN3) transcription by targeting the CLDN3 promoter region between −16 and 512 for demethylation. PPM1G functions as a protein dephosphorylase, catalyzing the dephosphorylation of TET1. This results in the destabilization of the TET1 protein, thereby impairing the targeting of the CLDN3 promoter for demethylation. Two phosphatase inhibitors, staurosporine and AZD0156, inhibit epithelial‐to‐mesenchymal transition (EMT) in cholangiocarcinoma cells by suppressing TET1 expression. In conclusion, it is also demonstrated that PPM1G can be employed as a therapeutic target to impede the progression of CCA by catalyzing the dephosphorylation of TET1, which diminishes the capacity of TET1 to target the CLDN3 promoter to activate transcription and inhibit EMT in CCA.
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spelling doaj-art-0d3342047f014f5fa1de10d45c4cacd92025-08-20T01:58:42ZengWileyAdvanced Science2198-38442024-12-011147n/an/a10.1002/advs.202407323PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 PromoterWenzheng Liu0Yiyang Kuai1Da Wang2Junsheng Chen3Fei Xiong4Guanhua Wu5Qi Wang6Wenhua Huang7Yongqiang Qi8Bing Wang9Yongjun Chen10Department of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of General Surgery Beijing Friendship Hospital Capital Medical University Beijing 100050 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of Emergency Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430074 ChinaKey Laboratory of Laparoscopic Technology of Zhejiang Province Department of General Surgery Sir Run‐Run Shaw Hospital Zhejiang University School of Medicine Hangzhou 310016 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaDepartment of Biliary‐Pancreatic Surgery Tongji Hospital Tongji Medical College Huazhong University of Science and Technology 1095 Jiefang Avenue Wuhan Hubei 430030 ChinaAbstract Ten–eleven translocation protein 1 (TET1) functions as an epigenetic regulatory molecule, mediating the majority of DNA demethylation, and plays a role in the development of different types of cancers by regulating the expression of proto‐oncogenes and oncogenes. Here it is found that TET1 is highly expressed in cholangiocarcinoma (CCA) and is associated with a poor prognosis. In addition, TET1 promotes claudin‐3 (CLDN3) transcription by targeting the CLDN3 promoter region between −16 and 512 for demethylation. PPM1G functions as a protein dephosphorylase, catalyzing the dephosphorylation of TET1. This results in the destabilization of the TET1 protein, thereby impairing the targeting of the CLDN3 promoter for demethylation. Two phosphatase inhibitors, staurosporine and AZD0156, inhibit epithelial‐to‐mesenchymal transition (EMT) in cholangiocarcinoma cells by suppressing TET1 expression. In conclusion, it is also demonstrated that PPM1G can be employed as a therapeutic target to impede the progression of CCA by catalyzing the dephosphorylation of TET1, which diminishes the capacity of TET1 to target the CLDN3 promoter to activate transcription and inhibit EMT in CCA.https://doi.org/10.1002/advs.202407323cholangiocarcinomademethylationdephosphorylationPPM1GTET1
spellingShingle Wenzheng Liu
Yiyang Kuai
Da Wang
Junsheng Chen
Fei Xiong
Guanhua Wu
Qi Wang
Wenhua Huang
Yongqiang Qi
Bing Wang
Yongjun Chen
PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter
Advanced Science
cholangiocarcinoma
demethylation
dephosphorylation
PPM1G
TET1
title PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter
title_full PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter
title_fullStr PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter
title_full_unstemmed PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter
title_short PPM1G Inhibits Epithelial–Mesenchymal Transition in Cholangiocarcinoma by Catalyzing TET1 Dephosphorylation for Destabilization to Impair Its Targeted Demethylation of the CLDN3 Promoter
title_sort ppm1g inhibits epithelial mesenchymal transition in cholangiocarcinoma by catalyzing tet1 dephosphorylation for destabilization to impair its targeted demethylation of the cldn3 promoter
topic cholangiocarcinoma
demethylation
dephosphorylation
PPM1G
TET1
url https://doi.org/10.1002/advs.202407323
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