Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality

Summary: Overexpression of USP7 and HDM2 inactivates P53 signaling in tumor cells and facilitates their progression, but suppression of these targets by conventional strategies to reactivate P53 function remains a challenge. We applied polyQ sequences and target-interacting peptides to engineer poly...

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Main Authors: Xiang-Le Zhang, Hong-Wei Yue, Ya-Jun Liu, Jian-Yang Wang, Heng-Tong Duan, Yin-Hu Liu, Lei-Lei Jiang, Hong-Yu Hu
Format: Article
Language:English
Published: Elsevier 2025-03-01
Series:iScience
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Online Access:http://www.sciencedirect.com/science/article/pii/S2589004225002858
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author Xiang-Le Zhang
Hong-Wei Yue
Ya-Jun Liu
Jian-Yang Wang
Heng-Tong Duan
Yin-Hu Liu
Lei-Lei Jiang
Hong-Yu Hu
author_facet Xiang-Le Zhang
Hong-Wei Yue
Ya-Jun Liu
Jian-Yang Wang
Heng-Tong Duan
Yin-Hu Liu
Lei-Lei Jiang
Hong-Yu Hu
author_sort Xiang-Le Zhang
collection DOAJ
description Summary: Overexpression of USP7 and HDM2 inactivates P53 signaling in tumor cells and facilitates their progression, but suppression of these targets by conventional strategies to reactivate P53 function remains a challenge. We applied polyQ sequences and target-interacting peptides to engineer polyQ fusion proteins that specifically sequester the targets, hence depleting their availabilities and modulating the P53 functionality. We have revealed that the designer fusion Atx793Q-N172-IRF (IRF sequence: SPGEGPSGTG) sequesters USP7 and/or HDM2 into aggregates and thereby increases the P53 level, but it depends on the IRF repeats fused, suggesting that depletion of the USP7 availability plays a dual role in controlling P53 stability. Direct sequestration of HDM2 by Atx793Q-N172-PMI (PMI: TSFAEYWNLLSP) remarkably reduces the protein level of soluble HDM2 and hence increases the P53 level, which consequently up-regulates expression of the downstream genes. The polyQ-fusion strategy is feasible to modulate the P53 stability and functionality, furnishing a therapeutic potential for cancers.
format Article
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institution OA Journals
issn 2589-0042
language English
publishDate 2025-03-01
publisher Elsevier
record_format Article
series iScience
spelling doaj-art-28b95e4d183441eea9f0d2828e4a36ee2025-08-20T02:11:05ZengElsevieriScience2589-00422025-03-0128311202510.1016/j.isci.2025.112025Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionalityXiang-Le Zhang0Hong-Wei Yue1Ya-Jun Liu2Jian-Yang Wang3Heng-Tong Duan4Yin-Hu Liu5Lei-Lei Jiang6Hong-Yu Hu7Key Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; University of Chinese Academy of Sciences, Beijing 100049, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; University of Chinese Academy of Sciences, Beijing 100049, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; University of Chinese Academy of Sciences, Beijing 100049, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; University of Chinese Academy of Sciences, Beijing 100049, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; University of Chinese Academy of Sciences, Beijing 100049, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; University of Chinese Academy of Sciences, Beijing 100049, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. ChinaKey Laboratory of RNA Innovation, Science and Engineering, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, Shanghai 200031, P.R. China; Corresponding authorSummary: Overexpression of USP7 and HDM2 inactivates P53 signaling in tumor cells and facilitates their progression, but suppression of these targets by conventional strategies to reactivate P53 function remains a challenge. We applied polyQ sequences and target-interacting peptides to engineer polyQ fusion proteins that specifically sequester the targets, hence depleting their availabilities and modulating the P53 functionality. We have revealed that the designer fusion Atx793Q-N172-IRF (IRF sequence: SPGEGPSGTG) sequesters USP7 and/or HDM2 into aggregates and thereby increases the P53 level, but it depends on the IRF repeats fused, suggesting that depletion of the USP7 availability plays a dual role in controlling P53 stability. Direct sequestration of HDM2 by Atx793Q-N172-PMI (PMI: TSFAEYWNLLSP) remarkably reduces the protein level of soluble HDM2 and hence increases the P53 level, which consequently up-regulates expression of the downstream genes. The polyQ-fusion strategy is feasible to modulate the P53 stability and functionality, furnishing a therapeutic potential for cancers.http://www.sciencedirect.com/science/article/pii/S2589004225002858BiochemistryProtein structure aspectsCancer
spellingShingle Xiang-Le Zhang
Hong-Wei Yue
Ya-Jun Liu
Jian-Yang Wang
Heng-Tong Duan
Yin-Hu Liu
Lei-Lei Jiang
Hong-Yu Hu
Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality
iScience
Biochemistry
Protein structure aspects
Cancer
title Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality
title_full Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality
title_fullStr Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality
title_full_unstemmed Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality
title_short Designer polyQ fusion proteins sequester USP7/HDM2 for modulating P53 functionality
title_sort designer polyq fusion proteins sequester usp7 hdm2 for modulating p53 functionality
topic Biochemistry
Protein structure aspects
Cancer
url http://www.sciencedirect.com/science/article/pii/S2589004225002858
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