Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation

Abstract The magnitude of Type I interferon (IFN) mediated innate immune response within the tumor microenvironment (TME) critically influences the effectiveness of radiotherapy. Unfortunately, due to a myriad of resistance mechanisms, the double‐stranded DNA (dsDNA) signals produced by tumor cells...

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Main Authors: Weilin Zhou, Yuxuan Zhao, Wenjing Qin, Weijian Wu, Chenyang Liao, Yiqiu Zhang, Xingli Yang, Xue Chen, Youqiao Wang, Yushan Kang, Jiaxin Wu, Jiaojiao Zhao, Junmin Quan, Xuecen Wang, Xianzhang Bu, Xin Yue
Format: Article
Language:English
Published: Wiley 2025-04-01
Series:Advanced Science
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Online Access:https://doi.org/10.1002/advs.202412687
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author Weilin Zhou
Yuxuan Zhao
Wenjing Qin
Weijian Wu
Chenyang Liao
Yiqiu Zhang
Xingli Yang
Xue Chen
Youqiao Wang
Yushan Kang
Jiaxin Wu
Jiaojiao Zhao
Junmin Quan
Xuecen Wang
Xianzhang Bu
Xin Yue
author_facet Weilin Zhou
Yuxuan Zhao
Wenjing Qin
Weijian Wu
Chenyang Liao
Yiqiu Zhang
Xingli Yang
Xue Chen
Youqiao Wang
Yushan Kang
Jiaxin Wu
Jiaojiao Zhao
Junmin Quan
Xuecen Wang
Xianzhang Bu
Xin Yue
author_sort Weilin Zhou
collection DOAJ
description Abstract The magnitude of Type I interferon (IFN) mediated innate immune response within the tumor microenvironment (TME) critically influences the effectiveness of radiotherapy. Unfortunately, due to a myriad of resistance mechanisms, the double‐stranded DNA (dsDNA) signals produced by tumor cells postradiotherapy often induce a diminished response from immune cells. Through chemical screening targeting deubiquitinating enzymes, we identified USP1 (Ubiquitin Specific Peptidase 1) inhibitor as an enhancer of post‐radiotherapy dsDNA responses. Mechanistically, within the context of immune‐stimulatory cells in TME, USP1 serves as a suppressor in the stress‐mediated stages of the cGAS (Cyclic GMP‐AMP synthase) ‐STING (Stimulator of interferon genes protein) signaling pathway, specifically affecting the trafficking of STING from endoplasmic reticulum to Golgi apparatus. It is elucidated that SAR1A (Secretion associated Ras related GTPase 1A) requires K27‐linked oligo‐ubiquitination to assemble the STING‐COP‐II (Coat protein II) transport complex for STING trafficking. USP1 counteracts this activation by removing SAR1A ubiquitination, thereby blocking STING trafficking and activation. Consequently, pharmacological USP1 inhibition using ML323 sustains SAR1A ubiquitination and COP‐II complex formation, significantly enhancing STING trafficking and subsequent Type I IFN production. This intervention substantially amplifies radiotherapy‐induced immune activation in the TME, providing a strategic approach to overcome therapeutic resistance and synergize radiotherapy with immunotherapies.
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spelling doaj-art-3ec5addfa24e4febad8f5ae106a8b3e42025-08-20T03:18:05ZengWileyAdvanced Science2198-38442025-04-011215n/an/a10.1002/advs.202412687Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and ActivationWeilin Zhou0Yuxuan Zhao1Wenjing Qin2Weijian Wu3Chenyang Liao4Yiqiu Zhang5Xingli Yang6Xue Chen7Youqiao Wang8Yushan Kang9Jiaxin Wu10Jiaojiao Zhao11Junmin Quan12Xuecen Wang13Xianzhang Bu14Xin Yue15School of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaThe First Affiliated Hospital Jinan University Guangzhou Guangdong 510630 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaDepartment of Radiation Oncology The First Affiliated Hospital Sun Yat‐sen University Guangzhou Guangdong 510080 ChinaState Key Laboratory of Oncology in South China Guangdong Provincial Clinical Research Center for Cancer Sun Yat‐sen University Cancer Center Guangzhou Guangdong 510257 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaState Key Laboratory of Oncology in South China Guangdong Provincial Clinical Research Center for Cancer Sun Yat‐sen University Cancer Center Guangzhou Guangdong 510257 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaLaboratory of Chemical Oncogenomics Guangdong Provincial Key Laboratory of Chemical Genomics Peking University Shenzhen Graduate School Shenzhen Guangdong 518072 ChinaDepartment of Radiation Oncology The First Affiliated Hospital Sun Yat‐sen University Guangzhou Guangdong 510080 ChinaSchool of Pharmaceutical Sciences Sun Yat‐Sen University Guangzhou Guangdong 510006 ChinaThe First Affiliated Hospital Jinan University Guangzhou Guangdong 510630 ChinaAbstract The magnitude of Type I interferon (IFN) mediated innate immune response within the tumor microenvironment (TME) critically influences the effectiveness of radiotherapy. Unfortunately, due to a myriad of resistance mechanisms, the double‐stranded DNA (dsDNA) signals produced by tumor cells postradiotherapy often induce a diminished response from immune cells. Through chemical screening targeting deubiquitinating enzymes, we identified USP1 (Ubiquitin Specific Peptidase 1) inhibitor as an enhancer of post‐radiotherapy dsDNA responses. Mechanistically, within the context of immune‐stimulatory cells in TME, USP1 serves as a suppressor in the stress‐mediated stages of the cGAS (Cyclic GMP‐AMP synthase) ‐STING (Stimulator of interferon genes protein) signaling pathway, specifically affecting the trafficking of STING from endoplasmic reticulum to Golgi apparatus. It is elucidated that SAR1A (Secretion associated Ras related GTPase 1A) requires K27‐linked oligo‐ubiquitination to assemble the STING‐COP‐II (Coat protein II) transport complex for STING trafficking. USP1 counteracts this activation by removing SAR1A ubiquitination, thereby blocking STING trafficking and activation. Consequently, pharmacological USP1 inhibition using ML323 sustains SAR1A ubiquitination and COP‐II complex formation, significantly enhancing STING trafficking and subsequent Type I IFN production. This intervention substantially amplifies radiotherapy‐induced immune activation in the TME, providing a strategic approach to overcome therapeutic resistance and synergize radiotherapy with immunotherapies.https://doi.org/10.1002/advs.202412687K27‐Ubn‐SAR1AradiotherapySTING trafficking and activationtargeting USP1Type I IFNs
spellingShingle Weilin Zhou
Yuxuan Zhao
Wenjing Qin
Weijian Wu
Chenyang Liao
Yiqiu Zhang
Xingli Yang
Xue Chen
Youqiao Wang
Yushan Kang
Jiaxin Wu
Jiaojiao Zhao
Junmin Quan
Xuecen Wang
Xianzhang Bu
Xin Yue
Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation
Advanced Science
K27‐Ubn‐SAR1A
radiotherapy
STING trafficking and activation
targeting USP1
Type I IFNs
title Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation
title_full Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation
title_fullStr Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation
title_full_unstemmed Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation
title_short Targeting USP1 Potentiates Radiation‐Induced Type I IFN‐Dependent Antitumor Immunity by Enhancing Oligo‐Ubiquitinated SAR1A‐Mediated STING Trafficking and Activation
title_sort targeting usp1 potentiates radiation induced type i ifn dependent antitumor immunity by enhancing oligo ubiquitinated sar1a mediated sting trafficking and activation
topic K27‐Ubn‐SAR1A
radiotherapy
STING trafficking and activation
targeting USP1
Type I IFNs
url https://doi.org/10.1002/advs.202412687
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