Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA

Abstract Protein phosphorylation plays a crucial role in regulating disease phenotypes and serves as a key target for drug development. Mapping nanoscale‐to‐single‐cell samples can unravel the heterogeneity of cellular signaling events. However, it remains a formidable analytical challenge due to th...

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Main Authors: Gul Muneer, Sofani Tafesse Gebreyesus, Ciao‐Syuan Chen, Tzu‐Tsung Lee, Fengchao Yu, Chih‐An Lin, Min‐Shu Hsieh, Alexey I. Nesvizhskii, Chao‐Chi Ho, Sung‐Liang Yu, Hsiung‐Lin Tu, Yu‐Ju Chen
Format: Article
Language:English
Published: Wiley 2025-01-01
Series:Advanced Science
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Online Access:https://doi.org/10.1002/advs.202402421
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author Gul Muneer
Sofani Tafesse Gebreyesus
Ciao‐Syuan Chen
Tzu‐Tsung Lee
Fengchao Yu
Chih‐An Lin
Min‐Shu Hsieh
Alexey I. Nesvizhskii
Chao‐Chi Ho
Sung‐Liang Yu
Hsiung‐Lin Tu
Yu‐Ju Chen
author_facet Gul Muneer
Sofani Tafesse Gebreyesus
Ciao‐Syuan Chen
Tzu‐Tsung Lee
Fengchao Yu
Chih‐An Lin
Min‐Shu Hsieh
Alexey I. Nesvizhskii
Chao‐Chi Ho
Sung‐Liang Yu
Hsiung‐Lin Tu
Yu‐Ju Chen
author_sort Gul Muneer
collection DOAJ
description Abstract Protein phosphorylation plays a crucial role in regulating disease phenotypes and serves as a key target for drug development. Mapping nanoscale‐to‐single‐cell samples can unravel the heterogeneity of cellular signaling events. However, it remains a formidable analytical challenge due to the low detectability, abundance, and stoichiometry of phosphorylation sites. Here, we present a Chip‐DIA strategy, integrating a microfluidic‐based phosphoproteomic chip (iPhosChip) with data‐independent acquisition mass spectrometry (DIA‐MS) for ultrasensitive nanoscale‐to‐single‐cell phosphoproteomic profiling. The iPhosChip operates as an all‐in‐one station that accommodates both quantifiable cell capture/imaging and the entire phosphoproteomic workflow in a highly streamlined and multiplexed manner. Coupled with a sample size‐comparable library‐based DIA‐MS strategy, Chip‐DIA achieved ultra‐high sensitivity, detecting 1076±158 to 15869±1898 phosphopeptides from 10±0 to 1013±4 cells, and revealed the first single‐cell phosphoproteomic landscape comprising druggable sites and basal phosphorylation‐mediated networks in lung cancer. Notably, the sensitivity and coverage enabled the illumination of heterogeneous cytoskeleton remodeling and cytokeratin signatures in patient‐derived cells resistant to third‐generation EGFR therapy, stratifying mixed‐lineage adenocarcinoma‐squamous cell carcinoma subtypes, and identifying alternative targeted therapy for late‐stage patients. With flexibility in module design and functionalization, Chip‐DIA can be adapted to other PTM‐omics to explore dysregulated PTM landscapes, thereby guiding therapeutic strategies toward precision oncology.
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spelling doaj-art-d8e21484a4a4423196bd8d05457c08e02025-08-20T02:47:33ZengWileyAdvanced Science2198-38442025-01-01121n/an/a10.1002/advs.202402421Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIAGul Muneer0Sofani Tafesse Gebreyesus1Ciao‐Syuan Chen2Tzu‐Tsung Lee3Fengchao Yu4Chih‐An Lin5Min‐Shu Hsieh6Alexey I. Nesvizhskii7Chao‐Chi Ho8Sung‐Liang Yu9Hsiung‐Lin Tu10Yu‐Ju Chen11Institute of Chemistry Academia Sinica Taipei 115201 TaiwanInstitute of Chemistry Academia Sinica Taipei 115201 TaiwanInstitute of Chemistry Academia Sinica Taipei 115201 TaiwanInstitute of Chemistry Academia Sinica Taipei 115201 TaiwanDepartment of Pathology University of Michigan Ann Arbor MI 48109 USADepartment of Internal Medicine National Taiwan University Hospital Taipei 10051 TaiwanDepartment of Pathology National Taiwan University Cancer Center Taipei 10617 TaiwanDepartment of Pathology University of Michigan Ann Arbor MI 48109 USADepartment of Internal Medicine National Taiwan University Hospital Taipei 10051 TaiwanDepartment of Clinical Laboratory Science and Medical Biotechnology College of Medicine National Taiwan University Taipei 10048 TaiwanInstitute of Chemistry Academia Sinica Taipei 115201 TaiwanInstitute of Chemistry Academia Sinica Taipei 115201 TaiwanAbstract Protein phosphorylation plays a crucial role in regulating disease phenotypes and serves as a key target for drug development. Mapping nanoscale‐to‐single‐cell samples can unravel the heterogeneity of cellular signaling events. However, it remains a formidable analytical challenge due to the low detectability, abundance, and stoichiometry of phosphorylation sites. Here, we present a Chip‐DIA strategy, integrating a microfluidic‐based phosphoproteomic chip (iPhosChip) with data‐independent acquisition mass spectrometry (DIA‐MS) for ultrasensitive nanoscale‐to‐single‐cell phosphoproteomic profiling. The iPhosChip operates as an all‐in‐one station that accommodates both quantifiable cell capture/imaging and the entire phosphoproteomic workflow in a highly streamlined and multiplexed manner. Coupled with a sample size‐comparable library‐based DIA‐MS strategy, Chip‐DIA achieved ultra‐high sensitivity, detecting 1076±158 to 15869±1898 phosphopeptides from 10±0 to 1013±4 cells, and revealed the first single‐cell phosphoproteomic landscape comprising druggable sites and basal phosphorylation‐mediated networks in lung cancer. Notably, the sensitivity and coverage enabled the illumination of heterogeneous cytoskeleton remodeling and cytokeratin signatures in patient‐derived cells resistant to third‐generation EGFR therapy, stratifying mixed‐lineage adenocarcinoma‐squamous cell carcinoma subtypes, and identifying alternative targeted therapy for late‐stage patients. With flexibility in module design and functionalization, Chip‐DIA can be adapted to other PTM‐omics to explore dysregulated PTM landscapes, thereby guiding therapeutic strategies toward precision oncology.https://doi.org/10.1002/advs.202402421library DIAlung cancermicrofluidicsphosphorylationsingle‐cell phosphoproteomics
spellingShingle Gul Muneer
Sofani Tafesse Gebreyesus
Ciao‐Syuan Chen
Tzu‐Tsung Lee
Fengchao Yu
Chih‐An Lin
Min‐Shu Hsieh
Alexey I. Nesvizhskii
Chao‐Chi Ho
Sung‐Liang Yu
Hsiung‐Lin Tu
Yu‐Ju Chen
Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA
Advanced Science
library DIA
lung cancer
microfluidics
phosphorylation
single‐cell phosphoproteomics
title Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA
title_full Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA
title_fullStr Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA
title_full_unstemmed Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA
title_short Mapping Nanoscale‐To‐Single‐Cell Phosphoproteomic Landscape by Chip‐DIA
title_sort mapping nanoscale to single cell phosphoproteomic landscape by chip dia
topic library DIA
lung cancer
microfluidics
phosphorylation
single‐cell phosphoproteomics
url https://doi.org/10.1002/advs.202402421
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