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Protease-Responsive Potential-Tunable AIEgens for Cell Selective Imaging of TMPRSS2 and Accurate Inhibitor Screening.
Cheng, Yong; Clark, Alex E; Yim, Wonjun; Borum, Raina M; Chang, Yu-Ci; Jin, Zhicheng; He, Tengyu; Carlin, Aaron F; Jokerst, Jesse V.
  • Cheng Y; Department of NanoEngineering, University of California, San Diego, La Jolla, California 92093, United States.
  • Clark AE; Department of Medicine, University of California, San Diego, La Jolla, California 92093, United States.
  • Yim W; Materials Science and Engineering Program, University of California, San Diego, La Jolla, California 92093, United States.
  • Borum RM; Department of NanoEngineering, University of California, San Diego, La Jolla, California 92093, United States.
  • Chang YC; Materials Science and Engineering Program, University of California, San Diego, La Jolla, California 92093, United States.
  • Jin Z; Department of NanoEngineering, University of California, San Diego, La Jolla, California 92093, United States.
  • He T; Materials Science and Engineering Program, University of California, San Diego, La Jolla, California 92093, United States.
  • Carlin AF; Department of Medicine, University of California, San Diego, La Jolla, California 92093, United States.
  • Jokerst JV; Department of Pathology, University of California, San Diego, La Jolla, California 92093, United States.
Anal Chem ; 95(7): 3789-3798, 2023 02 21.
Article in English | MEDLINE | ID: covidwho-2254734
ABSTRACT
Transmembrane protease serine 2 (TMPRSS2) is a plasma membrane protease that activates both spike protein of coronaviruses for cell entry and oncogenic signaling pathways for tumor progression. TMPRSS2 inhibition can reduce cancer invasion and metastasis and partially prevent the entry of SARS-CoV-2 into host cells. Thus, there is an urgent need for both TMPRSS2-selective imaging and precise screening of TMPRSS2 inhibitors. Here, we report a TMPRSS2-responsive surface-potential-tunable peptide-conjugated probe (EGTP) with aggregation-induced emission (AIE) features for TMPRSS2 selective imaging and accurate inhibitor screening. The amphiphilic EGTP was constructed with tunable surface potential and responsive efficiency with TMPRSS2 and its inhibitor. The rational construction of AIE luminogens (AIEgens) with modular peptides indicated that the cleavage of EGTP led to a gradual aggregation with bright fluorescence in high TMPRSS2-expressing cells. This strategy may have value for selective detection of cancer cells, SARS-CoV-2-target cells, and screening of protease inhibitors.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Peptide Hydrolases / COVID-19 Type of study: Diagnostic study Limits: Humans Language: English Journal: Anal Chem Year: 2023 Document Type: Article Affiliation country: Acs.analchem.2c04988

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Peptide Hydrolases / COVID-19 Type of study: Diagnostic study Limits: Humans Language: English Journal: Anal Chem Year: 2023 Document Type: Article Affiliation country: Acs.analchem.2c04988