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A Guided Materials Screening Approach for Developing Quantitative Sol-gel Derived Protein Microarrays
Published on: August 26, 2013
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Accelerated cellular on- and off-target screening of bioactive compounds using microarrays
Jiaqi Fu1, Zhenkun Na, Bo Peng
1Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
Organic & Biomolecular Chemistry
|November 21, 2015
Summary
This study used 9 drug-like probes for in situ proteome labeling in mammalian cells. The method identified potential drug targets and off-targets by capturing proteins on microarrays and screening with antibodies.
Area of Science:
- Chemical Biology
- Proteomics
- Drug Discovery
Background:
- Understanding cellular targets of drug-like molecules is crucial for drug development.
- In situ methods allow for the study of molecular interactions within a native cellular environment.
Purpose of the Study:
- To develop and apply a novel in situ proteome labeling technique.
- To identify both on- and off-target interactions of drug-like probes within live mammalian cells.
Main Methods:
- In situ proteome labeling of live mammalian cells using 9 distinct drug-like probes.
- Capture of labeled cellular targets onto microarrays.
- Simultaneous screening of captured targets using a diverse antibody set.
Main Results:
- Successful labeling and capture of cellular targets for all 9 probes.
- Identification of potential on-target interactions.
- Detection of potential off-target interactions, providing a comprehensive view of probe activity.
Conclusions:
- The developed in situ proteome labeling method is effective for profiling drug-like probes in live cells.
- This approach facilitates the discovery of specific and non-specific interactions.
- The findings aid in understanding drug mechanisms and potential side effects early in the discovery process.
