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Perturbation-Based Proteomic Correlation Profiling as a Target Deconvolution Methodology.
- Source :
-
Cell chemical biology [Cell Chem Biol] 2019 Jan 17; Vol. 26 (1), pp. 137-143.e8. Date of Electronic Publication: 2018 Nov 15. - Publication Year :
- 2019
-
Abstract
- Molecular target identification of small molecules, so-called target deconvolution, is a major obstacle to phenotype-based drug discovery. Here, we developed an approach called perturbation-based proteomic correlation profiling (PPCP) utilizing the correlation between protein quantity and binding activity of compounds under cellular perturbation by gene silencing and successfully identified lanosterol synthase as a molecular target of TGF-β pathway inhibitor. This PPCP concept was extended to the use of a cell line panel and provides a new option for target deconvolution.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Cells, Cultured
Enzyme Inhibitors chemistry
Gene Expression Profiling
Gene Silencing drug effects
Humans
Intramolecular Transferases genetics
Intramolecular Transferases metabolism
Male
Molecular Structure
RNA, Small Interfering pharmacology
Small Molecule Libraries chemistry
Enzyme Inhibitors pharmacology
Intramolecular Transferases antagonists & inhibitors
Proteomics
Small Molecule Libraries pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 2451-9448
- Volume :
- 26
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Cell chemical biology
- Publication Type :
- Academic Journal
- Accession number :
- 30449674
- Full Text :
- https://doi.org/10.1016/j.chembiol.2018.10.012