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Perturbation-Based Proteomic Correlation Profiling as a Target Deconvolution Methodology.

Authors :
Ohki Y
Sakurai H
Hoshino M
Terashima H
Shimizu H
Ishikawa T
Ogiyama T
Muramatsu Y
Nakanishi T
Miyazaki S
Tsuruoka H
Kobayashi H
Kubota K
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.)

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