A proteomic landscape of pharmacologic perturbations for functional relevance

Pharmacological perturbation studies based on protein-level signatures are fundamental for drug discovery. In the present study, we used a mass spectrometry (MS)-based proteomic platform to profile the whole proteome of the breast cancer MCF7 cell line under stress induced by 78 bioactive compounds....

Full description

Saved in:
Bibliographic Details
Published inJournal of pharmaceutical analysis Vol. 14; no. 1; pp. 128 - 139
Main Authors Liu, Zhiwei, Jiang, Shangwen, Hao, Bingbing, Xie, Shuyu, Liu, Yingluo, Huang, Yuqi, Xu, Heng, Luo, Cheng, Huang, Min, Tan, Minjia, Xu, Jun-Yu
Format Journal Article
LanguageEnglish
Published Xi'an Xi'an Jiaotong University, Journal of Pharmaceutical Analysis 01.01.2024
Subjects
Bioactive compounds
Breast cancer
Cancer therapies
Chromatography
Datasets
Enzymes
Histone methyltransferase
Lovastatin
Mass spectrometry
Mass spectroscopy
Peptides
Phenolic compounds
Proteins
Proteomes
Proteomics
Scientific imaging
Xanthohumol
Beijing China
United States > US
China
Online AccessGet full text

Cover

More Information
Summary:Pharmacological perturbation studies based on protein-level signatures are fundamental for drug discovery. In the present study, we used a mass spectrometry (MS)-based proteomic platform to profile the whole proteome of the breast cancer MCF7 cell line under stress induced by 78 bioactive compounds. The integrated analysis of perturbed signal abundance revealed the connectivity between phenotypic behaviors and molecular features in cancer cells. Our data showed functional relevance in exploring the novel pharmacological activity of phenolic xanthohumol, as well as the noncanonical targets of clinically approved tamoxifen, lovastatin, and their derivatives. Furthermore, the rational design of synergistic inhibition using a combination of histone methyltransferase and topoisomerase was identified based on their complementary drug fingerprints. This study provides rich resources for the proteomic landscape of drug responses for precision therapeutic medicine.
ISSN:2095-1779
2214-0883
DOI:10.1016/jjpha.2023.08.021