Systems Pharmacology Dissection of Cholesterol Regulation Reveals Determinants of Large Pharmacodynamic Variability between Cell Lines


Date

2017-12

Publication Type

Journal Article

ETH Bibliography

yes

Citations

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Data

Abstract

In individuals, heterogeneous drug-response phenotypes result from a complex interplay of dose, drug specificity, genetic background, and environmental factors, thus challenging our understanding of the underlying processes and optimal use of drugs in the clinical setting. Here, we use mass-spectrometry-based quantification of molecular response phenotypes and logic modeling to explain drug-response differences in a panel of cell lines. We apply this approach to cellular cholesterol regulation, a biological process with high clinical relevance. From the quantified molecular phenotypes elicited by various targeted pharmacologic or genetic treatments, we generated cell-line-specific models that quantified the processes beneath the idiotypic intracellular drug responses. The models revealed that, in addition to drug uptake and metabolism, further cellular processes displayed significant pharmacodynamic response variability between the cell lines, resulting in cell-line-specific drug-response phenotypes. This study demonstrates the importance of integrating different types of quantitative systems-level molecular measurements with modeling to understand the effect of pharmacological perturbations on complex biological processes.

Publication status

published

Editor

Book title

Journal / series

Volume

5 (6)

Pages / Article No.

604 - 6190000000

Publisher

Cell Press

Event

Edition / version

Methods

Software

Geographic location

Date collected

Date created

Subject

Organisational unit

03663 - Aebersold, Rudolf (emeritus) / Aebersold, Rudolf (emeritus) check_circle
03713 - Sauer, Uwe / Sauer, Uwe check_circle

Notes

Funding

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