Mechanism-Based Multitarget Modeling for Pathway-Level Prediction of PI3K/Akt Signaling Perturbation Induced by Liquid Crystal Monomers

Liquid crystal monomers (LCMs) are emerging contaminants whose system-level toxicity mechanisms remain poorly understood. Here, we developed a pathway-centric multitarget framework to characterize coordinated toxicological perturbations at the signaling network level. KEGG enrichment identified the PI3K/Akt pathway as a key mechanistic axis, and a minimal set of 19 proteins covering upstream receptors, central kinases, and downstream effectors was constructed. A multitask deep learning model trained on ChEMBL IC 50 data (53 694 molecules; 62 440 data points) achieved strong performance (accuracy >0.85, up to 0.94) and was applied to 1412 LCMs. EGFR/JAK1 showed up to 20.18% predicted active inhibitors, followed by PIK3CA (18.06%), with some LCMs exhibiting docking energies comparable to known inhibitors. Structural analysis identified fluorinated aromatic rings, cyclohexyl and bicyclic aliphatic scaffolds, and oxygen-containing groups as key contributors to pathway perturbation. Integration of pathway-level inhibition profiles with simulated Gene Ontology enrichment linked multinode interference to cell cycle arrest, apoptosis, immunosuppression, and impaired cell migration. Transcriptomic analysis in human lung epithelial (A549) cells further confirmed the predicted disruption of the PI3K/Akt signaling pathway. This study provides a transferable framework for mechanism-informed toxicity assessment and chemical prioritization under limited experimental data.

Authors

Institutions

Publication Details

Journal
Environmental Science & Technology
Published
2026-06-17
DOI
https://doi.org/10.1021/acs.est.6c00371
Primary Topic
Computational Drug Discovery Methods
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Mechanism-Based Multitarget Modeling for Pathway-Level Prediction of PI3K/Akt Signaling Perturbation Induced by Liquid Crystal Monomers

Yunsong Mu, Yawen Yuan, Yuhe He, Xiaoli Zhao et al.
Environmental Science & Technology
Computational Drug Discovery Methods
article

Mechanism-Based Multitarget Modeling for Pathway-Level Prediction of PI3K/Akt Signaling Perturbation Induced by Liquid Crystal Monomers

Yunsong Mu, Yawen Yuan, Yuhe He, Xiaoli Zhao, Christie M. Sayes, J D Giesy, Fengchang Wu, Jiawei Cheng
article en

Abstract

Liquid crystal monomers (LCMs) are emerging contaminants whose system-level toxicity mechanisms remain poorly understood. Here, we developed a pathway-centric multitarget framework to characterize coordinated toxicological perturbations at the signaling network level. KEGG enrichment identified the PI3K/Akt pathway as a key mechanistic axis, and a minimal set of 19 proteins covering upstream receptors, central kinases, and downstream effectors was constructed. A multitask deep learning model trained on ChEMBL IC 50 data (53 694 molecules; 62 440 data points) achieved strong performance (accuracy >0.85, up to 0.94) and was applied to 1412 LCMs. EGFR/JAK1 showed up to 20.18% predicted active inhibitors, followed by PIK3CA (18.06%), with some LCMs exhibiting docking energies comparable to known inhibitors. Structural analysis identified fluorinated aromatic rings, cyclohexyl and bicyclic aliphatic scaffolds, and oxygen-containing groups as key contributors to pathway perturbation. Integration of pathway-level inhibition profiles with simulated Gene Ontology enrichment linked multinode interference to cell cycle arrest, apoptosis, immunosuppression, and impaired cell migration. Transcriptomic analysis in human lung epithelial (A549) cells further confirmed the predicted disruption of the PI3K/Akt signaling pathway. This study provides a transferable framework for mechanism-informed toxicity assessment and chemical prioritization under limited experimental data.

Environmental Science & Technology
Baylor University (US), City University of Hong Kong (HK), University of Saskatchewan (CA), Society of Environmental Toxicology and Chemistry (US), Chinese Research Academy of Environmental Sciences (CN), Renmin University of China (CN), Michigan State University (US)
Openalex Percentile: Top 4%
Computational Drug Discovery Methods
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.