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April 24, 2025Materials Today BioOpen Access

Novel high throughput 3D ECM remodeling assay identifies MEK as key driver of fibrotic fibroblast activity

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Why the study?

Models generating quantitative data on 3D fibroblast-mediated ECM remodeling with the reproducibility and throughput needed for drug testing were lacking.

Does inhibition of specific signaling pathways (e.g., MEK, ROCK, LOX) reduce TGFβ-induced 3D ECM remodeling in primary human fibroblasts?

Population

TGFβ-activated primary human skin or lung fibroblasts

Design

Preclinical in vitro compound screening assay development study

Key result

Non-canonical activation of MEK-ERK signaling drives fibrotic ECM remodeling, and high concentrations of TGFβ receptor inhibitors paradoxically stimulate this MEK-mediated profibrotic activity.

Authors

CLChen‐Yi LiaoJHJasmijn H.M. HundscheidJCJustin Crawford

Discussion

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Member takes

Overview

High-dose TGFβ inhibitors may paradoxically promote fibrosis; leaves open MEK-ERK targeting in cardiac fibrotic remodeling.

Structured PICO

Does inhibition of specific signaling pathways (e.g., MEK, ROCK, LOX) reduce TGFβ-induced 3D ECM remodeling in primary human fibroblasts?

P
Population
Primary human dermal and lung fibroblasts (normal and TGFβ-activated) embedded in 3D collagen matrix.
I
Intervention
Anti-fibrotic compounds (including ROCK inhibitors, LIMK inhibitors, LOX inhibitors, TGFβ receptor inhibitors, and MEK inhibitors) and profibrotic stimuli (TGFβ, S1P).
C
Comparator
Control medium or untreated normal fibroblasts.
O
Outcome
3D fibroblast-mediated ECM remodeling (quantified by reflection microscopy) and cell viability (cytotoxicity).surrogate

A novel 3D high-throughput assay reveals that non-canonical MEK-ERK signaling drives fibrotic ECM remodeling and that high doses of TGFβ receptor inhibitors paradoxically stimulate this profibrotic activity.

Limitations

  • The model does not recapitulate the complex interplay between immune cells and fibroblasts that drives in vivo fibrosis.

Cite This Study

Liao et al. (2025) studied Fibrosis. MEK inhibitors and TGFβ receptor inhibitors vs. Control medium was evaluated on ECM remodeling between fibroblast clusters. Non-canonical activation of MEK-ERK signaling drives fibrotic ECM remodeling, and high concentrations of TGFβ receptor inhibitors paradoxically stimulate this MEK-mediated profibrotic activity.

synapsesocial.com/papers/6a1ea98d6540130b7faf274bhttps://doi.org/10.1016/j.mtbio.2025.101800
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Novel high throughput 3D ECM remodeling assay identifies MEK as key driver of fibrotic fibroblast activity2024
  2. 2Abstract 737: Arrays of 3D ECM-embedded fibroblast clusters for characterization of ECM remodeling by primary cancer associated fibroblasts and for evaluation of drugs attenuating fibrotic ECM remodeling2024
  3. 3O146: Investigating the cell-matrix interplay in fibrotic remodelling using renal 3D <i>in vitro</i> models2024
  4. 4Fibrotic Extracellular Matrix Preferentially Induces a Partial Epithelial-Mesenchymal Transition Phenotype in a 3-D Agent Based Model of Fibrosis2024
  5. 5BPS2026 – Scaffold-dependent matrix remodeling function of dermal fibroblasts2026