ULK1-driven autophagy modulation alters tumor-promoting pathways in triple-negative breast cancer
Merve Gulsen Bal Albayrak1,2, Sevinc Yanar3, Tuğcan Korak4
1Gastroenterology and Hepatology Institute, Department of Molecular Gastroenterology and Hepatology, Kocaeli University, Kabaoglu District, Baki Komsuoglu Blvd. No:21, Umuttepe, 41001, Kocaeli, Turkey. merve.bal@kocaeli.edu.tr.
Abstract:
Triple-negative breast cancer (TNBC) is an aggressive subtype with limited targeted therapies and poor prognosis. Unc-51-like kinase 1 (ULK1), a central regulator of autophagy, has emerged as a potential therapeutic node in cancer but remains poorly understood in TNBC. Here, we investigated the proteomic consequences of pharmacological ULK1 modulation in MDA-MB-231 TNBC cells. Cells were treated with the ULK1 activator LYN-1604 or inhibitor MRT68921 at EC₅₀ concentrations. Autophagic activity, validated through LC3B immunoblotting and fluorescence microscopy, increased under both treatments. Quantitative label-free LC-MS/MS proteomics prioritized 182 and 196 candidate differentially abundant proteins in response to LYN-1604 and MRT68921, respectively. ULK1 activation primarily altered transcriptional regulation and suppressed translation, whereas inhibition was associated with enrichment of immune-related pathway and vesicle-mediated transport. Five proteins consistently downregulated across both treatments (PSIP1, AGO2, MORF4L1, HNRNPC, and SETD2) were prioritized as candidate hubs based on shared regulation across perturbations and network ranking using CytoHubba/MCC. These candidates mapped to autophagy-associated pathway modules/terms related to MET-FAK signaling, extracellular matrix-related processes, and mitochondrial Ca²⁺ handling/transport. These findings suggest that ULK1 modulation, regardless of direction, associated with proteomic changes in pathways linked to tumor-promoting networks. Our study provides a comprehensive proteomic framework linking ULK1 perturbation to transcriptional, immune, and epigenetic regulation, and highlights downstream effectors as candidate targets for future functional and translational validation in TNBC.
Insights
Modulating autophagy regulator Unc-51-like kinase 1 (ULK1) impacts triple-negative breast cancer (TNBC) cell proteomes. This study identifies key proteins and pathways affected by ULK1 activation or inhibition, offering potential therapeutic targets for TNBC.
Area of Science:
- Oncology
- Molecular Biology
- Cell Biology
Background:
- Triple-negative breast cancer (TNBC) is aggressive with limited treatment options.
- Unc-51-like kinase 1 (ULK1), an autophagy regulator, is a potential therapeutic target but poorly understood in TNBC.
Purpose of the Study:
- To investigate the proteomic effects of pharmacological ULK1 modulation in TNBC cells.
- To identify candidate proteins and pathways regulated by ULK1 in TNBC.
Main Methods:
- MDA-MB-231 TNBC cells were treated with a ULK1 activator (LYN-1604) or inhibitor (MRT68921).
- Autophagic activity was assessed via LC3B immunoblotting and microscopy.
- Quantitative label-free LC-MS/MS proteomics identified differentially abundant proteins.
- Bioinformatic analysis (CytoHubba/MCC) prioritized candidate hub proteins and pathways.
Main Results:
- Both ULK1 activation and inhibition increased autophagic activity.
- Proteomics identified 182 (activator) and 196 (inhibitor) candidate proteins.
- ULK1 activation affected transcriptional regulation and translation; inhibition impacted immune pathways and vesicle transport.
- Five proteins (PSIP1, AGO2, MORF4L1, HNRNPC, SETD2) were consistently downregulated and identified as potential hubs.
- These hubs are linked to MET-FAK signaling, extracellular matrix, and mitochondrial calcium handling.
Conclusions:
- ULK1 modulation, irrespective of direction, induces proteomic changes in pathways associated with tumor promotion.
- This study provides a proteomic framework linking ULK1 to transcriptional, immune, and epigenetic regulation in TNBC.
- Downstream effectors of ULK1 present potential targets for future TNBC therapeutic strategies.
Related Concept Videos
Autophagy
An autophagic pathway consists of a series of signaling events activated in response to diverse stress and physiological conditions such as food deprivation,...
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
The Intrinsic Apoptotic Pathway
Interactions Between Signaling Pathways
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
PI3K/mTOR/AKT Signaling Pathway
mTOR Signaling and Cancer Progression
The mTOR pathway or the...


