TY - JOUR
T1 - FER kinase governs invasive growth of head and neck squamous cell carcinoma through dynamic control of growth factor receptor activity
AU - Haughton, Peter D.
AU - Enserink, Lotte N.F.L.
AU - Tavares, Sandra
AU - Haakma, Wisse
AU - Galustjan, Garik
AU - Koppes, Sjors
AU - Casasanta, Lorenza
AU - Driehuis, Else
AU - Clevers, Hans
AU - Zhang, Yanchun
AU - Fan, Gaofeng
AU - Willems, Stefan
AU - Yang, Xiaobao
AU - Derksen, Patrick W.B.
N1 - Copyright © 2025. Published by Elsevier Inc.
PY - 2025/12
Y1 - 2025/12
N2 - Promiscuous activation of growth factor receptors drives sustained MAP kinase signaling, which reinforces oncogene addiction in HPV-negative head and neck squamous cell carcinoma (HNSCC). This feature promotes invasive growth, complicating surgical resection and contributing to high rates of local relapse and poor patient outcomes. Current treatment strategies for locally advanced or non-resectable tumors targeting single growth factor receptors offer limited therapeutic benefit, underscoring the need for alternative targets. Using patient-derived tumor organoid (PDO) models of invasive HNSCC, we demonstrate that FER, a non-receptor tyrosine kinase that correlates with poor survival in HNSCC patients, is essential for growth factor receptor dependent invasive growth in Collagen-I extracellular matrix (ECM) networks. In this setting, FER promotes phosphorylation of EGFR-Y1068 and MET-Y1234/5. Additionally, FER controls ligand-dependent endocytic transport velocity, demonstrating a multifactorial regulation of proximal GFR activation during HNSCC invasion. Finally, genetic loss of function experiments or a FER-specific PROteolysis-TArgeting Chimera (PROTAC) strategy in PDO-based xenograft mouse models, demonstrate that FER is essential for invasive growth and metastasis of HNSCC. In sum, we propose that FER is an indiscriminate regulator of proximal GFR activation in HNSCC, a mechanism that may foster oncogene addition, thereby leading to invasive growth and metastasis. Based on its oncogenic roles and correlations with poor patient prognosis, we nominate FER as a potential candidate for targeted clinical intervention of HNSCC.
AB - Promiscuous activation of growth factor receptors drives sustained MAP kinase signaling, which reinforces oncogene addiction in HPV-negative head and neck squamous cell carcinoma (HNSCC). This feature promotes invasive growth, complicating surgical resection and contributing to high rates of local relapse and poor patient outcomes. Current treatment strategies for locally advanced or non-resectable tumors targeting single growth factor receptors offer limited therapeutic benefit, underscoring the need for alternative targets. Using patient-derived tumor organoid (PDO) models of invasive HNSCC, we demonstrate that FER, a non-receptor tyrosine kinase that correlates with poor survival in HNSCC patients, is essential for growth factor receptor dependent invasive growth in Collagen-I extracellular matrix (ECM) networks. In this setting, FER promotes phosphorylation of EGFR-Y1068 and MET-Y1234/5. Additionally, FER controls ligand-dependent endocytic transport velocity, demonstrating a multifactorial regulation of proximal GFR activation during HNSCC invasion. Finally, genetic loss of function experiments or a FER-specific PROteolysis-TArgeting Chimera (PROTAC) strategy in PDO-based xenograft mouse models, demonstrate that FER is essential for invasive growth and metastasis of HNSCC. In sum, we propose that FER is an indiscriminate regulator of proximal GFR activation in HNSCC, a mechanism that may foster oncogene addition, thereby leading to invasive growth and metastasis. Based on its oncogenic roles and correlations with poor patient prognosis, we nominate FER as a potential candidate for targeted clinical intervention of HNSCC.
KW - EFGR
KW - FER PROTAC
KW - FER kinase
KW - Growth factor receptors
KW - Head and neck cancer
KW - Inhibition
KW - Invasion
KW - MET
KW - Patient-derived organoids
KW - Phosphorylation
KW - Cell Proliferation
KW - Signal Transduction
KW - Neoplasm Invasiveness
KW - Humans
KW - Squamous Cell Carcinoma of Head and Neck/pathology
KW - Xenograft Model Antitumor Assays
KW - Animals
KW - Cell Line, Tumor
KW - Mice
KW - ErbB Receptors/metabolism
KW - Head and Neck Neoplasms/pathology
KW - Protein-Tyrosine Kinases/metabolism
UR - https://www.scopus.com/pages/publications/105018876602
UR - https://www.mendeley.com/catalogue/34fbb641-e5c5-3c93-bb09-f5008803a1ad/
U2 - 10.1016/j.neo.2025.101241
DO - 10.1016/j.neo.2025.101241
M3 - Article
C2 - 41115375
AN - SCOPUS:105018876602
SN - 1522-8002
VL - 70
JO - Neoplasia (United States)
JF - Neoplasia (United States)
M1 - 101241
ER -