Sign in
Cancer BiologybioRxiv
Preprint

Inactivation of HIF-P4H-1 Stabilizes IKKα, Modulates Non-Canonical NF-κB Signaling, and Sensitizes Cancer Cells to Cell Death

Karim UllahiD, Mizanur Rahman, Farhan QuadiriD, Valerio IzziiD, Ulrich BergmanniD, Jing ZhangiD, Qing ZhangiD, Rongxue WuiD, Joni M. MäkiiD, Johanna MyllyharjuiD

Abstract

Hypoxia and NF-{kappa}B signaling are well-established drivers of cancer progression and treatment failure, yet the oxygen-dependent regulation of non-canonical NF-{kappa}B signaling remains poorly defined. Here, we identify hypoxia-inducible factor prolyl-4-hydroxylase-1 (HIF-P4H-1/EGLN2) as a key modulator of the non-canonical NF-{kappa}B pathway. Using integrated biochemical, genetic, proteomic, and transcriptomic analyses across human cell lines, mouse models, and clinical tumor samples, we demonstrate that HIF-P4H-1 directly interacts with and hydroxylates IKK at proline 367, thereby promoting its ubiquitination and proteasomal degradation. Loss or inhibition of HIF-P4H-1 results in accumulation of IKK, impaired NF-{kappa}B2/p100 processing to p52, destabilization of NF-{kappa}B-inducing kinase (NIK), and suppression of non-canonical NF-{kappa}B-dependent survival gene expression. Structural modeling and mutagenesis identify proline 367 hydroxylation as a critical determinant of IKK turnover. Analysis of TCGA cohorts reveals an inverse correlation between HIF-P4H-1 and IKK expression, with elevated HIF-P4H-1 associating with advanced tumor stage and reduced overall survival in clear cell renal cell carcinoma. Functionally, targeting HIF-P4H-1 sensitizes cancer cells to cell death and impairs proliferation, clonogenic growth, and migration. Together, our findings define a previously unrecognized oxygen-dependent mechanism regulating non-canonical NF-{kappa}B signaling through direct control of IKK stability and nominate the HIF-P4H-1-IKK axis as a potential therapeutic vulnerability in hypoxia-adapted malignancies.

PDFDOI

02 /Specification & Classification

Click any tag to browse matching papers

Reproducibility ledger

Nobody has reported trying to reproduce this paper yet. Did you replicate an experiment or run the code? Your report saves the next lab a week.

Sign in to file a reproducibility report.

Similarity Map
SelectedSame fieldCross-field
THISZhao '20Schober '20Waele '25Shakir '25Green '25Casillas '21
74% semantic matchCancer Biology
S. Zhao, L. Zhou, D. Dicker+3 more·bioRxiv·Oct 20, 2020