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Targeting an IKBKE cytokine network impairs triple-negative breast cancer growth
Thanh U. Barbie, Gabriela Alexe, Amir R. Aref, Shunqiang Li, Zehua Zhu, Xiuli Zhang, Yu Imamura, Tran C. Thai, Ying Huang, Michaela Bowden, John Herndon, Travis J. Cohoon, Timothy Fleming, Pablo Tamayo, Jill P. Mesirov, Shuji Ogino, Kwok-Kin Wong, Matthew J. Ellis, William C. Hahn, David A. Barbie, William E. Gillanders
Thanh U. Barbie, Gabriela Alexe, Amir R. Aref, Shunqiang Li, Zehua Zhu, Xiuli Zhang, Yu Imamura, Tran C. Thai, Ying Huang, Michaela Bowden, John Herndon, Travis J. Cohoon, Timothy Fleming, Pablo Tamayo, Jill P. Mesirov, Shuji Ogino, Kwok-Kin Wong, Matthew J. Ellis, William C. Hahn, David A. Barbie, William E. Gillanders
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Research Article Oncology

Targeting an IKBKE cytokine network impairs triple-negative breast cancer growth

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Abstract

Triple-negative breast cancers (TNBCs) are a heterogeneous set of cancers that are defined by the absence of hormone receptor expression and HER2 amplification. Here, we found that inducible IκB kinase–related (IKK-related) kinase IKBKE expression and JAK/STAT pathway activation compose a cytokine signaling network in the immune-activated subset of TNBC. We found that treatment of cultured IKBKE-driven breast cancer cells with CYT387, a potent inhibitor of TBK1/IKBKE and JAK signaling, impairs proliferation, while inhibition of JAK alone does not. CYT387 treatment inhibited activation of both NF-κB and STAT and disrupted expression of the protumorigenic cytokines CCL5 and IL-6 in these IKBKE-driven breast cancer cells. Moreover, in 3D culture models, the addition of CCL5 and IL-6 to the media not only promoted tumor spheroid dispersal but also stimulated proliferation and migration of endothelial cells. Interruption of cytokine signaling by CYT387 in vivo impaired the growth of an IKBKE-driven TNBC cell line and patient-derived xenografts (PDXs). A combination of CYT387 therapy with a MEK inhibitor was particularly effective, abrogating tumor growth and angiogenesis in an aggressive PDX model of TNBC. Together, these findings reveal that IKBKE-associated cytokine signaling promotes tumorigenicity of immune-driven TNBC and identify a potential therapeutic strategy using clinically available compounds.

Authors

Thanh U. Barbie, Gabriela Alexe, Amir R. Aref, Shunqiang Li, Zehua Zhu, Xiuli Zhang, Yu Imamura, Tran C. Thai, Ying Huang, Michaela Bowden, John Herndon, Travis J. Cohoon, Timothy Fleming, Pablo Tamayo, Jill P. Mesirov, Shuji Ogino, Kwok-Kin Wong, Matthew J. Ellis, William C. Hahn, David A. Barbie, William E. Gillanders

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Figure 5

Inhibition of this network by CYT387 suppresses protumorigenic cytokines.

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Inhibition of this network by CYT387 suppresses protumorigenic cytokines...
(A) Cytokine antibody array incubated with media from 293T cells transfected with EGFP or IKBKE for 24 hours and pretreated with DMSO, 5 μM CYT387, or 5 μM ruxolitinib for 12 hours. Circles represent the location of CCL5, the predominant cytokine induced by IKBKE and inhibited by CYT387, compared with ruxolitinib. (B) ELISA measurement of CCL5 or IL-6 levels in 293T cells expressing IKBKE and treated with DMSO, 5 μM ruxolitinib, or 5 μM CYT387. Mean and SD of duplicate samples shown. (C) ELISA measuring CCL5 or IL-6 levels in MDA-MB-468 cells or MDA-MB-231 cells stimulated with IL-1β for 24 hours following pretreatment with DMSO or 5 μM CYT387 for 1 hour. Mean and SD of duplicate samples shown. (D) Phase-contrast images (original magnification, ×20) of MDA-MB-468 spheroids in microfluidic 3D culture at baseline and 24 and 48 hours following addition of CCL5/IL-6, EGF, or the combination of both, together with DMSO as a control (left). Treatment with 1 μM CYT387 inhibited EGF-induced MDA-MB-468 spheroid dispersal, but this was rescued by the addition of CCL5 and IL-6 (right). (E) Schematic of angiogenesis microfluidic device. HUVECs were seeded in central channel and subjected to cytokine/chemokine diffusion as indicated. (F) Compared with control media, diffusion of CCL5/IL-6–attracted HUVECs into collagen (original magnification, ×20) over the course of 24 hours. Cotreatment with the MEK inhibitor (MEKi), GSK1120212, at 10 nM strongly inhibited this effect. Mean and SD of cell migration per number from 3 independent devices shown.

Copyright © 2026 American Society for Clinical Investigation
ISSN: 0021-9738 (print), 1558-8238 (online)

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