- Zanca, Ciro;
- Villa, Genaro R;
- Benitez, Jorge A;
- Thorne, Amy Haseley;
- Koga, Tomoyuki;
- D'Antonio, Matteo;
- Ikegami, Shiro;
- Ma, Jianhui;
- Boyer, Antonia D;
- Banisadr, Afsheen;
- Jameson, Nathan M;
- Parisian, Alison D;
- Eliseeva, Olesja V;
- Barnabe, Gabriela F;
- Liu, Feng;
- Wu, Sihan;
- Yang, Huijun;
- Wykosky, Jill;
- Frazer, Kelly A;
- Verkhusha, Vladislav V;
- Isaguliants, Maria G;
- Weiss, William A;
- Gahman, Timothy C;
- Shiau, Andrew K;
- Chen, Clark C;
- Mischel, Paul S;
- Cavenee, Webster K;
- Furnari, Frank B
In glioblastoma (GBM), heterogeneous expression of amplified and mutated epidermal growth factor receptor (EGFR) presents a substantial challenge for the effective use of EGFR-directed therapeutics. Here we demonstrate that heterogeneous expression of the wild-type receptor and its constitutively active mutant form, EGFRvIII, limits sensitivity to these therapies through an interclonal communication mechanism mediated by interleukin-6 (IL-6) cytokine secreted from EGFRvIII-positive tumor cells. IL-6 activates a NF-κB signaling axis in a paracrine and autocrine manner, leading to bromodomain protein 4 (BRD4)-dependent expression of the prosurvival protein survivin (BIRC5) and attenuation of sensitivity to EGFR tyrosine kinase inhibitors (TKIs). NF-κB and survivin are coordinately up-regulated in GBM patient tumors, and functional inhibition of either protein or BRD4 in in vitro and in vivo models restores sensitivity to EGFR TKIs. These results provide a rationale for improving anti-EGFR therapeutic efficacy through pharmacological uncoupling of a convergence point of NF-κB-mediated survival that is leveraged by an interclonal circuitry mechanism established by intratumoral mutational heterogeneity.