(A) Volcano plot showing differential metabolites between high grade glioma (grade IV) and low grade (grade II) glioma. Data was derived from (34).
(B) Kaplan-Meier curve showing survival of patients in the TCGA HG-U133A glioblastoma dataset stratified based on signature score from the “GO regulation of lipid metabolic process” signature. Log-rank analysis (p = 0.0034, “Signature low” n=262, “Signature high” n=263).
(C) Schematic showing metabolic pathways involved in ω-3 and ω-6 polyunsaturated fatty acid synthesis and mechanism of SC-26196.
(D) qPCR analysis of mRNA expression of ELOVL2 in 7 matched GSCs and DGCs with four technical replicates. Student t-test with Sidak multiple test correction, **, p < 0.01. ****, p < 0.0001.
(E) Cell viability in the GSC387 and GSC3565 cell model following knockdown with three independent, non-overlapping shRNAs targeting FADS2 (shFADS2.1062, shFADS2.456, shFADS2.699) or a non-targeting shRNA (shCONT). Two-way repeated measures ANOVA was used for statistical analysis with Dunnett’s multiple hypothesis test correction with five technical replicates (****, p < 0.0001).
(F) FADS2 mRNA expression assessed by qPCR and EGFR signaling elements assessed by western blot following knockdown with three independent, non-overlapping shRNAs targeting FADS2 (shFADS2.1062, shFADS2.456, shFADS2.699) or a non-targeting shRNA (shCONT). Tubulin was used as a protein loading control.
(G) Cell viability in three GSCs was assessed following 6 days of treatment with SC-26196 at varying concentrations. Kruskal-Wallis test with Dunn’s multiple comparisons test with four technical replicates and three biological replicates. **, p < 0.01,***, p < 0.001. ****, p < 0.0001.
(H) In vitro synergy diagram of combinatorial lapatinib and SC-26196 treatment following combinatorial treatment with lapatinib (0,1,5,10 μM) and SC-26196 (0,5,10 μM). Cell viability was assessed after 3 days of treatment. ZIP score was used to assess synergy (55).
(I) (Top) Kaplan-Meier curve showing survival of mice following implantation with GSC387 following knockdown with two independent, non-overlapping shRNAs targeting ELOVL2 or a non-targeting shRNA (shCONT). n=5 mice per arm. shCONT vs. shELOVL2.308, p = 0.01. shCONT vs. shELOVL2.843, p = 0.001. (Bottom) Hematoxylin and eosin staining of brains following implantation with GSC387 following shCONT or shELOVL2 treatment.
(J) Kaplan-Meier curve showing survival of mice following implantation with GSC387 following treatment with vehicle control, SC-26196 (10μM), lapatinib (5μM), or a combination (10 μM SC-26196 + 5 μM lapatinib) in vitro. n=5 mice for vehicle, SC26196, and combination arms. n=6 for lapatinib arm. Log-rank, p = 0.0018.
(K) Kaplan-Meier curve showing survival of mice following implantation with GSC387 and treatment with vehicle, 125 mg/kg of SC-26196, 30 mg/kg of lapatinib, or a combination (125 mg/kg of SC-26196 and 30 mg/kg of lapatinib). n=5 mice per arm. Log-rank test was used for statistical analysis. Vehicle vs. SC-26196 (p = 0.009). Vehicle vs. lapatinib (p = 0.025). Vehicle vs. combination (p = 0.009). SC-26196 vs. combination (p = 0.27). Lapatinib vs. combination (p = 0.06).