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. Author manuscript; available in PMC: 2026 Sep 13.
Published in final edited form as: Eur J Med Chem. 2025 Oct 4;301:118228. doi: 10.1016/j.ejmech.2025.118228

Figure 6: New compounds targeting TG2 reduce tumor colonization and progression in mouse models.

Figure 6:

(A) Plasma PK of P374 and P404. Compounds were dosed in cassette format by intraperitoneal (IP) administration to female C57BL/6 mice at doses of 2 mg/kg each and plasma concentrations were measured at the indicated time points. (B, C) Omental colonization assay using luciferase-expressing OVCAR5 cells injected IP into nude mice and co-administered with either diluent vs. compound P374 (B) or P405 (C). Tumor colonization was assessed as luciferase signal intensity. Quantification of total tumor weights (D), tumor volumes (E), and tumor numbers (F) in IP OVCAR5 xenografts treated with diluent or P374 for 4 weeks. P374 or vehicle (control) were administered IP 55μg/Kg three times per week (n=5 mice per group). (G) TG2 expression assessed via IHC in xenografts from experiment in C-E (n= 5 tumors per group). Quantification of TG2 staining was performed using FIJI color deconvolution. (H) TG2 enzymatic activity was assessed in ascites fluid collected from the experiment in C-E (control n = 5; P374-treated n = 3). (I) TG2 enzymatic activity was assessed in malignant OC-associated ascites (n=5 specimens). All values represent means ± SD. *p < 0.05; ** < 0.01 by 2-tailed Student’s t-test.