Figure 4
From: Anti-Tumor Activity and Immunotherapeutic Potential of a Bisphosphonate Prodrug
Inhibition of geranylgeranylation of RAP1A in tumor cells by compound 7. Tumor cells were cultured with 7 for 16 h, lysed, and the prenylation of RAP1A assessed after protein separation by SDS-PAGE, transfer to PVDF membranes, and probing with anti-unprenylated RAP-1A antibodies. (A–F) Compound 7 inhibition of geranylgeranylation of RAP1A for various types of tumor cell lines: (A) lymphomas, ▫ MOLT-3, ∆ PEER, ⚪ C1R, ⬧ J.RT3-T3.5, ▪ Raji, ▴ RAMOS-RA1, ⚫ MOLT-4; (B) myeloid leukemias, ▫ HL60, ∆ U937, ⚪ THP-1, ⬧ SCC-3, ▪ P31/FUJ, ▴ K562, ⚫ NOMO-1; (C) mammary carcinomas, ▫ YMB-1-E, ∆ MRK-nu-1, ⚪ HMC-1-8, ⬧ MCF-7, ▪ MDA-MB-231, ▴ T-47D, ⚫ SK-BR-3; (D) renal cell carcinomas, ▴ 786-0, ∆ VMRC-RCZ, ⚫ UOK121, ⚪ Caki-1, ▪ A-704; (E) pancreatic carcinomas, ⚫ BXPC-3, ▴ KP4-1, ⚪ KP4-2, ▫ KP4-3, ∆ MiaPaCa2; (F) other tumor cells, ⚫ TGB24TKB cholangiocell carcinoma, ▴ ACS gastric carcinoma, ⚪ MG63 osteocarcoma, ▫ LK-2 lung carcinoma, ∆ EJ-1 bladder carcinoma. (G) Comparison of compound 7 (left panel) with zoledronic acid (right panel) concentrations required for half-maximal inhibition of prenylation of RAP1A in tumor cells. Ly = lymphomas, My = myeloid leukemia, Ma = mammary carcinomas, and Others = other tumor cell lines. Data for zoledronic acid effects are from Idrees et al.46 and are included for comparison.
