Fig. 2: PCLX-001 selectively inhibits myristoylation in vitro and induces apoptosis in lymphoma cell lines.
From: Targeting N-myristoylation for therapy of B-cell lymphomas
Click chemistry was used on alkyne-myristate labeled cell lysates to determine overall protein myristoylation levels in: BL2 cells (a) and IM9 cells (b) treated for 1 h with 0.01–1.0 µM PCLX-001, myristoylation levels of a WT-Src-EGFP construct expressed in COS-7 cells (c) and, myristoylation of immunoprecipitated endogenous pp60-Src in IM9 cells following 1 h treatment with 1.0–10 µM of PCLX-001 (d). Fluorescence micrographs of COS-7 cells transfected with a WT-Src-EGFP (left), non-myristoylatable G2A-Src-EGFP mutant (center), and a WT-Src-EGFP construct treated with 10 μM PCLX-001 for 24 h (right) (e). Scale bars are equal to 10 μm. Endogenous Src protein levels in IM9 and BL2 cells treated with 1 μM PCLX-001 for 0–5 days measured by Western blotting (f). Western blotting of cleaved PARP-1 and cleaved caspase-3 in IM9, BL2, and Ramos cell lysates following 72 h incubation with 0–1.0 µM PCLX-001 (composite gels) (g). All data shown are representative of at least three independent experiments. GAPDH serves as loading control. Source data are provided as a Source Data file.
