epigenetic inhibitors  (TargetMol)

Journal: eLife

Article Title: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites

doi: 10.7554/eLife.98221

Figure Lengend Snippet: ( A ) Index chart of an epigenetic inhibitor library screened against P. vivax hypnozoites in a v3 (12-day 1-aminobenzotriazole [1-ABT]) assay. Teal circle: library, black square: DMSO, pink triangle: 200 nM nigericin. (B) Structures of epigenetic inhibitor hits which were confirmed to be active against P. vivax hypnozoites in dose–response assays; blue: histone deacetylase inhibitors.

Article Snippet: The Epigenetic Inhibitor library (Targetmol, cat L1200), containing 773 compounds at 10 mM, was purchased and re-plated in pintool-ready 384-well source plates with 200 μM nigericin and DMSO control wells.

Techniques: Histone Deacetylase Assay

Journal: Scientific Reports

Article Title: EZH2 as a major histone methyltransferase in PDGF-BB-activated orbital fibroblast in the pathogenesis of Graves’ ophthalmopathy

doi: 10.1038/s41598-024-57926-x

Figure Lengend Snippet: EZH2, G9a and DOT1L inhibition reduced PDGF-BB-induced orbital fibroblasts proliferation and hyaluronan production. ( A ) GO orbital fibroblasts (n = 9) were pre-incubated with selective HKMT inhibitors for 24 h and then stimulated with PDGF-BB (50 ng/ml) in the presence or absence of selective HKMT inhibitors. ( B ) GO orbital fibroblasts (n = 9) were stimulated with PDGF-BB (50 ng/ml) and simultaneously treated with selective HKMT inhibitors. After 24 h, proliferation was determined by methylene blue staining. ( C ) GO orbital fibroblasts (n = 6) were pre-incubated with selective HKMT inhibitors for 24 h and then stimulated with PDGF-BB (50 ng/ml) in the presence or absence selective HKMT inhibitors. ( D ) For treatment setting, the orbital fibroblasts (n = 6) were stimulated with PDGF-BB (50 ng/ml) and selective HKMT inhibitors for 24 h. Afterwards, supernatant was collected, and hyaluronan levels were measured by ELISA. Each dot represents the orbital fibroblast strain from one individual and horizontal bars represent the mean values ± standard deviation (SD). Data were analyzed using the paired Student’s t -test. ***, ** and * represent a p -value of < 0.001, < 0.01 and < 0.05, respectively, compared to PDGF-BB stimulation.

Article Snippet: For the screening experiments, orbital fibroblasts were pre-incubated with selective HKMT inhibitors from Epigenetics Compound Library (Catalog No. L1900, Selleck Chemicals, Inc., TX) for 24 h and stimulated with 50 ng/ml of PDGF-BB (Biolegend Inc., USA), either with or without the HKMTs inhibitors for another 24 h. For further experiments on orbital fibroblast activation, only EZH2, G9a and DOT1L inhibitors were used as shown in Supplementary Table .

Techniques: Inhibition, Incubation, Staining, Enzyme-linked Immunosorbent Assay, Standard Deviation