Journal: European journal of medicinal chemistry

Article Title: Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity.

doi: 10.1016/j.ejmech.2024.116202

Figure Lengend Snippet: Fig. 5. Validation of the mechanism of PROTACs 5 and 6. A) Human 293T cells were pre-treated with 15 at 25 μM and then transfected to overexpress SARS- CoV-2 Mpro. Non-trasfected (NT) cells and cells pre-treated with either DMSO or INM were included as controls. B) Human 293T cells were pre-treated with 5 and 6 at 25 μM in the absence or in the presence of 50 μM VHL inhibitor VH298 and then transfected to overexpress SARS-CoV-2 Mpro. NT cells and cells pre- treated with either DMSO were included as controls. In both panels, whole cell lysates obtained from cells collected at 24 h post-transfection were analyzed by Western Blot with an antibody recognizing SARS-CoV-2 Mpro. β-actin was used as a loading control. Molecular masses in kDa are indicated on the left.

Article Snippet: BOC and the VHL inhibitor VH298 were purchased from Selleckchem and Abcam, respectively.

Techniques: Biomarker Discovery, Transfection, Western Blot, Control

Journal: Scientific Reports

Article Title: SOCS domain targets ECM assembly in lung fibroblasts and experimental lung fibrosis

doi: 10.1038/s41598-024-83187-9

Figure Lengend Snippet: VHL protein inhibition does not decrease SMA intensity in myofibroblasts. ( A ) IMR90 lung fibroblasts were untreated or differentiated with 5 ng/mL TGFβ for 48 h. Differentiated myofibroblasts were then treated with 100 µM VH298 for 1 h. Cells were then lysed in SDS buffer and immunoblotted for HIF1-⍺. β-Tubulin was used as the loading control. ( B ) Fibroblasts, myofibroblasts and myofibroblasts treated as in ( A ) were immunostained for FN (red) or SMA (red) and nuclear stain, DAPI (blue). Scale bar = 10 µm.

Article Snippet: VH298 (Axon MedChem, #2810) was used at working concentrations of 100 μM for 1 h in serum media.

Techniques: Inhibition, Control, Staining