Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Selected thiazole/chalcone-based tubulin polymerization inhibitors (I–VII) and combretastatin A-4.

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques:

Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Tubulin polymerization inhibitory activity of compounds 9a–o and the reference inhibitor CA-4, expressed as IC 50 values (µM), as determined from a fluorescence-based polymerization assay monitored kinetically for 60 min at 37 °C. Data are presented as mean ± SEM.

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques: Activity Assay, Fluorescence, Polymerization Assay

Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Superimposition of the co-crystallized (green) and redocked (brown) colchicine poses within the colchicine-binding site of tubulin (PDB ID: 4O2B).

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques: Binding Assay

Journal: RSC Advances

Article Title: Design, synthesis, and mechanistic evaluation of novel pyrazole/thiazole chalcone hybrids as dual tubulin polymerization and COX-2 inhibitors with potent antiproliferative activity

doi: 10.1039/d6ra03557d

Figure Lengend Snippet: Binding interactions of compound 9l within the colchicine-binding site of tubulin (PDB ID: 4O2B): (A) 2D interaction diagram and (B) 3D binding mode.

Article Snippet: The effects of compounds 9a–o on tubulin polymerization were assessed using a fluorescence-based tubulin polymerization assay (Cytoskeleton, Inc., Cat. No. BK011P), with combretastatin A-4 as the reference inhibitor.

Techniques: Binding Assay

Journal: International Journal of Molecular Sciences

Article Title: The Intrabody Against Murine Double Minute 2 via a p53-Dependent Pathway Induces Apoptosis of Cancer Cell

doi: 10.3390/ijms26115286

Figure Lengend Snippet: Single-domain antibodies against RING finger domain of MDM2 induce apoptosis. ( A ) Cell proliferation assays were conducted after the three VH antibodies (VH-HT1–VH-HT3) transfected MCF-7 cells by MTT assays. ( B ) Cell proliferation assays were conducted after the three VH antibodies (VH-HT1–VH-HT3) transfected A549 cells by MTT assays. All experiments were repeated at least three times, and similar results were obtained each time. ( C ) For 72 h, the intrabody VH-HT3 showed increased transition of live cells (AV-PI-) to early apoptotic cells (AV+PI-), late apoptotic cells (AV+PI+), and necrotic cells (AV-PI+) in MCF-7 cells using annexin V/propidium iodide probe analysis. ( D ) For 72 h, the intrabody VH-HT3 showed increased transition of live cells (AV-PI-) to early apoptotic cells (AV+PI-), late apoptotic cells (AV+PI+), and necrotic cells (AV-PI+) in A549 cells using annexin V/propidium iodide probe analysis. (* p < 0.01, ** p < 0.001).

Article Snippet: The apoptosis was analyzed using a Cell Meter TUNEL Apoptosis Assay Kit *Green Fluorescence* (T2130, Solarbio, Beijing, China) according to the manufacturer’s instructions (525 nm) and counterstained with DAPI (460 mm) for nuclei in paraffin sections.

Techniques: Transfection

Journal: International Journal of Molecular Sciences

Article Title: The Intrabody Against Murine Double Minute 2 via a p53-Dependent Pathway Induces Apoptosis of Cancer Cell

doi: 10.3390/ijms26115286

Figure Lengend Snippet: The intrabody VH- HT3 are functional in vivo. ( A ) The tumor volumes over time were calculated by the formula width 2 × length × 0.5. ( B ) The tumors were harvested and photographed on the 30th day (bars, 0.5 cm). ( C ) The final tumor weights were recorded and compared. ( D ) Apoptosis in tumors was analyzed by TUNEL assay (bars, 50 μm) (* p < 0.01, ** p < 0.001).

Article Snippet: The apoptosis was analyzed using a Cell Meter TUNEL Apoptosis Assay Kit *Green Fluorescence* (T2130, Solarbio, Beijing, China) according to the manufacturer’s instructions (525 nm) and counterstained with DAPI (460 mm) for nuclei in paraffin sections.

Techniques: Functional Assay, In Vivo, TUNEL Assay