Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway

doi: 10.1080/14756366.2023.2230388

Figure Lengend Snippet: Viability of MDA-MB-231 cells treated with 4 μM of compounds (A) 13h-1–3 , 13b-4–6 , 7b-2 , 7b-4 , and 12j-3–4 , and (B) MDA-MB-231, (C) A549, (D) HCC-827, (E) MCF-7, and (F) MRC-5 treated with compounds 12j-4 , 13h-1 , and 13h-3 with 0, 1, 2, 4, 8, 16, and 32 μM for 60 h, respectively. Cell viability was determined using the Cell Counting Kit-8 assay. Positive control: paclitaxel and BMS202. Negative control: 1% DMSO. Data are expressed as mean ± SEM ( n = 3). * p < 0.05, ** p < 0.01, *** p < 0.001.

Article Snippet: BMS202 (CAS: 1675203–84-5) was purchased from TOPSCIENCE (Singapore).

Techniques: Cell Counting, Positive Control, Negative Control

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway

doi: 10.1080/14756366.2023.2230388

Figure Lengend Snippet: Inhibition of the proliferation and migration of MDA-MB-231 cells with compound 12j-4. ( A ) The clone formation rates of MDA-MB-231 cells were treated with 12j-4 for 24 h at a concentration of 1 μM. ( B ) Migration ability of MDA-MB-231 cells treated with 12j-4 (1 μM) for 24 h and 48 h. Positive control: paclitaxel and BMS202. Negative control: 1% DMSO. Data are expressed as mean ± SEM ( n = 3). * p < 0.05, ** p < 0.01, *** p < 0.001.

Article Snippet: BMS202 (CAS: 1675203–84-5) was purchased from TOPSCIENCE (Singapore).

Techniques: Inhibition, Migration, Concentration Assay, Positive Control, Negative Control

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway

doi: 10.1080/14756366.2023.2230388

Figure Lengend Snippet: The expression level of PD-L1 is regulated by compound 12j-4. MDA-MB-231 cells were treated with 12j-4 for 48 h at a concentration of 1, 2, and 4 μM, respectively. BMS202 was used as a positive drug. ( A ) The expression of the PD-L1 protein and ( B ) PD-L1 mRNA was detected by Western blot and qPCR, respectively. The expression of PD-L1 protein was detected by ( C ) Western blot after MDA-MB-231 cells were treated with or without 12j-4 (4 μM) combined with GSK-3β inhibitor (40 nM) for 48 h. Data are expressed as mean ± SEM ( n = 3). * p < 0.05, ** p < 0.01, *** p < 0.001.

Article Snippet: BMS202 (CAS: 1675203–84-5) was purchased from TOPSCIENCE (Singapore).

Techniques: Expressing, Concentration Assay, Western Blot

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Schematic diagram illustrating the enhancement of immune cells infiltration and their anticancer activities. ( a ) Exposure to BMS202-conjugated NDs for 6 h. ( b and d ) Melanoma cells co-cultured with hPBMCs for an additional 24 h. ( c ) Immune cells/cancer cells interaction. ( e ) Induction of cytotoxicity by Immune cells.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques: Cell Culture

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Physical–chemical characterization and hydrodynamic size distribution of bare NDs and BMS 202-loaded NDs.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques:

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Representative images of hPBMCs/CD+ T cells and Melanoma cells interactions. WM793P1 Melanoma cells were exposed to BMS202-NDs for 6 h and then incubated with hPBMCs for an additional 24 h. ( A ) Non-ND treated cells, ( B ) ND-treated and hPBMCs co-cultured cells were stained with anti-CD8 antibodies (red). Cells then were labelled with cell tracker (green, CMFDA Dye, ThermoFisher Scientific, Dublin, Ireland) and counterstained with Hoechst 33,342, (blue) for visualization of cell nuclei, and indicating interaction of Immune cells with cancer cells. Imaging was performed using an inverted microscope (10X), and scale bar represents 400 µm.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques: Incubation, Cell Culture, Staining, Imaging, Inverted Microscopy

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Cell viability inhibition post-exposure to and interaction with hPBMCs. Melanoma cell lines were either left untreated (NT) or treated with either nanodiamonds (NDs) alone; BMS202 alone (10 µM), or ND-BMS202 (2.5 µM, 5 µM, 10 µM) for 6 h, then subsequently co-cultured with hPBMCs for an additional 24 h. Cells were stained with Hoechst 33,342 and scanned and analyzed using the Cytell™ imaging system. Viable cells were automatically counted, and data were presented as mean ± SEM (n = 3). ( a – c ) Overall effects on overall cell viability for all treatments. ( d – f ) comparison of nanocomplexes compared to ND/PBMCs exposure and continue to show significantly enhanced effects on cell viability. All data were analyzed using one‐way ANOVA with Tukey’s post-hoc test, “**” for p < 0.01.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques: Inhibition, Cell Culture, Staining, Imaging, Comparison

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Cell Membrane Permeability (CMP) Damage and Lysosomal mass/pH changes. Melanoma cell lines were either not treated (NT) or treated with 2.5 µM, 5 µM, 10 µM of BMS202-NDs or to 10 µM of BMS202 alone for 6 h, then cells were co-cultured with hPBMCs for an additional 24 h. Cells were probed with CMP dye (green), Lysosomal mass/pH (red), and counterstained with Hoechst 33,342 ( a – f ). Cells were then scanned and analyzed using the Cytell™ imaging system and BioApp software. Changes in CMP (green) ( g – i ) and induction of lysosomal mass/pH changes (red) cells ( k – l ) were automatically counted, and data were presented as mean ± SEM (n = 3) and were analyzed using one‐way ANOVA coupled with a non-parametric Kruskal-Willis test, “*” for p < 0.05; “**” for p < 0.01; and “***” for p < 0.001.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques: Membrane, Permeability, Cell Culture, Imaging, Software

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Upregulation of γ‑H2AX expression post exposure to ND/BMS202/PBMCs. Melanoma cell lines were either not treated (NT) or treated with 2.5 µM, 5 µM, 10 µM of BMS202-NDs or/to 10 µM of BMS202 alone for 6 h, then cells were co-cultured with hPBMCs for an additional 24 h. Cell lysates were harvested and then (40 μg) were resolved by SDS-PAGE and probed with anti- γ‑H2AX. Relative densitometric analysis of the individual bands was performed. The top band represents γH2aX and the bottom band represents GAPDH. Data were presented as mean ± SEM (n = 3) and were analyzed using one‐way ANOVA coupled with a non-parametric Kruskal–Wallis test carried out on the experimental data, with respect to the corresponding untreated controls (NT), “*” for p < 0.05, and “**” for p < 0.01.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques: Expressing, Cell Culture, SDS Page

Journal: Scientific Reports

Article Title: Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

doi: 10.1038/s41598-023-34638-2

Figure Lengend Snippet: Cleaved caspase 3 expression. Melanoma cell lines were either not treated (NT) or treated with 2.5 µM, 5 µM, 10 µM of BMS202-NDs or/to 10 µM of BMS202 alone for 6 h, then cells were co-cultured with hPBMCs for an additional 24 h. Cell lysates were harvested and then (40 μg) were resolved by SDS-PAGE and probed with anti-cleaved caspase 3. Relative densitometric analysis of the individual bands was performed. The top row represents cleaved caspase 3 and the bottom row represents GAPDH. Data were presented as mean ± SEM (n = 3) and were analyzed using one‐way ANOVA coupled with a non-parametric Kruskal–Wallis test carried out on the experimental data, with respect to the corresponding untreated controls (NT), “*” for p < 0.05, and “**” for p < 0.01.

Article Snippet: BMS202 (Cat. No. S7912-SEL—10 mM in 1 ml of DMSO) was purchased from Stratech (Stratech, Ely, United Kingdom).

Techniques: Expressing, Cell Culture, SDS Page