Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Synthesis, X-ray diffraction analysis, quantum chemical studies and α -amylase inhibition of probenecid derived S -alkylphthalimide-oxadiazole-benzenesulfonamide hybrids

doi: 10.1080/14756366.2022.2078969

Figure Lengend Snippet: X-ray Parameters of both hybrids 1 and 2 .

Article Snippet: Multi-scan CrysAlis PRO 1.171.38.46 (Rigaku Oxford Diffraction, 2015) is used for empirical absorption correction spherical harmonics, implemented in SCALE3 ABSPACK.

Techniques:

Journal: Scientific Reports

Article Title: The anti-tumoral potential of the saporin-based uPAR-targeting chimera ATF-SAP

doi: 10.1038/s41598-020-59313-8

Figure Lengend Snippet: UPAR expression in bladder and breast cancer cell lines. Bladder and breast cancer cell lines resembling respectively different grades (RT4 -grade 1-, RT112 and 5637- grade 2-, HT1376 and ECV304 -grade 3-) and subtypes (MDA-MB-468, BT549, SUM149, SUM159 -TNBC-, SKBR3 -HER2 + -) were analyzed by quantitative PCR (see “Materials and Methods”) for UPAR gene expression ( A ) and by flow cytometry for uPAR protein expression (b and c). UPAR protein expression is shown as histogram plots ( B ) and Relative Fluorescence Intensity (RFI) (see “Materials and Methods”) ( C ). SKBR3 HER2 + breast cancer cell line was used as subtype control. The dashed line represents the threshold arbitrarily defining positive expression (RFI = 2).

Article Snippet: Human bladder RT4, RT112, 5637 (purchased in 2015 from Cell Lines Service), HT1376 (2015, SIGMA) and breast -MDA-MB 231, MDA-MB 468, BT549, SKBR3 (2015, ATCC) cancer cell lines were maintained in RPMI1640 (bladder) or DMEM medium (breast), respectively, supplemented with 10% FCS, 2 mM L-Glutamine and antibiotics (100 U/mL penicillin and 100 μg/mL streptomycine-sulphate).

Techniques: Expressing, Real-time Polymerase Chain Reaction, Gene Expression, Flow Cytometry, Fluorescence, Control

Journal: Scientific Reports

Article Title: The anti-tumoral potential of the saporin-based uPAR-targeting chimera ATF-SAP

doi: 10.1038/s41598-020-59313-8

Figure Lengend Snippet: Cytotoxic activity of ATF-SAP on bladder and breast cancer cells. ATF-SAP activity and target specificity were evaluated on RT4, RT112, 5637, HT1376 and ECV304 bladder cancer cell lines ( A ) and on MDA-MB-468, SUM149, SUM159, BT549 TNBC and HER2 + SKBR3 breast cancer cell lines. ( B ) Cells were incubated for 72 h with scalar logarithmic concentrations of the toxin and cell viability was analyzed by MTT assay. The untargeted seed SAP and the catalytically inactive mutant ATF-SAP KQ were used as controls. The IC50 from three different experiments is reported as mean ± SE.

Article Snippet: Human bladder RT4, RT112, 5637 (purchased in 2015 from Cell Lines Service), HT1376 (2015, SIGMA) and breast -MDA-MB 231, MDA-MB 468, BT549, SKBR3 (2015, ATCC) cancer cell lines were maintained in RPMI1640 (bladder) or DMEM medium (breast), respectively, supplemented with 10% FCS, 2 mM L-Glutamine and antibiotics (100 U/mL penicillin and 100 μg/mL streptomycine-sulphate).

Techniques: Activity Assay, Incubation, MTT Assay, Mutagenesis

Journal: Scientific Reports

Article Title: The anti-tumoral potential of the saporin-based uPAR-targeting chimera ATF-SAP

doi: 10.1038/s41598-020-59313-8

Figure Lengend Snippet: UPA and LRP1 expression in bladder and breast cancer cell lines. ( A ) Skin fibroblasts, bladder and breast cancer cell lines respectively resembling different stages (RT4 -T1 superficial-, RT112 and 5637- T2 muscle invasive-, HT1376 and ECV304 -T3 muscle invasive-) and subtypes (MDA-MB-468, MDA-MB-231, BT549, SUM149, SUM159 -TNBC-, SKBR3 -HER2 + -) were analyzed by qPCR for UPA gene expression (see “Materials and Methods”). ( B ) Competition assay between ATF-SAP and uPAR natural ligands. MDA-MB-468 cells were incubated with ATF-SAP 20 nM in the presence of equal or increasing concentrations of uPA or PAI. The effect on cell viability was evaluated after 72 h by MTT assay. Seed SAP was used as untargeted control. ( C ) Comparison of pro-uPA-SAP and ATF-SAP toxic activity on fibroblasts and MDA-MB-231 cells. Results from one representative experiment are shown as mean ± SD. Three independent experiments were performed for each assay. LRP1 gene ( D ) and protein ( E ) expression on bladder and breast cancer cells. LRP1 protein expression is displayed as histogram plots ( E , left panel) and RFI (see “Materials and Methods”) ( E , right panel). The dashed line represents the threshold arbitrarily defining positive expression (RFI = 2).

Article Snippet: Human bladder RT4, RT112, 5637 (purchased in 2015 from Cell Lines Service), HT1376 (2015, SIGMA) and breast -MDA-MB 231, MDA-MB 468, BT549, SKBR3 (2015, ATCC) cancer cell lines were maintained in RPMI1640 (bladder) or DMEM medium (breast), respectively, supplemented with 10% FCS, 2 mM L-Glutamine and antibiotics (100 U/mL penicillin and 100 μg/mL streptomycine-sulphate).

Techniques: Expressing, Gene Expression, Competitive Binding Assay, Incubation, MTT Assay, Control, Comparison, Activity Assay