1,734,332 research outputs found

    Design and Synthesis of Potential Inhibitors of Golgi Endo-α-mannosidase:  5-Thio-d-glucopyranosyl-α(1→3)-1-deoxymannojirimycin and Methyl 5-Thio-d-glucopyranosyl-α(1→3)-5-thio-α-d-mannopyranoside

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    Design and Synthesis of Potential Inhibitors of Golgi Endo-α-mannosidase:  5-Thio-d-glucopyranosyl-α(1→3)-1-deoxymannojirimycin and Methyl 5-Thio-d-glucopyranosyl-α(1→3)-5-thio-α-d-mannopyranosid

    Supplementary fig 5 from A Modified Nucleoside 6-Thio-2′-Deoxyguanosine Exhibits Antitumor Activity in Gliomas

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    Supplementary Figure 5. (A-C) The heatmap of proteins changed by THIO in M059K, LN229 and U87MG cells from RPPA data. (D-F) Western blot was performed to confirm the change of these proteins in H4 (more sensitive to THIO) (D), U87MG (less sensitive to THIO) (E), and U251MG (more resistant to THIO) (F) after treatment with THIO at 5 µM. Actin serves as a loading control. (G) Heatmap of pathways regulated by THIO in M059K, LN229 and U87MG cells.</p

    Novel Perfluoroacyl Olefinations of Aldehydes Using β-Thio-Substituted Perfluoroalkyl Enol Ethers

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    α-(Methylthio)- or α-(phenylthio)-substituted perfluoroacylolefinations of nonenolizable aldehydes using the β-lithio-β-thio-perfluoroalkyl enol ethers 1−4 stereoselectively proceeded to give (Z)-α,β-unsaturated perfluoroalkyl ketones 9a−e, 10a−c, 11a−c, and 12a. The α-(thio)-α,β-unsaturated trifluoromethyl ketones were easily converted to 3-(thio)-2-(trifluoromethyl)-1,3-butadienes 21a−c and 22a,b in moderate to high yields (41−85%)

    Supplementary fig 3 from A Modified Nucleoside 6-Thio-2′-Deoxyguanosine Exhibits Antitumor Activity in Gliomas

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    Supplementary Figure 3. (A) Relative initial telomere length of 17 glioma cell lines and NHA. (B) Correlation of IC50s of THIO and initial telomere length in 17 glioma cell lines. (C) Baseline relative expression of hTERT in 17 glioma cell lines and NHA. (D) RNAseq data of hTERT expression in 11 glioma cell lines obtained from CCLE. (E) Correlation of IC50s of THIO and baseline expression of hTERT in 17 glioma cell lines. (F) Correlation of IC50s of THIO and baseline expression of hTERT in 11 glioma cell lines from CCLE. (G) The heatmap of the enrichment scores of 5 telomere/telomerase-related gene signatures for 65 glioma cell lines from CCLE. (H-I) Relative telomere length of M059K and DBTRG-05MG cells following THIO treatment at 2.5 µM for 5 days. (J-K) Telomerase activity of M059K and DBTRG-05MG cells following THIO treatment at 5 µM for 72 hours. (L) Baseline telomerase activity of 10 glioma cell lines, including 5 cell lines that more sensitive to THIO and 5 cell lines that more resistant to THIO. (M) Correlation of baseline telomerase activity and cell viability (%) following THIO treatment. (N) Quantification of western blot of γH2AX expression in 8 glioma cell lines treated with THIO for 72 hours.</p

    Supplementary fig 6 from A Modified Nucleoside 6-Thio-2′-Deoxyguanosine Exhibits Antitumor Activity in Gliomas

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    Supplementary Figure 6. (A) Creation of primary patient-derived glioblastoma organoids. (B) Quantification of tumor weight of U87MG xenograft model. (C) The curve of body weight of mice of U87MG xenograft model during THIO treatment. (D) Quantification of tumor weight of GBM PDX model. (E) The curve of body weight of mice of GBM PDX model during THIO treatment. (F) The curve of body weight of mice of U251MG xenograft model during THIO treatment.</p

    MOESM1 of 2-thio-6-azauridine inhibits Vpu mediated BST-2 degradation

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    Additional file 1: Figure S1. 2-thio-6-azauridine inhibits Vpu-mediated down-regulation of cell surface BST-2 (FACS). HeLa-Vpu and HeLa cells were treated with increasing concentrations of 2-thio-6-azauridine (0.05 µM、0.5 µM、5 µM) for 24 h. Cell surface BST-2 was measured using flow cytometry

    MOESM3 of 2-thio-6-azauridine inhibits Vpu mediated BST-2 degradation

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    Additional file 3: Figure S3. FACS result of Figure 6. A) 2-thio-6-azauridine dose not affect Vpu induced down-regulation of cell surface CD4. (B) 2-thio-6-azauridine has no inhibitory effect upon K5 induced BST-2 degradation

    Supplementary fig 2 from A Modified Nucleoside 6-Thio-2′-Deoxyguanosine Exhibits Antitumor Activity in Gliomas

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    Supplementary Figure 1. (A-B) Successful labeling of CellTrace Violet for M059K and H4 cells. M059K and H4 cells were labeled with a cell membrane dye CellTrace Violet and verified the success of labeling by FACS. (C-D) Cell viability of M059K and H4 following THIO treatment. M059K and H4 cells were treated with control medium or THIO at 5µM and then determined the cell viability percentage via detecting PSVue643 and PI by FACS. (E-F) Western blot results of time-course and dose-titration experiments in M059K and H4. For the time-course experiment, cells were treated with THIO at 5µM and proteins were tested at 0, 24, 48 and 72 hours. For dose-titration experiments, cells were treated with serious doses of THIO for 72 hours. TMZ functions as control. Actin serves as a loading control. Supplementary Figure 2. (A) Crystal violet staining images for acquired TMZ-resistant (TR) cell lines after treatment. (B) The heatmap of quantification results of the crystal violet images of TR cells. % relative to control. (C) Senescence assay for DBTRG-05MG, M059K and H4 cells following THIO treatment at 1 µM for 7 days, and then fixed and stained using Senescence β-Galactosidase Staining Kit and taken images by microscope. (D-F) Quantification results of senescence assay for DBTRG-05MG, M059K and H4 cells. 7 fields were counted for each group. (G-J) Neurosphere growth curves for T98G, U87MG, 13.0302 and TS-603 treated with or without THIO at 5 µM.</p

    Supplementary fig 1 from A Modified Nucleoside 6-Thio-2′-Deoxyguanosine Exhibits Antitumor Activity in Gliomas

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    Supplementary Figure 1. (A-B) Successful labeling of CellTrace Violet for M059K and H4 cells. M059K and H4 cells were labeled with a cell membrane dye CellTrace Violet and verified the success of labeling by FACS. (C-D) Cell viability of M059K and H4 following THIO treatment. M059K and H4 cells were treated with control medium or THIO at 5µM and then determined the cell viability percentage via detecting PSVue643 and PI by FACS. (E-F) Western blot results of time-course and dose-titration experiments in M059K and H4. For the time-course experiment, cells were treated with THIO at 5µM and proteins were tested at 0, 24, 48 and 72 hours. For dose-titration experiments, cells were treated with serious doses of THIO for 72 hours. TMZ functions as control. Actin serves as a loading control.</p
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