Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a Representative images of colony formation in multiple human colorectal cancer cell lines HCT15, LST174T, RKO, SW620, NCI-H508, Caco2, and mouse colon cell line CT26 treated with the indicated concentrations of TMPyP4. b The line graph represents the relative colony formation of colorectal cancer cells treated with the indicated concentrations of TMPyP4. c Cell viability of colorectal cancer cells and normal cells was measured with the CCK8 assay. Cells were treated with TMPyP4 for 72 h. d , e Cells were treated with 4 μM or 8 μM TMPyP4 for 48 h. Then, the proportion of apoptotic cells was detected using annexin V-propidium iodide-based flow cytometry. Values are represented as mean ± SD, **** p ≤ 0.0001, by multiple t-tests. f , g Cell cycle analysis of colorectal cancer cells treated with or without TMPyP4 for 24 h. Cellular DNA content was determined by propidium iodide staining and flow cytometry. h, i The tumor size ( h ) and tumor weight ( i ) of nude mice bearing SW620 colorectal tumors treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. Values are represented as mean ± SD, **** p ≤ 0.0001, by unpaired t-test. j , k The tumor size ( j ) and tumor weight ( k ) of nude mice treated with vehicle or 30 mg/kg TMPyP4 in the PDX model. n = 6 mice for both groups. Values are represented as mean ± SD, **** p ≤ 0.0001, by two-way ANOVA ( h , j ) or unpaired t-test ( i , k ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: CCK-8 Assay, Flow Cytometry, Cell Cycle Assay, Staining

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a Experimental treatment strategy for tumor growth inhibition in a syngeneic mouse tumor model. When tumors were palpable, mice were treated with vehicle or 30 mg/kg TMPyP4 three times a week (days 0, 3, 6). b , c The tumor size and tumor weight of BALB/C mice bearing CT26 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. d , e The tumor size and tumor weight of C57BL/6 mice bearing MC38 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. ( f , g ) The tumor size and tumor weight of nude mice bearing MC38 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 6 mice for both groups. h, i Tumor growth inhibition comparison between C57BL/6 and nude mice after TMPyP4 treatment. j – p Graphs show the frequencies of CD45 + cells ( j ), CD3 + T cells ( k ), CD8 + T cells ( l ), DCs ( m ), CD4 + T cells ( n ), NK cells ( o ), and B cells ( p ) in CT26 tumors after TMPyP4 treatment or vehicle control treatment. q – w Graphs show the frequencies of CD45 + cells ( q ), CD3 + T cells ( r ), CD8 + T cells ( s ), DCs ( t ), CD4 + T cells ( u ), NK cells ( v ), and B cells ( w ) in MC38 tumors after TMPyP4 treatment or vehicle control treatment. ns : not significant, * p ≤ 0.05, *** p ≤ 0.001, **** p ≤ 0.0001, by two-way ANOVA ( b , d , f ), or by untailed t-tests ( c , e , g – w ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Inhibition, Comparison, Control

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a – h Representative FACS plots and quantification of IFNγ expression ( a , b ), TNFα expression ( c , d ), perforin expression ( e , f ), and PD-1 expression ( g , h ) among CD8 + T cells in MC38 tumors with TMPyP4 treatment or vehicle control treatment. i – l Surface expression of CD80, CD86, and MHC-I on DCs was determined by FACS. Values are represented as mean ± SD, * p ≤ 0.05, ** p ≤ 0.01, **** p ≤ 0.0001, by untailed t-tests ( b , d , f , h , l ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Expressing, Control

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a , b GSEA of the signaling pathway, including regulation of double-strand break repair and DNA double-strand break response in MC38 tumors with TMPyP4 treatment or vehicle control treatment. c Mean tail moment of the HCT116 and MC38 cells treated with or without TMPyP4 in a comet assay. d Quantification of foci/nucleus of γ-H2AX immunofluorescence staining of HCT116 and MC38 cells treated with or without TMPyP4. e Statistical analysis of γ-H2AX in MC38 tumors with TMPyP4 treatment or vehicle control treatment. f Representative images of G4 and γ-H2AX immunofluorescence staining of HCT116 treated with plasmids pCDNA3.1 or PIF1-pCDNA3.1 in the presence of TMPyP4. g , h Quantification of foci/nucleus of G4 and γ-H2AX in ( f ). i , j Western blots of p-TBK1, TBK1, p-STING, STING, and GAPDH in colorectal cancer cells with the indicated concentrations of TMPyP4. k – m RNA levels of Ccl5, Cxcl10, and Ifn-β were detected in CT26 and MC38 treated with or without TMPyP4 for 48 h. n Representative immunostainings of CD8, CD11c, and P-STING in paraffin sections of MC38 tumors with TMPyP4 treatment or vehicle control treatment (CD8 [green], CD11c [orange], P-STING [red], DAPI [blue]) (magnification ×200). o , p The tumor size and tumor weight of C57BL/6 mice bearing indicated MC38 colon cancer treated with vehicle or 30 mg/kg TMPyP4. n = 5 mice for both groups. Values are represented as mean ± SD, ns : not significant, ** p ≤ 0.01, *** p ≤ 0.001, **** p ≤ 0.0001, by untailed t-tests ( c , d , e , g , h , k , l , m ), or by two-way ANOVA ( g ).

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Control, Single Cell Gel Electrophoresis, Immunofluorescence, Staining, Western Blot

Journal: Cell Death & Disease

Article Title: Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity

doi: 10.1038/s41419-024-07215-2

Figure Lengend Snippet: a – f Tumor growth of vehicle, TMPyP4 alone (30 mg/kg), anti-PD1 alone (200 μg/body), and TMPyP4 plus anti-PD1 groups in BALB/C mice injected with CT26 cells ( a – c ) or C57BL/C mice injected with MC38 cells ( d – f ). n = 4 mice for each group. g , h The frequencies of CD8 + T cells in CT26 ( g ) and MC38 ( h ) tumors after vehicle, TMPyP4 alone (30 mg/kg), anti-PD1 alone (200 μg/body), and TMPyP4 plus anti-PD1 groups treatment. Values are represented as mean ± SD, * p ≤ 0.05, ** p ≤ 0.01, *** p ≤ 0.001, by two-way ANOVA ( b , e ), or by untailed t-tests ( c , f , g , h ). i Relationship between G4 expression and immunotherapy efficacy in colorectal patients. j The overview of the study.

Article Snippet: TMPyP4 was purchased from MCE (HY-108477).

Techniques: Injection, Expressing

Journal: Journal of Biomedical Science

Article Title: Targeting the G-quadruplex as a novel strategy for developing antibiotics against hypervirulent drug-resistant Staphylococcus aureus

doi: 10.1186/s12929-024-01109-3

Figure Lengend Snippet: Confirmation of antibacterial activity. A The antibacterial activities of NMM, TMPyP2, BRACO19, TMPyP4, and Thioflavin T against SAUSA300 were examined by measuring cell growth in terms of OD at 600 nm. B, C SAUSA300 cell growth assessed as CFU/mL ( B ); representative sheep-blood agar plates showing the appearance of colonies during CFU enumeration ( C ). D , E Comparative killing kinetics of vancomycin (Van), Tetracycline (Tet), and NMM against SAUSA300 based on CFU/mL at 1.0 × ( D ); and 10 × ( E ) MIC of Van, Tet, NMM, and 0.05% Triton X-100 at different time points (0 to 12 h). F Comparative live/dead assay of SAUSA300 with 1 × MIC of NMM (5 µM) and Van (0.6 µM) using confocal microscopy, showing the proportion of live/dead SAUSA300 cells. SYTO9 and PI were used to stain the number of total and dead cells as green-fluorescent and red-fluorescent cells, respectively. All experiments were performed in triplicate and the average data was plotted with standard deviation. Significance of the data was analyzed using Student’s t -test. p -values less than 0.05 were considered significant (ns = non-significant p > 0.05, * p < 0.05, ** p < 0.01, *** p < 0.005, and **** p < 0.0001)

Article Snippet: The G4 compounds were procured as BRACO19 trihydrochloride (GC50140, GLPBIO); Quarfloxin or CX-3543 (A12380, AdooQ), TMPyP2 or meso-Tetra (3-pyridyl) porphine (T40846, Frontier Scientific), TMPyP4 tosylate (GC12092, GLPBIO), PDS or Pyridostatin trifluoroacetate salt (18013, Cayman Chemical), PhenDC3 trifluoromethanesulfonate (CS-7711, Chemscene), Thioflavin T (2390-54-7, MedChemExpress), Quinacrine dihydrochloride (69-05-6, MedChemExpress), N-methyl mesoporphyrin IX or NMM (GC44416, GLPBIO), and Quercetin (117-39-5, MedChemExpress) (Fig. S1).

Techniques: Activity Assay, Live Dead Assay, Confocal Microscopy, Staining, Standard Deviation