antagonist cilengitide  (MedChemExpress)

Journal: Science Advances

Article Title: Dynamic adaptive coassembled sericin protein orchestrating stem cell development for nucleus pulposus regeneration

doi: 10.1126/sciadv.adx2768

Figure Lengend Snippet: ( A ) 3D coculture of stem cells with the coassembled BS gel. ( B ) Time-dependent gene expression trend of stem cells regulated by coassembled BS protein gel. ( C ) Up-regulated genes and their associated biological events based on Gene Ontology (GO) analysis comparing BS versus B. ( D ) Flow relationships between activated molecular pathways and up-regulated genes based on Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis comparing BS versus B. JAK-STAT, Janus kinase–signal transducer and activator of transcription; MAPK, mitogen-activated protein kinase. ( E ) Gene interaction network analysis and Gantt chart analysis of temporal gene expression in three gene categories. ( F ) Gene expression heatmap analysis comparing BS versus B, n = 3 independent samples. ( G ) In vitro validation of gene expression by qPCR, n = 3 independent samples. ( H ) Local interaction residues in molecular docking. Color-coded representation shows BPAA-GFF (green), sericin protein (magenta), and the integrin αvβ3 complex (blue and orange). ( I ) Time-course analysis of stem cells cocultured with the hydrogel at 1, 2, and 4 weeks. ( J ) Integrin β3 expression analysis at 1 week, n = 3 independent samples. ( K ) Cytoskeletal staining and cell aspect ratio analysis at 1 week. ( L ) YAP staining and nuclear/cytoplasmic ratio analysis. ( M ) Coassembled BS gel activates integrin-mediated cell-matrix interactions, driving YAP nuclear translocation and downstream mechanotransduction signaling. Statistical analyses were performed with Student’s t tests (unpaired and two-tailed): * P < 0.05, ** P < 0.01, and *** P < 0.001.

Article Snippet: To investigate the role of integrin β3 in mediating stem cell adhesion and cytoskeletal regulation, functional inhibition was performed using the αvβ3 integrin antagonist cilengitide (MedChemExpress, USA).

Techniques: Gene Expression, In Vitro, Biomarker Discovery, Expressing, Staining, Translocation Assay, Two Tailed Test

Journal: Oncoimmunology

Article Title: Loss of the extracellular protease ADAMTS1 reveals an antitumorigenic program involving the action of NIDOGEN-1 on macrophage polarization

doi: 10.1080/2162402X.2025.2508057

Figure Lengend Snippet: In vitro macrophage polarization by control and NID1 overexpressing cells. (a) Relative mRNA Fold change expression of M1 ( Nos2 , Tnf , Il1b , Il6 , Cd86 and H2-Aa ) and M2 ( Mrc1 ) polarization-related genes in BMDMs treated with M0 control media, or CM from B16F1 or B16Nid1 cells ( n = 6 per group). (b-c) Relative mRNA Fold change expression of M1-related genes in RAW 264.7 cells (b) ( n = 3) or THP-1-derived macrophages (c) ( n = 2) treated as in (a). (d-e) FC plots showing NOS2 (d), MHC-II and CD206 (e) expression levels in BMDMs treated with CM from B16F1 and B16Nid1 cells, along with graph representation of their quantification. (f) Relative mRNA Fold change expression of M1-related genes ( Nos2 , Tnf , Il1b , and Il6 ) in BMDMs polarized with B16Nid1 CM, control or pre-treated with 2 μM cilengitide ( n = 6 per group). (g) p-AKT and total AKT western blot (WB) analysis of lysates from BMDMs treated during 15 min with M0 control media, or CM from B16F1 or B16Nid1 cells. When indicated, cells were pre-treated with 2 μM cilengitide. Digits below each lane correspond to the relative intensity of p-AKT/AKT ratio. (h) Graph representing quantification of p-AKT WB levels normalized to total AKT for each condition ( n = 4) (* p < 0.05; ** p < 0.01).

Article Snippet: To investigate its role, BMDMs were pre-treated with the αvβ3 antagonist cilengitide (HY-16141, MedChemExpress) prior to polarization.

Techniques: In Vitro, Control, Expressing, Derivative Assay, Western Blot

Journal: Pancreas

Article Title: The differentiation of pancreatic tumor-initiating cells by vitronectin can be blocked by Cilengitide

doi: 10.1097/MPA.0b013e318279d568

Figure Lengend Snippet: (A) Growth of pancreatospheres in the presence of human serum with the addition of Cilengitide. (B) Log2 values are shown for qRT-PCR performed in triplicate, normalized to 18s rRNA and shown relative to the respective pancreatospheres treated with human serum. Bars in white represent PANC1 cells treated with serum + 2.5 µM Cilengitide and bars in gray represent PANC1 cells treated with serum + 5µM Cilengitide, respectively. qRT-PCR data was analyzed with an unpaired t-test using Holm-Sidak method with the criteria of statistical significance of alpha=5%, significance is indicated by “*”. (C) Oncomine analysis in pancreatic cancer studies comparing the gene expression level of ITGAV in normal versus pancreatic carcinoma and pancreatitis. The expression level of ITGAV (VN receptor) is statistically significant (p-value=5.37E-12). (D) Oncomine analysis in pancreatic studies focusing on pancreatic intraepithelial neoplasia, high PanIN grade and high grade pancreatic ductal adenocarcinoma. The expression level of ITGAV is statistically significant (p-value=0.015). (www.oncomine.org)

Article Snippet: Promoting and blocking differentiation of pancreatospheres with the integrin antagonist Cilengitide As the data demonstrates that the differentiation of pancreatospheres by human serum is mediated by the integrin receptors, αVβ3 and αVβ5, we sought to determine if we could block this process by a compound currently in clinical trial, Cilengitide (EMD 121974, Merck KGaA).

Techniques: Quantitative RT-PCR, Gene Expression, Expressing