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Expression data from tumor samples treated with a tankyrase inhibitor in a mouse xenograft model

ABSTRACT: Expression data from tumor samples treated with a tankyrase inhibitor in a mouse xenograft model

PROVIDER: PRJNA454695 | ENA |

REPOSITORIES: ENA

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Expression data from tumor samples treated with a tankyrase inhibitor in a mouse xenograft model

Project description:Tankyrase enhances beta-catenin signaling via PARsylation and subsequent degradation of Axin, a negative regulator of beta-catenin. Tankyrase inhibitors stabilize Axin and suppress beta-catenin signaling. We developed a novel tankyrase inhibitor, RK-287107. We used microarrays to elucidate the gene expression profile of human colorectal cancer cells treated with RK-287107 in a mouse xenograft model.

2018-12-26 | GSE113965 | GEO

Expression data of colon cancer COLO320DM cells and tankyrase inhibitor-resistant variant 320-IWR cells

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Gene expression data of colorectal cancer patient-derived cells treated with tankyrase inhibitors

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Gene expression data of APC-mutated colorectal cancer patient-derived cells treated with tankyrase inhibitors

Project description:Tankyrase, a poly(ADP-ribose) polymerase family member, regulates multiple cellular processes. Tankyrase inhibitors efficiently suppress APC-mutated colorectal cancer (CRC) cell proliferation. To examine the mechanism of anti-proliferative effect of tankyrase inhibitors (G007LK and RK582), we analyzed gene expression profiles of patient-derived APC-mutated CRC cells (JC21 and JC475) left untreated or treated with 0.3 µM G007LK or RK582 for 24 h by cDNA microarray analysis.

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Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines

Project description:Small-molecule tankyrase 1 and tankyrase 2 (TNKS1/2) inhibitors are effective anti-tumor agents in selected tumor cell lines and mouse models. Here, we characterized the response signatures and the in-depth mechanisms for the anti-proliferative effect of tankyrase inhibition (TNKSi). The TNKS1/2-specific inhibitor G007-LK was used to screen 537 human tumor cell lines and a panel of in particular TNKSi-sensitive tumor cell lines was identified. Transcriptome, proteome and bioinformatic analyses revealed the overall TNKSi-induced response signatures in the selected panel. TNKSi-mediated inhibition of WNT/β-catenin, YAP and PI3K/AKT signaling was validated and correlated with lost expression of the key oncogene MYC and impaired cell growth. Moreover, we show that TNKSi induces accumulation of TNKS1/2-containing β-catenin degradasomes functioning as central complexes interacting with YAP and AMOT proteins during attenuation of YAP signaling. These findings provide a contextual and mechanistic framework for using TNKSi in anti-cancer treatment that warrants further comprehensive preclinical and clinical evaluations.

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Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines

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Expression data from 8 xenograft L2987 lung tumor tissue samples

Project description:Transcriptional profiling was conducted on RNA from 8 xenograft L2987lung tumor tissue samples to identify genes affected by treatment with a VEGFR-2 small molecule inhibitor Keywords: Identfication of genes modulated by treatment with a small mollecule VEGFR-2 inhibitor

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Regulation of gene expression in ALK inhibitor CH5424802-treated NCI-H2228 xenograft tumors

Project description:To clarify the downstream signal pathway of EML4-ALK in NSCLC, we performed Affymetrix GeneChip analysis using ALK inhibitor CH5424802-treated NCI-H2228 xenograft tumors, and comprehensively characterized the gene expression regulated by inhibition of activated ALK. Mice bearing NCI-H2228 cells were orally administered at dose of 0 (vehicle), 4 or 20 mg/kg of CH5424802, and the tumors were collected and lysed at 6 hours post-dose. Total RNA were extracted from xenograft tumors.

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