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Asymmetrically-substituted quadruplex-binding napththalene diimides showing potent activity in models for pancreatic cancer

ABSTRACT: Asymmetrically-substituted quadruplex-binding napththalene diimides showing potent activity in models for pancreatic cancer

PROVIDER: PRJNA637074 | ENA |

REPOSITORIES: ENA

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			Action	DRS
	SRR11919229_1.fastq.gz	Fastqsanger.gz
	SRR11919229_2.fastq.gz	Fastqsanger.gz
	SRR11919230_1.fastq.gz	Fastqsanger.gz
	SRR11919230_2.fastq.gz	Fastqsanger.gz
	SRR11919231_1.fastq.gz	Fastqsanger.gz

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Asymmetrically-substituted quadruplex-binding napththalene diimides showing potent activity in models for pancreatic cancer

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G-quadruplex-binding molecule based on napththalene diimides showing potent activity on pancreatic cancer cells

Project description:G-quadruplex-binding molecule based on napththalene diimides showing potent activity on pancreatic cancer cells

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Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models.

Project description:Targeting of genomic quadruplexes is an approach to treating complex human cancers. We describe a series of tetra-substituted naphthalene diimide (ND) derivatives with a phenyl substituent directly attached to the ND core. The lead compound (SOP1812) has 10 times superior cellular and in vivo activity compared with previous ND compounds and nanomolar binding to human quadruplexes. The pharmacological properties of SOP1812 indicate good bioavailability, which is consistent with the in vivo activity in xenograft and genetic models for pancreatic cancer. Transcriptome analysis shows that it down-regulates several cancer gene pathways, including Wnt/β-catenin signaling.

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The Potent G-Quadruplex-Binding Compound QN-302 Downregulates S100P Gene Expression in Cells and in an In Vivo Model of Pancreatic Cancer

Project description:The naphthalene diimide compound QN-302, designed to bind to G-quadruplex DNA sequences within the promoter regions of cancer-related genes, has high anti-proliferative activity in pancreatic cancer cell lines and anti-tumor activity in several experimental models for the disease. We show here that QN-302 also causes down-regulation of the expression of the S100P gene and the S100P protein in cells and in vivo. This protein is well-established as being involved in key proliferation and motility pathways in several human cancers and has been identified as a potential biomarker in pancreatic cancer. The S100P gene contains 60 putative quadruplex-forming sequences, one of which is in the promoter region, 48 nucleotides up-stream from the transcription start site. We report biophysical and molecular modeling studies showing that this sequence forms a highly stable G-quadruplex in vitro, which is further stabilized by QN-302. We also report transcriptome analyses showing that S100P expression is highly upregulated in tissues from human pancreatic cancer tumors, compared to normal pancreas material. The extent of up-regulation is dependent on the degree of differentiation of tumor cells, with the most poorly differentiated, from more advanced disease, having the highest level of S100P expression. The experimental drug QN-302 is currently in pre-IND development (as of Q1 2023) and its ability to down-regulate S100P protein expression supports a role for this protein as a marker of therapeutic response in pancreatic cancer. These results are also consistent with the hypothesis that the S100P promoter G-quadruplex is a potential therapeutic target in pancreatic cancer at the transcriptional level for QN-302.

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G-Quadruplex structures are stable and detectable in human genomic DNA.

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