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A potent and selective small-molecule degrader of STAT3 achieves complete tumor regression in vivo

ABSTRACT: A potent and selective small-molecule degrader of STAT3 achieves complete tumor regression in vivo

PROVIDER: PRJNA543332 | ENA |

REPOSITORIES: ENA

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			Action	DRS
	SRR9074380.fastq.gz	Fastqsanger.gz
	SRR9074390.fastq.gz	Fastqsanger.gz
	SRR9074381.fastq.gz	Fastqsanger.gz
	SRR9074391.fastq.gz	Fastqsanger.gz
	SRR9074382.fastq.gz	Fastqsanger.gz

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A potent and selective small-molecule degrader of STAT3 achieves complete tumor regression in vivo

Project description:Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. We report herein the discovery of SD-36, a small-molecule degrader of STAT3. SD-36 potently induces the degradation of STAT3 protein in vitro and in vivo and demonstrates high selectivity over other STAT members. Induced degradation of STAT3 results in a strong suppression of its transcription network in leukemia and lymphoma cells. SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large cell lymphoma cell lines by inducing cell cycle arrest and/or apoptosis. SD-36 achieves complete and long-lasting tumor regression in multiple xenograft mouse models at well tolerated dose schedules. Degradation of STAT3 protein therefore represents a promising cancer therapeutic strategy.

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A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo.

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