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THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER
THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER
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机译:靶向治疗突变性息肉性息肉样结肠炎(APC)的治疗
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摘要
The present disclosure reports an extensive medicinal chemistry evaluation of a large collection of Truncating APC-Selective Inhibitor (TASIN) compounds. The compounds were evaluated for activity against a series of colon cancer cell lines with and without truncating APC-mutations, as well as in an isogenic cell line pair reporting on the status of APC- dependent selectivity. A number of very potent and selective compounds were identified, including compounds with good metabolic stability and PK properties. The small molecules reported herein thus represent a first-in-class genotype-selective series that specifically target ape mutations present in the vast majority of CRC patients, and therefore serves as a translational platform towards a potential targeted therapy for colon cancer.
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