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Article

A Medicinal Chemistry-Driven Approach Identified the Sterol Isomerase EBP as the Molecular Target of TASIN Colorectal Cancer Toxins.

Journal of the American Chemical Society - 1 Apr 2020

Theodoropoulos Panayotis C, Wang Wentian, Budhipramono Albert, Thompson Bonne M, Madhusudhan Nikhil, Mitsche Matthew A, McDonald Jeffrey G, De Brabander Jef K, Nijhawan Deepak

Abstract excerpt

TASIN (Truncated APC-Selective Inhibitors) compounds are selectively toxic to colorectal cancer cells with APC mutations, although their mechanism of action remains unknown. Here, we found that TASINs inhibit three enzymes in the postsqualene cholesterol biosynthetic pathway including EBP, DHCR7, and DHCR24. Even though all three of these enzymes are required for cholesterol biosynthesis, only inhibition of the...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 32163279
DOI: 10.1021/jacs.9b13407
PMCID: PMC7236545

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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