Structural basis for asymmetric bis-intercalator targeting of DNA triplex junctions enabling dual inhibition of topoisomerase I and oncogene transcription

Shun-Ching Wang, Chang-Chih Hsieh, Tzu-Chun Yuan, Shan-Meng Lin, Chia-Wei Chen, Chih-Chun Chang, Shih-Chun Huang, En-Chi Wang, Yu-Jhen Huang, Ming-Hsi Chiang, Yih-Chern Horng, Ming-Hon Hou · 2026

Read Structural basis for asymmetric bis-intercalator targeting of DNA triplex junctions enabling dual inhibition of topoisomerase I and oncogene transcription by Shun-Ching Wang, Chang-Chih Hsieh, Tzu-Chun Yuan, Shan-Meng Lin, Chia-Wei Chen, Chih-Chun Chang, Shih-Chun Huang, En-Chi Wang, Yu-Jhen Huang, Ming-Hsi Chiang, Yih-Chern Horng, Ming-Hon Hou (2026) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-13216744.txt.

Description

Wang and colleagues published in twenty twenty-six a structural study of drug-like molecules that wedge into unusual DNA junctions. Most DNA is a double helix, but three-stranded junctions also form. The team studied two compounds that combine a weak and a strong flat ring system. Crystal structures show how they grip a three-stranded junction. The grip distorts the DNA and breaks the junction's integrity in a local way.

One compound, with a four-carbon linker, fit the junction best. Its strong ring mainly blocked an enzyme that cancer cells need. Its weak ring mainly suppressed several cancer-linked genes. In mouse tumors of colon and lung origin, it worked potently with little liver harm. The work marks triplex junctions as real drug targets.

Catalog record

CREATORShun-Ching Wang, Chang-Chih Hsieh, Tzu-Chun Yuan, Shan-Meng Lin, Chia-Wei Chen, Chih-Chun Chang, Shih-Chun Huang, En-Chi Wang, Yu-Jhen Huang, Ming-Hsi Chiang, Yih-Chern Horng, Ming-Hon Hou
YEAR2026
COLLECTIONPAPERS
FORMATTXT
FILE SIZE65 KB
VERSION1.0
LICENSECC BY 4.0
RIGHTSCC BY
SOURCEEurope PMC

Source: https://europepmc.org/articles/PMC13216744

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