DNA recognition by a novel Bis-Intercalator, potent anticancer drug XR5944

Clement Lin, Danzhou Yang

Research output: Contribution to journalArticlepeer-review

4 Scopus citations


XR5944 is a potent anticancer drug with a novel DNA binding mode: DNA bisintercalationg with major groove binding. XR5944 can bind the estrogen response element (ERE) sequence to block ER-ERE binding and inhibit ERα activities, which may be useful for overcoming drug resistance to currently available antiestrogen treatments. This review discusses the progress relating to the structure and function studies of specific DNA recognition of XR5944. The sites of intercalation within a native promoter sequence appear to be different from the ideal binding site and are context- and sequence- dependent. The structural information may provide insights for rational design of improved EREspecific XR5944 derivatives, as well as of DNA bis-intercalators in general.

Original languageEnglish (US)
Pages (from-to)1385-1397
Number of pages13
JournalCurrent topics in medicinal chemistry
Issue number12
StatePublished - Mar 1 2015


  • Anticancer drug
  • DNA bis-intercalation
  • DNA bis-intercalation with major groove binding
  • NMR solution structure
  • XR5944 or MLN944

ASJC Scopus subject areas

  • Drug Discovery


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