DNA binding of a short lexitropsin

N.G. Anthony, K.R. Fox, B.F. Johnston, A.I. Khalaf, S.P. Mackay, I.S. McGroarty, J.A. Parkinson, G.G. Skellern, C.J. Suckling, R.D. Waigh

Research output: Contribution to journalArticle

34 Citations (Scopus)

Abstract

Footprinting, capillary electrophoresis, molecular modelling and NMR studies have been used to examine the binding of a short polyamide to DNA. This molecule, which contains an isopropyl-substituted thiazole in place of one of the N-methylpyrroles, is selective for the sequence 5′-ACTAGT-3′ to which it binds with high affinity. Two molecules bind side-by-side in the minor groove, but their binding is staggered so that the molecule reads six base pairs, unlike the related natural products, which tend to bind to four-base-pair sequences. The result suggests that high affinity and selectivity may be gained without resort to very large molecules, which may be difficult to deliver to the site of action.
Original languageEnglish
Pages (from-to)1353-1356
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number5
DOIs
Publication statusPublished - 8 Mar 2004

Keywords

  • capillary electrophoresis
  • short polyamide to DNA
  • isopropyl-substituted thiazole
  • side-by-side in the minor groove
  • high affinity
  • applied chemistry

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