Computer modeling of actinomycin D interactions with double-helical DNA

J Mol Biol. 1986 Oct 5;191(3):495-507. doi: 10.1016/0022-2836(86)90144-0.

Abstract

We have performed molecular mechanical calculations on intercalation complexes of actinomycin D with a series of base-paired hexanucleoside pentaphosphates; d(GCGCGC)2, d(GCCGGC)2, d(GCATGC)2, d(GCTAGC)2 and d(ATGCAT)2. Our results are in good agreement with previous experimental work on sequence selectivity. The results provide a rationalization for the strong preference of actinomycin D to intercalate on the 3' side of guanine residues, consistent with previously proposed models. Finally, the computed structures for d(ATGCAT)2-actinomycin D complexes have been compared with two-dimensional nuclear magnetic resonance nuclear Overhauser effect experimental results. To our knowledge, this is the first extensive comparison of molecular mechanical model structures for a drug-DNA complex with experimental solution phase data. We find generally good agreement between our computational models and the experimental solution phase structures.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Computers*
  • DNA / metabolism*
  • Dactinomycin / metabolism*
  • Hydrogen Bonding
  • Magnetic Resonance Spectroscopy
  • Models, Molecular*
  • Nucleic Acid Conformation
  • Thermodynamics

Substances

  • Dactinomycin
  • DNA