Preface (G.B. Jones, M. Palumbo). Introduction to DNA Sequence-specific agents (M. Palumbo). Sequence-specific poisons of type II DNA topoisomerases (G. Capranico et al.). Topoisomerase I-targeting drugs: new developments in cancer pharmacology (B. Gatto, L.F. Liu). DNA sequence recognition altered BIS-benzimidazole minor-groove binders (J.W. Lown). Sequence-specific recognition and modification of double-helical DNA by minor-groove binding conjugates structurally related to netropsin and distamycin (C. Bailly). New developments in the use of nitrogen mustard alkylating agents as anticancer drugs (W.A. Denny). DNA binding of nonclassical platinum antitumor complexes (N. Farrell). Kedarcidin and maduropeptin: two novel antitumor chromoproteins with selective protease activity and DNA cleaving properties (N. Zein, D.R. Schroeder). Antisense- and antigene-based drug design strategies in oncology (K.H. Altmann et al.). Sequence-specific recognition of double-stranded DNA by peptide nucleic acids (P.E. Nielsen).