Nature of activated bleomycin

Authors
Citation
Rm. Burger, Nature of activated bleomycin, STRUCT BOND, 97, 2000, pp. 287-303
Citations number
99
Categorie Soggetti
Current Book Contents
ISSN journal
00815993
Volume
97
Year of publication
2000
Pages
287 - 303
Database
ISI
SICI code
0081-5993(2000)97:<287:NOAB>2.0.ZU;2-5
Abstract
Activated bleomycin is the drug species seen to be kinetically competent to initiate DNA degradation in the reaction of bleomycin, Fe(II), and O-2 It also forms in reactions of bleomycin with Fe(III) and peroxide, or bleomyci n with superoxide and either Fe(III) or Fe(II). Efforts to characterize thi s transient species proceeded by kinetic and spectroscopic strategies. Acti vated bleomycin now appears to be a drug-ferric-peroxide complex, but this may not be the proximate active drug species. Assuming that activated bleom ycin peroxide cleavage yields a reactive product analogous to peroxidase co mpound I explains many characteristics of bleomycin-mediated DNA degradatio n reactions. DNA degradation is responsible for the cytotoxic and antitumor activities of this clinically useful antibiotic.