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Synthesis of N-methyl-N-nitrosourea linked to a methidium chloride analogue and its reactions with /sup 32/P-end-labeled DNA

Journal Article · · Biochemistry; (United States)
OSTI ID:6208654

The synthesis and characterization of an N-methyl-N-nitrosourea (MNU) analogue that is covalently linked to methidium nucleus (9) is described. At 37/degrees/C in pH 8.0 buffer 9 hydrolyzes via pseudo-first-order kinetics, with a calculated t/sub 1/2/ = 77 min. By use of polyacrylamide sequencing gels the formation of piperidine-labile N/sup 7/-methylguanine adducts from the reaction of 9 and MNU with 5'-/sup 32/P-end-labeled DNA restriction fragments is reported. DNA methylation by 9 in 10 mM Tris buffer is enhanced with increasing ionic strength (50-200 mM NaCl), which contrasts to the inhibition of MNU-induced cleavage with increasing salt. In addition, 9 methylates all G sites equally, while MNU shows a clear preference for d(G)/sub n/ (n greater than or equal to 3) runs and an asymmetrical methylation pattern within these G-rich regions. The results are discussed in terms of the delivery of the MNU moiety to the DNA target by a non-sequence-specific intercalation process and the subsequent hydrolytic generation of a nondiffusible alkylating intermediate.

Research Organization:
Univ. of Nebraska Medical Center, Omaha (USA)
OSTI ID:
6208654
Journal Information:
Biochemistry; (United States), Journal Name: Biochemistry; (United States) Vol. 27:23; ISSN BICHA
Country of Publication:
United States
Language:
English