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PMID: 4530265 Published · ppublish English Journal Article

Metallointercalation reagents. 2-hydroxyethanethiolato(2,2',2'-terpyridine)-platinum(II) monocation binds strongly to DNA by intercalation.

Jennette KW, Lippard SJ, Vassiliades GA, Bauer WR

Abstract

The red, cationic complex 2-hydroxy-ethanethiolato(2,2',2''-terpyridine)platinum(II), [(terpy)-Pt(SCH(2)CH(2)OH)](+), binds strongly to DNA by a mechanism involving intercalation. By means of fluorescence spectroscopy, the platinum complex was shown to inhibit competitively the binding of the intercalating dye ethidium bromide to calf thymus DNA. This platinum complex increases the viscosity of calf thymus DNA, raises the melting temperature by up to 5 degrees , and exhibits induced circular dichroism when bound to the DNA. The closed circular viral DNA from bacteriophage PM2 is unwound by the complex in a manner that is similar to that of ethidium bromide and with an unwinding angle that appears to be slightly less than that of ethidium. Studies of the related complex [(terpy)PtCl](+), which has a substitutionally more labile chloride ligand, suggest that it also intercalates, especially at [DNA-P]:[Pt] ratios greater than 2. The potential utility of these new metallointercalation reagents as heavy atom probes in fiber diffraction or electron microscopic studies of the interaction process is discussed.

MeSH Terms
Animals Binding Sites Binding, Competitive Cattle Chemical Phenomena Chemistry Cisplatin Coliphages DNA DNA, Circular DNA, Viral Ethidium Hot Temperature Mercaptoethanol/analogs & derivatives Molecular Conformation Nucleic Acid Conformation Nucleic Acid Denaturation Organometallic Compounds Platinum Pyridines Spectrometry, Fluorescence Spectrophotometry Thymus Gland Ultracentrifugation Viscosity
Chemicals
DNA, Circular DNA, Viral Organometallic Compounds Pyridines Platinum Mercaptoethanol DNA Ethidium Cisplatin
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Jennette K W
Lippard S J
Vassiliades G A
Bauer W R
References (20)
20 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
Published
1974-10-00
Pages
3839-43
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC434279
Subset
IM
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