The Library
An estrogen-platinum terpyridine conjugate : DNA and protein binding and cellular delivery
Tools
Hannon, M. J. (Michael J.), Green, Philip S., Fisher, Dianne M., Derrick, Peter J., Beck, Jennifer L., Watt, Stephen J., Ralph, Stephen F., Sheil, Margaret M., Barker, Philip R., Alcock, Nathaniel W., Price, Robert J., Sanders, Karen J., Pither, Richard, Davis, Julie and Rodger, Alison (2006) An estrogen-platinum terpyridine conjugate : DNA and protein binding and cellular delivery. CHEMISTRY-A EUROPEAN JOURNAL, 12 (31). pp. 8000-8013. doi:10.1002/chem.200501012 ISSN 0947-6539.
Research output not available from this repository.
Request-a-Copy directly from author or use local Library Get it For Me service.
Official URL: http://dx.doi.org/10.1002/chem.200501012
Abstract
A platinum metal complex in which terpyridine joins estradiol (via an ethynyl link) to a platinum with a labile ligand (chloride) has been designed, synthesised and its X-ray crystal structure determined. The aim of this work was to link a targeting motif (in this case estrogen) to a metal-based biomolecule recognition unit (the platinum moiety). The target molecule: 17 alpha-[4'-ethynyl-2,2':6',2'-terpyridine]-17 beta-estradiol platinum(n) chloride (PtEEtpy) has been shown to bind to both human and bovine serum albumin (SA) and to DNA. FTICR mass spectrometry shows that the bimolecular units are in each case linked through coordination to the platinum with displacement of the chloride ligand. Circular dichroism indicates that a termolecular entity involving PtEEtpy, SA and DNA is formed. A range of electrospray mass spectrometry experiments showed that the PtEEtpy complex breaks and forms coordination bonds relatively easily. A whole cell estrogen receptor assay in an estrogen receptor positive cell (MCF-7) confirms binding of both EEtpy and PtEEtpy to the estrogen receptor in cells. The work demonstrates the concept of linking a targeting moiety (in this case estrogen) to a DNA binding agent.
Item Type: | Journal Article | ||||
---|---|---|---|---|---|
Subjects: | Q Science > QD Chemistry | ||||
Journal or Publication Title: | CHEMISTRY-A EUROPEAN JOURNAL | ||||
Publisher: | WILEY-V C H VERLAG GMBH | ||||
ISSN: | 0947-6539 | ||||
Official Date: | 25 October 2006 | ||||
Dates: |
|
||||
Volume: | 12 | ||||
Number: | 31 | ||||
Number of Pages: | 14 | ||||
Page Range: | pp. 8000-8013 | ||||
DOI: | 10.1002/chem.200501012 | ||||
Publication Status: | Published |
Data sourced from Thomson Reuters' Web of Knowledge
Request changes or add full text files to a record
Repository staff actions (login required)
View Item |