Otto, Angela M. and Faderl, Michael and Schönenberger, Helmut (1991) Dissociation of estrogenic and cytotoxic properties of an estrogen receptor-binding platinum complex in human breast cancer cell lines. Cancer research 51 (12), pp. 3217-3223.
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The Pt complex [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]diaqua-Pt(II) sulfate (meso-6-PtSO4) was designed with the concept of combining the cytotoxic cisplatin with an estrogen receptor (ER)-binding ligand for targeting to ER+ mammary tumor cells. This Pt complex selectively inhibits growth of ER+ mammary tumors in rodents. To study the cellular mechanisms of action, cultures of 2 human mammary tumor cell lines, MCF-7 (ER+) and MDA-MB231 (ER-), were used and the effects of estradiol, tamoxifen, and cisplatin compared with those of meso-6-PtSO4. The relative binding affinity of the meso-6-PtSO4 to the ER in MCF-7 cells was 0.35 compared to estradiol (relative binding affinity, 100). The Pt complex was able to induce ER processing and increase the level of the progesterone receptor at concns. of 1-10 nM. Growth of MCF-7 cells was inhibited at concns. of meso-6-PtSO4 > 10 micro M. MDA-MB231 cells were inhibited likewise by the Pt complex, indicating a lack of selectivity for the ER+ cells. Meso-6-PtSO4 possesses both estrogen-like and cisplatin-like properties. Since growth inhibition did not correlated with ER-mediated processes, these 2 properties are expressed independently at the cellular level. The selective growth inhibitory effect of meso-6-PtSO4 in vivo is suggested to involve endocrinol. and/or immunol. factors.
|Additional information (public):||CAN 115:64205 1-6 Pharmacology 105856-32-4 Role: PRP (Properties) (antitumor effects of, mammary estrogen receptor binding in relation to)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Receptors Role: BIOL (Biological study) (for estrogens, platinum complexes antitumor effects and binding to mammary) Neoplasm inhibitors (platinum complexes as, mammary estrogen receptor binding in relation to) Estrogens Role: BIOL (Biological study) (receptors for, platinum complexes antitumor effects and binding to mammary) Mammary gland (neoplasm, estrogen receptors of, platinum complexes cytotoxicity in relation to binding to) platinum complex antitumor mammary estrogen receptor|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||12 Nov 2010 07:08|
|Last Modified:||12 Nov 2010 07:08|