Premium
The potent anti‐proliferative effect of 20‐EPI analogues of 1,25 dihydroxyvitamin D 3 in human breast‐cancer MCF‐7 cells is related to promoter selectivity
Author(s) -
Hansen Christina Mørk,
Danielsson Carina,
Carlberg Carsten
Publication year - 1996
Publication title -
international journal of cancer
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.475
H-Index - 234
eISSN - 1097-0215
pISSN - 0020-7136
DOI - 10.1002/(sici)1097-0215(19960904)67:5<739::aid-ijc24>3.0.co;2-z
Subject(s) - mcf 7 , cancer research , hormone response element , biological activity , biology , cancer cell , growth inhibition , medicine , breast cancer , cancer , reporter gene , endocrinology , chemistry , cell growth , gene , pharmacology , in vitro , human breast , biochemistry , gene expression , estrogen receptor
The hormone 1,25‐dihydroxyvitamin D 3 (VD) has a potential use as an anti‐tumor agent, but its clinical applications are restricted by its strong calcemic activity. This has led to the development of VD analogues with selectively increased growth‐inhibitory activity. One of the most potent analogues is KH1060, which is a 20‐epi‐22‐oxa‐derivative of VD. In human breast cancer MCF‐7 cells, we studied the growth‐inhibitory activities of a set of 8 analogues that cover conservative structural changes from 20‐epi‐VD (MC 1288) to KH1060. In the same cellular system, we analyzed the potential of these 8 analogues to stimulate reporter gene activity driven by a recently discovered novel‐type VD response element. We found that this VD response element is more appropriate than classical VD response elements to correlate anti‐proliferative effects of VD analogues with their gene‐regulatory properties. © 1996 Wiley‐Liss, Inc.