PMID- 6327286
OWN - NLM
STAT- MEDLINE
DCOM- 19840709
LR  - 20220511
IS  - 0261-4189 (Print)
IS  - 1460-2075 (Electronic)
IS  - 0261-4189 (Linking)
VI  - 3
IP  - 4
DP  - 1984 Apr
TI  - DNA binding properties of glucocorticosteroid receptors bound to the steroid 
      antagonist RU-486.
PG  - 751-5
AB  - RU-486 is an anti-fertility steroid which also has anti-glucocorticosteroid 
      effects. RU-486 is shown to be a strong antagonist of the 
      glucocorticosteroid-induced cytolytic response of the murine thymoma lines W7TB 
      and T1M1b , and of the induction of mouse mammary tumor virus (MMTV) mRNA in 
      T1M1b cells. The glucocorticosteroid receptor of W7 cells has high affinity for 
      RU-486 (Kd = 3 X 10(-9) M) but the complex formed has low nuclear transfer 
      capacity. Binding of RU-486, as compared with the glucocorticosteroid agonist 
      triamcinolone acetonide, to mouse receptor results in a decreased affinity for 
      DNA in general and a reduced specific recognition of a site in the promoter 
      region of MMTV proviral DNA. The RU-486 complex formed with rat liver receptor 
      exhibits the same behavior; in addition, it is shown that only a fraction of 
      these complexes are activated by temperature and these form highly salt-sensitive 
      interactions with DNA. These results indicate that the binding of RU-486 to 
      glucocorticosteroid receptors mimics pharmacologically the properties of a class 
      of receptor variants (nt-) which are non-functional and have reduced nuclear 
      transfer and altered DNA binding capacity. These results substantiate the 
      importance of DNA binding in receptor function.
FAU - Bourgeois, S
AU  - Bourgeois S
FAU - Pfahl, M
AU  - Pfahl M
FAU - Baulieu, E E
AU  - Baulieu EE
LA  - eng
GR  - CA36146/CA/NCI NIH HHS/United States
GR  - GM20868/GM/NIGMS NIH HHS/United States
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, Non-P.H.S.
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - England
TA  - EMBO J
JT  - The EMBO journal
JID - 8208664
RN  - 0 (DNA, Viral)
RN  - 0 (Estrenes)
RN  - 0 (Glucocorticoids)
RN  - 0 (RNA, Messenger)
RN  - 0 (RNA, Viral)
RN  - 0 (Receptors, Glucocorticoid)
RN  - 0 (Receptors, Steroid)
RN  - 320T6RNW1F (Mifepristone)
RN  - 7S5I7G3JQL (Dexamethasone)
RN  - 9007-49-2 (DNA)
SB  - IM
MH  - Animals
MH  - Cell Line
MH  - DNA/*metabolism
MH  - DNA, Viral/metabolism
MH  - Dexamethasone/metabolism
MH  - Estrenes/metabolism/*pharmacology
MH  - Glucocorticoids/*antagonists & inhibitors
MH  - Mammary Tumor Virus, Mouse/genetics
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Mifepristone
MH  - RNA, Messenger/biosynthesis
MH  - RNA, Viral/biosynthesis
MH  - Receptors, Glucocorticoid/*metabolism
MH  - Receptors, Steroid/*metabolism
MH  - Thymoma/*metabolism
MH  - Transcription, Genetic/drug effects
PMC - PMC557421
EDAT- 1984/04/01 00:00
MHDA- 1984/04/01 00:01
PMCR- 1985/04/01
CRDT- 1984/04/01 00:00
PHST- 1984/04/01 00:00 [pubmed]
PHST- 1984/04/01 00:01 [medline]
PHST- 1984/04/01 00:00 [entrez]
PHST- 1985/04/01 00:00 [pmc-release]
AID - 10.1002/j.1460-2075.1984.tb01879.x [doi]
PST - ppublish
SO  - EMBO J. 1984 Apr;3(4):751-5. doi: 10.1002/j.1460-2075.1984.tb01879.x.