PMID- 10611474
OWN - NLM
STAT- MEDLINE
DCOM- 20000124
LR  - 20190621
IS  - 0014-5793 (Print)
IS  - 0014-5793 (Linking)
VI  - 464
IP  - 1-2
DP  - 1999 Dec 24
TI  - Specific hydroxylations determine selective corticosteroid recognition by human
      glucocorticoid and mineralocorticoid receptors.
PG  - 9-13
AB  - The ligand binding domains of the human mineralocorticoid receptor (hMR) and
      glucocorticoid receptor (hGR) display a high sequence homology. Aldosterone and
      cortisol, the major mineralocorticoid and glucocorticoid hormones, are very
      closely related, leading to the cross-binding of these hormones to both
      receptors. The present study reports on the mechanism by which hMR and hGR are
      activated preferentially by their cognate hormones. We found that the ability of 
      corticosteroids to stimulate the receptor's transactivation function is depending
      on the stability of the steroid-receptor complexes. In the light of a hMR
      structural model we propose that contacts through the corticosteroid C21 hydroxyl
      group are sufficient to stabilize hMR but not hGR and that additional contacts
      through the C11- and C17-hydroxyl groups are required for hGR.
FAU - Hellal-Levy, C
AU  - Hellal-Levy C
AD  - INSERM U478, Faculte de Medecine Xavier Bichat, Institut Federatif de Recherche
      02, 16 rue Henri Huchard, P.O. Box 416, 75780, Paris, France.
FAU - Couette, B
AU  - Couette B
FAU - Fagart, J
AU  - Fagart J
FAU - Souque, A
AU  - Souque A
FAU - Gomez-Sanchez, C
AU  - Gomez-Sanchez C
FAU - Rafestin-Oblin, M
AU  - Rafestin-Oblin M
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - FEBS Lett
JT  - FEBS letters
JID - 0155157
RN  - 0 (Adrenal Cortex Hormones)
RN  - 0 (Anti-Inflammatory Agents)
RN  - 0 (Glucocorticoids)
RN  - 0 (Receptors, Glucocorticoid)
RN  - 0 (Receptors, Mineralocorticoid)
RN  - 4964P6T9RB (Aldosterone)
RN  - 7S5I7G3JQL (Dexamethasone)
RN  - WI4X0X7BPJ (Hydrocortisone)
SB  - IM
MH  - Adrenal Cortex Hormones/*pharmacology
MH  - Aldosterone/metabolism
MH  - Animals
MH  - Anti-Inflammatory Agents/metabolism
MH  - Binding Sites
MH  - COS Cells
MH  - Dexamethasone/metabolism
MH  - Glucocorticoids/metabolism
MH  - Hydrocortisone/metabolism
MH  - Hydroxylation
MH  - Kinetics
MH  - Plasmids/metabolism
MH  - Protein Binding/drug effects
MH  - Protein Conformation
MH  - Receptors, Glucocorticoid/*metabolism
MH  - Receptors, Mineralocorticoid/*metabolism
MH  - Time Factors
MH  - Transfection
EDAT- 1999/12/28 00:00
MHDA- 1999/12/28 00:01
CRDT- 1999/12/28 00:00
PHST- 1999/12/28 00:00 [pubmed]
PHST- 1999/12/28 00:01 [medline]
PHST- 1999/12/28 00:00 [entrez]
AID - S0014579399016671 [pii]
AID - 10.1016/s0014-5793(99)01667-1 [doi]
PST - ppublish
SO  - FEBS Lett. 1999 Dec 24;464(1-2):9-13. doi: 10.1016/s0014-5793(99)01667-1.