On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.
J Med Chem
; 50(26): 6722-4, 2007 Dec 27.
Article
in En
| MEDLINE
| ID: mdl-18052088
ABSTRACT
The estrogen-related receptor alpha (ERRalpha) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRalpha have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRgamma. The results suggest that ERRalpha may be intractable as a direct target for pharmacologic activation.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Receptors, Estrogen
/
Hydrazones
Limits:
Humans
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2007
Type:
Article
Affiliation country:
United States