Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists
Journal Article
·
· Bioorg. Med. Chem. Lett.
Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring was designed. Members of this class of N-alkylpyrrolidines demonstrate potent and highly selective partial agonism of the progesterone receptor, and one of these analogs was shown to be efficacious upon oral dosing in the OVX rat model of estrogen opposition.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1006164
- Journal Information:
- Bioorg. Med. Chem. Lett., Vol. 19, Issue (16) ; 08, 2009; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
Similar Records
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
Effects of ovarian hormones on beta-adrenergic and muscarinic receptors in rat heart
Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-[gamma]
Journal Article
·
Fri Sep 17 00:00:00 EDT 2010
· Bioorg. Med. Chem. Lett.
·
OSTI ID:1006164
+18 more
Effects of ovarian hormones on beta-adrenergic and muscarinic receptors in rat heart
Journal Article
·
Fri Jan 01 00:00:00 EST 1988
· Life Sci.; (United States)
·
OSTI ID:1006164
Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-[gamma]
Journal Article
·
Thu Mar 07 00:00:00 EST 2013
· J. Med. Chem.
·
OSTI ID:1006164
+14 more