Progesterone receptor (PR) is hormone receptor protein. There are already a lot of PR binding ligands tested by experiments. So my question is, is there a ligand, also tested in experiments, that could not bind to this protein?
Additional information: Here I am doing some molecular docking against PR LBD. And I know RU486 and progesterone, or asoprisnil are good binders of PR LBD. However, I'd like to know, whether there are some published papers using some other molecules as negative controls, which show very low or absolutely no binding affinities against PR LBD?
Curr Opin Investig Drugs. 2006 Oct;7(10):882-90.
Progesterone receptor antagonists.
Spitz IM1.
Author information
1 Institute of Hormone Research, 14 Nili Street, Jerusalem 92548, Israel. [email protected]
Abstract
Since the discovery of the progesterone receptor antagonist MIFEPRISTONE, numerous additional compounds, which display a spectrum of biological actions ranging from full antagonist to those with mixed agonist/antagonist activity, have been synthesized. The latter are referred to as selective progesterone receptor modulators. Long-term administration of these agents is associated with an antiproliferative action on the endometrium as well as amenorrhea and often inhibition of ovulation. Thus far, the majority of clinical data have been obtained with mifepristone but studies are currently underway with other compounds. These compounds have application in the treatment of uterine myoma, endometriosis, dysfunctional uterine bleeding, as potential contraceptives and in steroid responsive tumors.
PMID:
17086932
[PubMed - indexed for MEDLINE]
MIFEPRISTONE is also known as RU486, which is also a glucocorticoid receptor antagonist.
Thanks @Andrea Romano. I did a search about estrogen, I didn't see information about the complex of PR LBD with estrogen. Does this mean estrogen not binding to PR LBD?
Thank you @Merry Sherman. I understand that RU486 is a PR LBD antagonist with high binding affinity. In experiments, people may use some negative controls which totally not bind to PR LBD. Is there any those molecues?
@Pamela D. Noyes, thank you for the answer. Since I am doing some in silica screening for ligands against PR. Both new agonists and antagonist would be fine for me. However, I need to know some totally-no-binding-against-PR ligands. If there is any been tested in experiments, that would be useful for my virtual screening.
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