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Virtual and biomolecular screening converge on a selective agonist for GPR30
The identification of the first G PR30-specific agonist, G-1 (1), capable of activating GPR30 in a complex environment of classical and new estrogen receptors is described.
Estrogen signaling through the transmembrane G protein-coupled receptor GPR30.
- E. Prossnitz, J. B. Arterburn, H. Smith, T. Oprea, L. Sklar, H. Hathaway
- BiologyAnnual review of physiology
- 13 February 2008
An overview of the evidence for the cellular and physiological actions of GPR30 in estrogen-dependent processes and the relationship of G PR30 with classical estrogen receptors is provided.
BDDCS Applied to Over 900 Drugs
The potential use of BDDCS to estimate the disposition characteristics of novel chemicals (new molecular entities) in the early stages of drug discovery and development and the influence of several measured and in silico parameters in the process of B DDCS category assignment is discussed in detail.
In vivo Effects of a GPR30 Antagonist
In vivo administration of G15 reveals that GPR30 contributes to both uterine and neurological responses initiated by estrogen, and the identification and characterization of a G-1 analog, G15, that binds to G PR30 with high affinity and acts as an antagonist of estrogen signaling through GPR28.
A comprehensive map of molecular drug targets
An updated comprehensive map of molecular targets of approved drugs is presented and the relationships between bioactivity class and clinical success, as well as the presence of orthologues between human and animal models and between pathogen and human genomes are explored.
Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity
Property distribution of drug-related chemical databases*
- T. Oprea
- ChemistryJ. Comput. Aided Mol. Des.
- 1 March 2000
Property distribution was examined in the following compound databases: MACCS-II Drug Data Report (MDDR), Current Patents Fast-alert, Comprehensive Medicinal Chemistry, Physician Desk Reference, New Chemical Entities, and the Available Chemical Directory.
Temporal disease trajectories condensed from population-wide registry data covering 6.2 million patients
A discovery-driven analysis of temporal disease progression patterns using data from an electronic health registry covering the whole population of Denmark, which suggests such trajectory analyses may be useful for predicting and preventing future diseases of individual patients.
G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells.
It is shown that, in ERalpha-positive BG-1 ovarian cancer cells, both E2 and the GPR30-selective ligand G-1 induced c-fos expression and estrogen-responsive element (ERE)-independent activity of a c- fos reporter gene, whereas only E2 stimulated an ERE-responsive reporter gene.
The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.
GPR30 antagonizes growth of ERalpha-positive breast cancer and may represent a new target to combat this disease.