Methods using estrogen receptor as a constitutive transcriptional activator and a repressor
AssigneeLa Jolla Cancer Research Foundation
InventorsMagnus Pfahl, Maty Tzukerman
Life of this patent
Estimating the term…
Abstract
The invention provides the discovery that estrogen receptor is a constitutive transcriptional activator and a repressor. These activities are lacking in the mutant estrogen receptor. The invention provides assays and methods for determining estrogen binding activity of ligands. The invention also provides therapeutic methods and the detection of pathologies associated with a mutated estrogen receptor.
Claims17
A method of comparatively determining the ability of a ligand to effect the constitutive activator or repressor activity of an estrogen receptor which has the constitutive activator or repressor activity and a estrogen receptor which lacks the constitutive activator or repressor activity comprising separately binding the ligand to the estrogen receptor which has the constitutive activator or repressor activity and the estrogen receptor which lacks the constitutive activator or repressor activity, determining the effect of the ligand on the activity of the estrogen receptor which has the constitutive activator or repressor activity and the estrogen receptor which lacks the constitutive activator or repressor activity, and comparing the activity.
A method of selecting a ligand which increases or decreases the basal level transcription or repressor activity of a estrogen receptor which lacks the constitutive activator or repressor activity comprising the steps of contacting the ligand with the estrogen receptor which lacks the constitutive activator or repressor activity, determining the effect of the ligand on basal level transcription, and selecting those ligands which either increase or decrease the basal level transcription.
A method of selecting a ligand for increasing or decreasing the constitutive activator or repressor activity of a estrogen receptor which lacks the constitutive activator or repressor activity compared to estrogen receptor which has the constitutive activator or repressor activity comprising the steps of separately contacting the estrogen receptor which lacks the constitutive activator or repressor activity and the estrogen receptor which has the constitutive activator or repressor activity with the ligand in separate reactions, comparing the effect of the ligand on the activity of the estrogen receptor which lacks the constitutive activator or repressor activity and the estrogen receptor which has the constitutive activator or repressor activity, and selecting those ligands which increase or decrease the activity of the estrogen receptor which lacks the constitutive activator or repressor activity more than the activity of the estrogen receptor which has the constitutive activator or repressor activity.
A method of diagnosing or predicting the predisposition of an individual to a pathology, associated with the constitutive activator or repressor activity of estrogen receptor, in an individual comprising detecting an estrogen receptor which lacks the constitutive activator or repressor activity, the presence of an estrogen receptor which lacks the constitutive activator or repressor activity indicating the pathology or a predisposition to the pathology.
Dependencies are inferred from the claim text.