334 results about "Estrogen receptor" patented technology

This invention describes a system for generating multiple simultaneous tunable electron and photon beams and monochromatic x-rays for all field simultaneous radiation therapy (AFSRT), tumor specific AFSRT and screening for concealed elements worn on to the body or contained in a container. Inverse Compton scattering renders variable energy spent electron and tunable monochromatic x-rays. It's spent electron beam is reused for radiation with electron beam or to generate photon beam. Tumor specific radiation with Auger transformation radiation is facilitated by exposing high affinity tumor bound heavy elements with external monochromatic x-rays. Heavy elements like directly iodinated steroid molecule that has high affinity binding to estrogen receptor in breast cancer and to iodinated testosterone in prostate cancer or with directly implanted nanoparticles into the tumor are exposed with tuned external monochromatic x-rays for tumor specific radiation therapy. Likewise, screening element's atom's k, l, m, n shell specific Auger transformation radiation generated by its exposure to external monochromatic x-rays is used to screen for concealed objects. Multiple beam segments from a beam storage ring or from octagonal beam lines are simultaneously switched on for simultaneous radiation with multiple beams. The beam on time to expose a tumor or an object is only a few seconds. It also facilitates breathing synchronized radiation therapy. The intensity modulated radiation therapy (IMRT) and intensity modulated screening for concealed objects (IMSFCO) is rendered by varying beam intensities of multiple simultaneous beams. The isocentric additive high dose rate from simultaneously converging multiple beams, the concomitant hyperthermia and chemotherapy and tumor specific radiation therapy and the AFSRT's very low radiation to the normal tissue all are used to treat a tumor with lower radiation dose and to treat a radioresistant and multiple times recurrent tumors that heave no other alternative treatments.

Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.

Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.

The present disclosure relates to methods of determining a treatment course of action. In particular, the present disclosure relates to mutations in the gene encoding estrogen receptor and their association with responsiveness to estrogen therapies for cancer.

Disclosed herein are systems, methods and compositions for rapidly and reversibly destabilizing a target protein in vitro or in vivo, in the presence or absence of a cell-permeable, synthetic molecule or ligand.

3,15-substituted estrone compounds which act as inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I enzymes and / or requiring the lowering of the endogenous 17β-estradiol concentration, as well as the general use of selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.

Compounds of the formula (I) for use as an estrogen receptor -β-selective ligand are described wherein: X is O or S; and R1, R3-R6 are as described in the specification. The use of these compounds in treating Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis, cardiovascular disease, rheumatoid arthritis and prostate cancer is described; as are processes for making them.

A novel classification system for breast cancer based on normal breast cell phenotypes and various expression levels of estrogen receptor (ER), androgen receptor (AR), and vitamin D receptor (VDR). The various categories of the classification system are associated with different survival rates and prognoses. The invention includes a method of classifying breast cancer comprises measuring the levels of ER, AR, and VDR in the cancerous tissue, and classifying the breast cancer into one of the above-noted categories according to expression levels. The invention includes a method of predicting the prognosis of breast cancer in a patient and a method of determining a treatment regimen for breast cancer depending on the category in which the breast cancer is classified. The invention includes a method of treating breast cancer according to the expression profile of ER, AR, and VDR detected in the cancerous tissue. Kits for detecting the same are also provided.

The various embodiments of the present disclosure relate generally to compositions and methods for the targeted cellular delivery of nanoparticles. More particularly, the various embodiments of the present invention are directed to the cellular delivery of nanoparticles tethered to a ligand by way of a poly(ethylene glycol) linkage, wherein the ligand demonstrates a binding specificity for a cellular target. In an exemplary embodiment, the ligand is tamoxifen and the cellular target is the estrogen receptor, which is upregulated in many breast cancer cells.

Disclosed herein are methods for diagnosing or treating pregnancy related hypertensive disorders that include the use of a polypeptide or a nucleic acid encoding a polypeptide selected from the following: follistatin related protein, interleukin 8, inhibin A, VEGF-C, angiogenin, beta fertilin, hypothetical protein, leukocyte associated Ig-like receptor secreted protein, erythroid differentiation protein, adipogenesis inhibitory factor, corticotropin releasing factor binding protein, alpha-1 anti-chymotrypsin, insulin-like growth factor binding protein-5, CD33L, cytokine receptor like factor 1, platelet derived endothelial growth factor, lysyl hydroxylase isoform 2, stanniocalcin precursor, secreted frizzled related protein, galectin-3, alpha defensin, ADAM-TS3, cholecystokinin precursor, interferon stimulated T-cell alpha chemoattractant precursor, azurocidin, sperminine oxidase, UDP glycosyltransferase 2 family polypeptide B28, neurotrophic tyrosine kinase receptor 2, neutral endopeptidase, CDC28 protein kinase regulatory subunit 2, beta glucosidase, lanosterol synthase, calcium / calmodulin-dependent serine protein kinase, estrogen receptor-alternatively spliced transcript H, chemokine (CX3C motif) receptor 1, tyrosinase-related protein 1, hydoxy-delta-5-steroid dehyrogenase, dihydropyramidinase-like-4, and cytochrome P450-family 11.

The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

The present invention is directed to novel heterocyclic benzo[c]chromene derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

The present invention concerns a method of treatment or prevention of myocardial ischemia-reperfusion injury by diagnosing that a person is in need of treatment or prevention of myocardial ischemia-reperfusion injury and administering a therapeutically effective amount of a ligand which modulates NF-kB transcription factor by interaction with estrogen receptor ER-α, estrogen receptor ER-β, or both ER-α and ER-β estrogen receptors with a substantial absence of creatine kinase stimulation. In certain preferred embodiments, the administration is substantially without uterotropic activity.

The present invention relates generally to a method for modulating steroidogenic activity and a composition useful for same. The present invention further relates to a composition comprising a steroidogenic modulator useful for modulating physiological processes mediated by the androgen receptor or an active form thereof or complex comprising same and / or for modulating physiological processes mediated by estrogen receptors. The composition of the present invention preferably comprises an extract of herbs or botanical or horticultural equivalents of the herbs or chemical or functional equivalents of one or more components of the herbal extract thereof.

The invention provides a two-hybrid yeast for detecting estrogen-like compounds in environmental samples and a preparation method thereof, wherein the yeast contains pGBKT7-ER yeast expression plasmids and pGAD424-GRIP1 yeast expression plasmids, wherein the pGBKT7-ER yeast expression plasmids contain estrogen receptor genes, and the pGAD424-GRIP1 yeast expression plasmids contain estrogen receptor coactivated factor genetic fragments with the sequence of SEQ ID No.2. The invention also provides a bioassay method for detecting the estrogen-like compounds in the environment, which comprises: co-culturing two-hybrid yeast cells and a sample to be detected, adding a reaction liquid of o-nitrobenzene-beta-D-galactopyranoside for reaction, and calculating the concentration of the estrogen-like compounds according to the detected absorbance value of supernatant at 420 nanometers after the reaction stops. The invention adopts the two-hybrid yeast of recombinant estrogen receptor genes for test, and is more close to the actual action conditions of an endocrine system of a mammal; constructed yeast cell genes have stable character and are easy to culture and screen; the screening process of the whole estrogen-like effect is simple to operate; and the required quantity of the sample is small, and the cost is low.

This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.

The present invention provides isolated polypeptides having an amino acid sequence having at least 70% identity to SEQ ID N0:20, wherein the polypeptide has ER-α36 activity. The invention further provides methods for identifying agents that bind to such polypeptides, methods for detecting such polypeptides, and methods for altering the activity of such polypeptides. Also provided are antibodies that specifically bind to an amino acid sequence depicted at SEQ ID NO:1, or an immunogenic fragment thereof, and methods for making and using such antibodies.

The invention relates to the technical field of medicaments, in particular to application of 12 isoflavone compound monomers comprising belamcanda chinensis total isoflavone or tecoridin, wild tectoridin, tectorigenin, iridin and the like in preparing medicaments and food for preventing and treating lower women's estrogen level and retarding womb and ovarian failure or climacteric syndrome. Animal experiment results show that the total isoflavone or 12 isoflavone compound monomers in the belamcanda chinensis have remarkable pharmacological effects of improving the estrogen level, promoting the growth of follicle, promoting epitheliosis of womb and vagina, retarding womb and ovarian failure, improving the expression of an epithelial cell estrogen receptor of the vagina and the like, so the total isoflavone or 12 isoflavone compound monomers can be used for preparing the medicaments or food for preventing and treating lower women's estrogen level and retarding womb and ovarian failure or climacteric syndrome. The application provides a new source for seeking a plant estrogen medicament.

The invention relates to an inducible inheritance recombinase system CrexER. The CrexER is a fusion protein; the fusion protein is a protein formed by fusing recombinase Cre, estrogen receptors ER andrecombination sites rox specifically recognized by recombinase Dre. The invention also provides a coding sequence of the fusion protein, a nucleic acid construct containing the coding sequence, a host cell and the like. The ahead occurrence of Dre-rox homologous recombination is used for inducing the subsequent occurrence of Cre-loxP homologous recombination; the targeted operation of the A-Dre and B-Cre mark cell intersection (A+B+) is realized. The application range of the inheritance targeted operation is greatly expanded; a precious strategy is provided for the precise inheritance targeted operation and biomedical research.

Disclosed herein are methods for diagnosing or treating pregnancy related hypertensive disorders that include the use of a polypeptide or a nucleic acid encoding a polypeptide selected from the following: follistatin related protein, interleukin 8, inhibin A, VEGF-C, angiogenin, beta fertilin, hypothetical protein, leukocyte associated Ig-like receptor secreted protein, erythroid differentiation protein, adipogenesis inhibitory factor, corticotropin releasing factor binding protein, alpha-1- anti-chymotrypsin, insulin-like growth factor binding protein-5, CD33L, cytokine receptor like factor 1, platelet derived endothelial growth factor, lysyl hydroxylase isoform 2, stanniocalcin precursor, secreted frizzled related protein, galectin-3, alpha defensin, ADAM-TS3, cholecystokinin precursor, interferon stimulated T-cell alpha chemoattractant precursor, azurocidin, sperminine oxidase, UDP glycosyltransferase 2 family polypeptide B28, neurotrophic tyrosine kinase receptor 2, neutral endopeptidase, CDC28 protein kinase regulatory subunit 2, beta glucosidase, lanosterol synthase, calcium / calmodulin-dependent serine protein kinase, estrogen receptor-alternatively spliced transcript H, chemokine (CX3C motif) receptor 1, tyrosinase-related protein 1, hydoxy-delta-5-steroid dehyrogenase, dihydropyramidinase-like-4, and cytochrome P450-family 11.

The invention relates to the fields of pharmaceutical chemistry and organic chemistry, in particular to isoquinolinone derivatives. The compounds can be used for treating various medical indications associated with postmenopausal symptoms, uterine fiber lesions and arterial smooth muscle cell proliferation, particularly ER-(+) breast cancer by inhibiting alpha-estrogen receptor subtype (ER alpha) and through vascular endothelial growth factor receptor (VEGFR-2) bi-target. Meanwhile, the compounds have an obvious inhibiting effect on tumor metastasis, and have a general formula I.

Compounds of the formula (I) for use as an estrogen receptor-β-selective ligand are described wherein: X is O or S; and R1, R3 R6 are as described in the specification. The use of these compounds in treating Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis, cardiovascular disease, rheumatoid arthritis and prostate cancer is described; as are processes for making them.

The invention belongs to the field of Chinese medicine pharmacy, and relates to a traditional Chinese medicine composition for treating menopausal syndrome and a preparation method of the traditional Chinese medicine composition. The traditional Chinese medicine composition comprises traditional Chinese medicine radix rehmanniae, radix paeoniae alba, rhizoma anemarrhenae, golden cypress, morinda officinalis, herba epimedii, raw oyster shell, crude dragon bone, radix bupleuri and tuber fleeceflower stem as main medicines, and is blended with auxiliary materials to be prepared into the preparation for treating the symptoms related to menopause, i.e. the heating, the sweating, the agitated emotion, the insomnia and the like. The experiment proves that the traditional Chinese medicine composition provided by the invention has the definite functions for improving the blood serum E2 and reducing the blood serum FSH (follicle-stimulating hormone), the hypothalamus estrogen receptors Er alpha, Er beta gene expression and protein expression can be continuously adjusted, and the situation of hypothalamus aging can be improved, so that the menopausal syndrome can be effectively cured.

The invention relates to a furan-azo-[3,2-g] chromene derivative and application thereof, belonging to the technical field of medicine. The furan-azo-[3,2-g] chromene derivative comprises stereoisomers and pharmaceutically applicable salts of a compound of the furan-azo-[3,2-g] chromene derivative and has a structural general formula shown in the specification of the invention. The furan-azo-[3,2-g] chromene derivative and pharmaceutically applicable acid addition salts of the compound can be used as an estrogen receptor regulator singly or by combining with traditional drugs to treat or prevent various diseases related to estrogen functions, such as bone loss, fracture, osteoporosis, hot flash, LDL (Low Density Lipoprotein) cholesterol level rise, angiocardiopathy, cognitive function impairment, brain-wasting diseases, anxiety, depression caused by estrogen shortage, inflammation, inflammatory bowel diseases, sexual dysfunction, hypertension, retinosis and cancer, especially breast cancer, ovarian cancer, osteosarcoma, endometrial cancer and prostatic cancer.

The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative.

Disclosed herein are novel di-phenyl compounds and methods for using various di-phenyl compounds for treatment and prevention of diseases and disorders related to estrogen receptors.

The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject.