80 results about "Thyroid hormone receptor" patented technology

The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three dimensional structure of nuclear receptors, particularly the thyroid receptor (herein referred to as "TR"). Also provided are crystals, nuclear receptor synthetic ligands, and related methods.

The invention concerns the use of TGF-beta inhibitors to counteract a pathologic change in the expression level, activity and / or signaling of a receptor of the steroid-thyroid hormone receptor superfamily. In particular, the invention concerns a method for counteracting a pathologic change in a signal-transduction pathway involving a member of the steroid / thyroid hormone super-family, comprising administering to a mammalian subject in need an effective amount of a compound capable of inhibiting TGF-beta signaling through a TGF-beta receptor.

The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.

The invention discloses an FSHR (follicle stimulating hormone receptor) gene based molecular marker related to porcine reproduction traits as well as a detection method and an application of the molecular marker. The molecular marker is a porcine FSHR gene segment which contains a polymorphic locus, and the polymorphic locus is at the 1,166th site in a sequence shown in the SEQ ID NO.1 and has C / T base variation. The detection method comprises the following steps: a primer is designed according to the nucleotide sequence of the molecular marker; PCR (polymerase chain reaction) amplification is performed with genomic DNA of a to-be-detected pig as a template; the type of a polymorphic locus in a PCR amplification product is judged. The invention further discloses the application of the molecular marker in selection of the porcine reproduction traits. According to an FSHR gene mutation site, the FSHR gene based molecular marker related to the porcine reproduction traits as well as the detection method and the application of the molecular marker are provided, and foundation is provided for porcine molecular breeding and development of a physiological mechanism for porcine reproduction.

The invention discloses a group of genes used for prognosis of hormone receptor-positive breast cancer and applications thereof. The genes comprise genes ESR1, PGR, ERBB2 and MKI67. The applications of the genes include a multiple parallel detection liquid-phase gene chip used for the prognosis of the hormone receptor-positive breast cancer, a kit used for the prognosis of the hormone receptor-positive breast cancer and a gene evaluating system for the prognosis of the hormone receptor-positive breast cancer. By liquid-phase gene chip detection for the gene ESR1, the gene PGR, the gene ERBB2 and the gene MKI67, a large amount of film reading and identification by doctors in a pathology department can be largely reduced, doubtful film reading results in pathology are overcome, the accuracy is almost the same as that of IHC, and the genes and the applications are advantaged by being efficient and sensitive in parallel detection, easy in operation, and the like.

The present invention relates to deuterated pyridazinone and derivatives and pharmaceutical compositions thereof. Specifically, the compound has a structure shown as a formula (I), and the definitionsof all groups and substituents are as described in the specification. The compounds have a selective agonistic effect and / or better pharmacodynamic properties on thyroid hormone beta receptors.

New thyroid receptor ligands are provided which have the general formula I wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.

A previously isolated hepatitis B virus (HBV) integration in a 147 bp cellular DNA fragment linked to hepatocellular carcinoma (HCC) was used as a probe to clone the corresponding complementary DNA from a human liver cDNA library. Nucleotide sequence analysis revealed that the overall structure of the cellular gene, which has been named hap, is similar to that of the DNA-binding hormone receptors. Six out of seven hepatoma and hepatoma-derived cell-lines express a 2.5 kb hap mRNA species which is undetectable in normal adult and fetal livers, but present in all non-hepatic tissues analyzed. Low stringency hybridization experiments revealed the existence of hap related genes in the human genome. The cloned DNA sequence is useful in the preparation of pure hap protein and as a probe in the detection and isolation of complementary DNA and RNA sequences. The hap protein is a retinoic acid (RA) receptor identified as RAR-β.

The present invention provides a mouse hybrid tumor cell strain (preserving number: ATCC GHR-106PTA-10252) and a monoclonal antibody (GHR-106) of anti-gonadotropin-releasing hormone receptor which is secreted from the mouse hybrid tumor cell strain. The antibody can perform effective inbibitional effect for the tumor cell through combining with the surface receptor of tumor cell. Then the antibody can be used for the diagnosis and treatment process of tumor and the application for preparing the antitumor drug.

The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and / or diabetes.

In accordance with the present invention, there are provided expression systems for the production of function glucocorticoid receptor proteins, methods for the recombinant production of glucocorticoid receptor proteins as well as sequences encoding novel members of the steroid / thyroid hormone superfamily of receptors (e.g., glucocorticoid receptor). Invention expression systems comprise host cells containing DNA encoding functional glucocorticoid receptor proteins, wherein the DNA is operably linked to control sequences compatible with host cells, thereby enabling the expression of functional receptor proteins. The invention method is carried out by culturing such recombinant host cells, and recovering the functional glucocorticoid receptor proteins produced thereby. In accordance with the present invention, there are also provided substantially pure DNA's comprised of sequences which encode members of the steroid / thyroid hormone receptor superfamily having the hormone-binding and / or transcription-activating characteristics of a glucocorticoid receptor. The invention also provides various plasmids containing receptor sequences which exemplify the DNA's of the invention. The invention further provides receptor proteins, including modified functional forms thereof, expressed from the DNA's (or mRNA's) of the invention.

Monoclonal antibodies against gonadotropin releasing hormone (GnRH) receptor induce cellular apoptosis of various cancer cells expressing this surface receptor. The monoclonal antibodies and their humanized forms, or fragments thereof, can serve as anti-cancer agents for the treatment of cancer in humans, and can function as analogs of GnRH to affect regulation of reproductive functions or fertility in humans.

The invention belongs to the field of aquatic product biogenetic engineering, and discloses an electroporation transfection method of eyespot larvae of mytilus coruscus. siRNA is designed according toa full-length sequence of thyroid hormone receptor genes of the mytilus coruscus obtained by clone, and different parameter settings are adopted to analyze the knock reduction situations of differentpulse patterns on the thyroid hormone receptor genes; the larvae after 96 hours of electroporation transfection are collected, and larvae RNA is extracted; and thyroid hormone receptor gene primers are designed, and the expression situation of the thyroid hormone receptor genes is detected by a fluorogenic quantitative PCR. According to the electroporation transfection method of the eyespot larvae of the mytilus coruscus, compared with the treatment without siRNA and non-sense siRNA, results show that the addition of the thyroid hormone receptor gene siRNA significantly reduces the expressionquantity of the genes, and the knock reduction efficiency is nearly 100%.

The invention provides an anti-tumor compound, and the structural formula of the anti-tumor compound is as followed (please see the structural formula in the description). The invention further provides a preparation method of the compound, and the method has the advantages of being simple in step and high in yield. According to the compound, proliferation of tumor cells can be inhibited through targeted thyroid hormone receptor interaction 13 genes or proteins, the purpose of preventing and treating tumors is achieved, and experiments prove that the compound can be used for preventing and treating the tumors such as multiple myeloma and lymphoma. Due to the fact that the compound is a small-molecule targeted compound, compared with an untargeted drug, the compound is better in effect and fewer in side effect and has the good application prospect in the cancer field.

The invention provides a two-hybrid yeast cell for detecting thyrotropic hormone-like / antithyrotropic hormone compounds in a sample and a preparation method thereof, wherein a yeast contains pGBT9-TR yeast expression plasmids and pGAD424-GRIP1 yeast expression plasmids, wherein the pGBT9-TR yeast expression plasmids contain thyroid hormone receptor genes, and the pGAD424-GRIP1 yeast expression plasmids contain thyroid hormone receptor coactivated factor genetic fragments with the sequence of SEQ ID No.2. The invention also provides a bioassay method for detecting the thyrotropic hormone-like / antithyrotropic hormone compounds in the sample. The yeast and the bioassay method greatly improve the sensitivity of the thyrotropic hormone-like / antithyrotropic hormone compounds. The constructed yeast has stable characteristics and is easy to culture and screen; the screening process of the whole thyrotropic hormone-like / antithyrotropic hormone effect is simple to operate; and the required quantity of the sample is small, and the cost is low.

The invention relates to a 6-oxo-1, 6-dihydropyridine derivative, a preparation method of the 6-oxo-1, 6-dihydropyridine derivative and application of the 6-oxo-1, 6-dihydropyridine derivative in medicine. Specifically, the invention relates to a 6-oxo-1, 6-dihydropyridine derivative as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative and application of the derivative as a therapeutic agent, especially in preparation of drugs for treating and / or preventing thyroid hormone receptor regulation diseases. Each substituent in the general formula (I) is as defined in the specification.

The invention discloses a deuterated pyridazinone compound as shown in a formula (I), a stereoisomer, a solvate, a co-crystal or pharmaceutically acceptable salt and a composition thereof, and a corresponding preparation method, and provides application of the compound in preparation of medicines for treating thyroid hormone receptor mediated diseases. In the formula (I), R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently selected from H and D respectively and are not H at the same time.

Belonging to the technical field of goat genetic marker preparation, the invention in particular relates to a molecular marker related to goat growth traits and application thereof. The molecular marker is obtained by cloning of a sixth intron sequence of a goat TR alpha gene, and the nucleotide sequence of the gene is shown as a sequence table SEQ ID NO:1. Base mutation of C230-T230 occurs at a 230th base of the sequence shown as the sequence table SEQ ID NO:1, and results in NdeI-RFLP polymorphism. The invention also discloses a preparation method of the molecular marker and application of a polymorphic detection method, and provides a new genetic marker for marker assisted selection of goat.

The present invention relates to a method for searching myelin using gonadotropin-releasing hormone receptors (GnRH-R) as a biomarker, more precisely, a method for investigating the distribution of myelin by immunohistochemical staining using GnRH-R antibody, based on the fact that GnRH-R and myelin are observed in the same region. The method for searching myelin of the invention can contribute to the studies on demyelination related degenerative brain disease and the disclosure of functions of myelin and the relation of myelin and GnRH-R.