38 results about "Hormone activity" patented technology

Compositions and methods are disclosed for the treatment of diabetes and related diseases using peptides with incretin hormone activity. Preferably, the peptide with incretin hormone activity is GLP-1, exendin or an analog of GLP-1 or exendin. The peptides with incretin hormone activity are administered transepithelially using a transepithelial carrier peptide. The transepithelial peptide contains sufficient amino, guanidine or amidino groups to stimulate transepithelial delivery. In some embodiments, the transepithelial carrier and the peptide with incretin hormone activity are embedded in a pressure sensitive adhesive layer of a plaster or patch.

A bifunctional hormone exhibiting an alpha-MSH activity and a natriuretic peptide activity is described. The bifunctional hormone comprises for example a first domain having alpha-MSH related hormonal activity covalently linked to a second domain having natriuretic peptide related hormonal activity. The bifunctional hormone of the present invention is useful for example for the prevention and / or treatment of renal related diseases or conditions, such as acute renal failure (ARF) or acute kidney injury (AKI).

A method of reducing extracellular brain glutamate levels is provided. The method comprising administering to a subject in need thereof an agent capable of modulating stress hormone activity thereby reducing blood glutamate levels, thereby reducing extracellular brain glutamate levels.

The invention discloses 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone of dye lignin derivative, a preparation method and an application of the 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone. The 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone obtained by chemically modifying the dye lignin derivative has the acetylcholinesterase inhibition activity, the estrogen activity and the nerve cell protective action; and the 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone which is taken as a multi-function target spot can be used for preparing the alzheimer disease-resistant medicament.

Disclosed are novel peptides inhibitory of the activity of vascular endothelial growth factor (VEGF) and their use in the treatment of angiogenesis-related diseases, including cancer. A combinatorial library of peptides consisting of six amino acid residues were chemically synthesize and, from the library, specific amino acid residues for each amino acid position were screened by comparing their inhibitory activity against VEGF binding to the cell surface receptor. The novel peptide sequences thus obtained bind to VEGF and block the binding of VEGF to its receptors present on the surface of vascular endothelial cells, thereby inhibiting the hormonal activity of VEGF. The peptides inhibit the angiogenesis induced by VEGF and human cancer cells. Also, the peptides inhibit growth and metastasis of human cancer cells transplanted to mice. Thus, the peptides can be used to treat angiogenesis-related diseases, including cancer, diabetic retinopathy, rheumatoid arthritis, etc.

The invention relates to the field of proteins, more specifically to those proteins that are located on the surface of the cell. The invention, among other things, provides an inhibitor or pharmaceutical composition capable of inhibiting down-regulation of a cell surface receptor. The invention provides a method to control or up-regulate hormone activity by using inhibitors or reagents that modify down-regulation of a protein. The invention further provides a method to control or up-regulate protein activity wherein ligand-induced receptor uptake and / or degradation by endocytosis of a receptor is inhibited, preferably by inhibiting the ubiquitin / proteasome system.

The invention relates to the field of proteins, more specifically to those proteins that are located on the surface of the cell. The invention, amongst others, provides an inhibitor or pharmaceutical composition that is capable of inhibiting down-regulation of a cell surface receptor. The invention provides a method to control or up-regulate hormone activity by using inhibitors or reagents that modify down-regulation of a protein. The invention further provides a method to control or up-regulate protein activity wherein ligand-induced receptor uptake and / or degradation by endocytosis of a receptor is inhibited, preferably by inhibiting the ubiquitin / proteasome system.

This invention discloses a determination kit box combining with protein testing the growing hormone activity in and animals and its preparation and test method characterizing that the box is composed of a solution prepared by a labeled growing hormone, unlabeled growing hormone, glucose enveloped carbon, general buffer solution and analytical solution and a specification. The method is that apart from setting 4-8 NSB tubes, two correspondent NSB tubes are specially designed for every sample to make the test more accurate. The glucose enveloped carbon preparation and quatily are necessary conditions for the accurate test.

The present invention obtains human proinsulin-KGD peptide protein molecule based on modern biochemical technology, by using the human proinsulin mutant, (CysA6Serú¼CysA11Serú¼DeltaB29- B30ú¼Delta A1)-human proinsulin, as molecular rack and through specific replacement with functional sequence CAKGDWNC containing Lys-Gly-Asp(KGD) in the original C peptide position. It is expressed effectively in pronucleus cell-colibacillus expression system, and the expressed product is purified through ultrasonic crushing, isoelectric precipitation, molecular sieve chromatographic separation, ion exchange chromatographic separation and other steps. The physical and chemical property analysis and the biological function detection show that the human proinsulin-KGD peptide protein has excellent molecular homogeneity, high GPIIb-IIIa acceptor recognizing and combining activity, powerful blood platelet coagulation inhibiting activity, no insulin hormone activity and no immunogenicity.

The subject invention provides for materials and methods of using dietary calcium, calcium-containing products, dairy and antagonists of calcitrophic hormone activity for inducing apoptosis in adipocytes in order to reduce the number of adipocytes in an individual regulating body weight.

The invention belongs to the field of medicine, and especially relates to an external preparation used for promoting hair growth and nourishing hair, and a preparation method thereof. 1000 parts of the external preparation comprise following ingredients, by weight, 1 to 7 parts of ginsenoside, 4 o 7 parts of cathe rine genistein, 40 to 60 parts of minoxidil, 1 to 7 parts of allantoin, 6 to 12 parts of menthol, 10 to 30 parts of azone, 200 to 350 parts of propylene glycol, 1 to 15 parts of phytosterol, 80 to 120 parts of purified water, and the balance ethyl alcohol. Beneficial effects of the external preparation are that: the external preparation is prepared via combination of traditional Chinese medicines with Western medicines; and phytosterol is added. The most significant function of phytosterol is 'intelligent management' parahormone function; phytosterol possesses a certain degree of hormone activity in body, but no hormone side effect is caused; when the hormone level of human body is higher than a normal value, phytosterol is capable of preventing bile hormone absorption, and reducing the hormone level of human body.

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

A method and apparatus for measuring binding between a plurality of molecules of a biological receptor protein and a plurality of molecules of a type which binds to said biological receptor is presented. Apparatus utilizes a sensor possessing a waveguide to which have been attached in close proximity to its surface, features resembling molecules having binding affinity for said biological receptor. Light is injected into said waveguide so as to produce an evanescent field at its surface. Molecules of receptor protein are tagged with a tag belonging to that class of chemicals which alters a characteristic of light, when said light passes through said chemical tag. Apparatus utilizes a rapid means of monitoring the change in optical signal coming from the waveguide as binding proceeds between tagged receptor protein and the binding molecular feature of the waveguide. This allows direct measurement of binding and dissociation rates between the receptor and the binding feature of the waveguide. By using a waveguide having a feature resembling a ligand for the receptor, the potential hormonal activity of a test substance may be evaluated from its ability to compete with the waveguide for binding with the receptor. The effect of a test compound on binding of receptor protein to a subsequent element in a hormonal signal transduction mechanism is evaluated by measuring the impact of the test compound on binding between receptor protein and a feature resembling said next element of the signal transduction mechanism. Methods are provided whereby such data may be used to compute affinity constants, binding activity, complex affinity constants resulting from cooperativity, and kinetic parameters for the receptor and test ligand and for the receptor and the next element of the signal transduction mechanism. Preferred embodiments of the invention illustrate application of the method and apparatus to measuring binding between biological receptors and their nuclear response elements, and the use of this type of measurement for assessment of the activity of estrogen mimics present in a test sample, and for evaluation of pharmaceuticals intended to treat hormone dependent cancers.

A construction method of an estrogen activity prediction model, a screening method of estrogen activity, an electronic device and a computer readable storage medium. the construction method of the estrogen activity prediction model comprises: obtaining known chemical data with estrogen activity, the chemical data comprising initial three-dimensional structure information of chemicals; optimizing the initial three-dimensional structure information to obtain optimized three-dimensional structure information; based on the optimized three-dimensional structure information, obtaining a molecular surface point cloud matrix of the chemical; and taking the molecular surface point cloud matrix as an input training convolutional neural network model to obtain the estrogen activity prediction model. According to the deep artificial neural network model constructed by the invention, quantifiable structure parameters which are artificially defined do not need to be used as molecular descriptors, so that the time and computing resources of molecular descriptor calculation and descriptor selection are saved, and the requirement on computational chemistry basis is lower during application.

The invention discloses a method for increasing the weight of silk gland of bombyx mori. According to the sequence pQLTFTSGWGa, bombyx mori adipokinetic hormone A polypeptide synthesis is carried out from a C terminal (carboxyl terminal) to an N terminal (amino terminal); the activity of synthesized bombyx mori adipokinetic hormone A polypeptides is detected by adopting a luciferase reporter gene method; a bombyx mori adipokinetic hormone A active polypeptide solution is degermed by a filtering membrane, and injected into the abdomen of the 5-day bombyx mori in the second day to the third day, the bombyx mori is raised with mulberry leaves to be mature, so that the weight of the silk gland is increased. The method achieves the increase of the weight of the silk gland of the bombyx mori by regulating the distribution of bombyx mori energy by newly discovered active polypeptides without increasing the mulberry leaf eating quantity of the bombyx mori, which has a positive effect on the study of the energy distribution mechanism of the bombyx mori, further improvement of economic characters of the bombyx mori and the like.

The invention relates to pegylated long-acting growth hormone as well as a preparation method and medical application thereof. The PEG-rhGH molecule modified by the branched PEG provided by the invention is modified by a single site, the intermolecular consistency is good, the modification and purification processes are more controllable, and the yield of a modifier is higher; on the basis of retaining the activity of the growth hormone to a greater extent, the pharmacokinetic property of the growth hormone is well improved, and an unexpected technical effect is achieved.

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

The invention discloses a method for increasing the weight of silkworm eggs. The method for increasing the weight of the silkworm eggs comprises the following steps: according to the sequence pQLTFTSGWGa, synthesizing silkworm adipokinetic hormone A polypeptide from a C-terminal (carboxy terminal) to an N-terminal (amino terminal); detecting the activity of the synthesized silkworm adipokinetic hormone A polypeptide by a luciferase reporter gene method; and degerming a silkworm adipokinetic hormone A active polypeptide solution by a filtering membrane, injecting the abdomens of female silkwormchrysalises 2-3 days after pupating with the silkworm adipokinetic hormone A active polypeptide solution, and allowing normal copulation after eclosion to produce silkworm eggs with increased weight.The method disclosed by the invention improves the weight of the silkworm eggs by adjusting energy distribution of silkworms by the newly discovered active polypeptide, and has a positive effect on studying the energy distribution mechanism of the silkworms, further improving the quality of the silkworm eggs, and the like.

The invention discloses 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone of dye lignin derivative, a preparation method and an application of the 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone. The 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone obtained by chemically modifying the dye lignin derivative has the acetylcholinesterase inhibition activity, the estrogen activity and the nerve cell protective action; and the 4', 5-dyhydroxyl-7-(4-(N, N-diethylamino group) butoxy) isoflavone which is taken as a multi-function target spot can be used for preparing the alzheimer disease-resistant medicament.

The invention discloses a method for increasing silkworm cocoon shell weight. The method includes: synthesizing silkworm adipokinetic hormone A polypeptide from terminal C (carboxyl terminal) to terminal N (amino terminal) according to a sequence pQLTFTSGWGa; adopting a luciferase reporter gene method to detect activity of the synthesized silkworm adipokinetic hormone A polypeptide; allowing silkworm adipokinetic hormone A active polypeptide liquid to pass a filtering membrane for degerming, injecting into stomachs of silkworms, and using mulberry leaves to fed till being mature and cocooning,wherein the silkworm cocoon shell weight is increased. The method can increase the silkworm cocoon shell weight without increasing mulberry leaf intake of the silkworms and is realized by regulatingsilkworm energy distribution through newly found active polypeptide, and the method can play a positive role in studying energy distribution mechanism of the silkworms and further increasing silk yield of the silkworms.

The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-I activity according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereo chemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, whereinthe variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and / or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.

The invention discloses a method for increasing silkworm cocoon shell weight. The method includes: synthesizing silkworm adipokinetic hormone A polypeptide from terminal C (carboxyl terminal) to terminal N (amino terminal) according to a sequence pQLTFTSGWGa; adopting a luciferase reporter gene method to detect activity of the synthesized silkworm adipokinetic hormone A polypeptide; allowing silkworm adipokinetic hormone A active polypeptide liquid to pass a filtering membrane for degerming, injecting into stomachs of silkworms, and using mulberry leaves to fed till being mature and cocooning,wherein the silkworm cocoon shell weight is increased. The method can increase the silkworm cocoon shell weight without increasing mulberry leaf intake of the silkworms and is realized by regulatingsilkworm energy distribution through newly found active polypeptide, and the method can play a positive role in studying energy distribution mechanism of the silkworms and further increasing silk yield of the silkworms.

A bifunctional hormone exhibiting an alpha-MSH activity and a natriuretic peptide activity is described. The bifunctional hormone comprises for example a first domain having alpha-MSH related hormonal activity covalently linked to a second domain having natriuretic peptide related hormonal activity. The bifunctional hormone of the present invention is useful for example for the prevention and / or treatment of renal related diseases or conditions, such as acute renal failure (ARF) or acute kidney injury (AKI).

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

Provided are peptides having melanocyte stimulating hormone activity. Also provided are vectors encoding these peptides and transgenic cells comprising the above vectors. Additionally, methods of reducing or preventing release of an inflammatory cytokine from mammalian cells are provided, as are methods for treating a mammal suffering from, or at risk for, a condition mediated by an inflammatory cytokine cascade. Further provided are methods of reducing levels of an inflammatory cytokine in a mammal, methods of treating an overweight mammal, methods of decreasing food intake in a mammal and methods of inhibiting innate immunity in the digestive system of a mammal.