37 results about "Hormone activity" patented technology

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 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.

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.