31 results about "Antiapoptotic protein" patented technology

Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided:wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

A spontaneous transferring cell strain SPC-A-1BM is taken as human-lung adenocarcinoma SPC-A-1 cell strain. It has high spontaneous transferring rate and missed rate, lung transferring rate reaches to 80%, nodus lymphoideus transferring rate reaches to 85% and bone transferring rate reaches to 25%. It has excellent DNA cell stability and can be used to make research for human-lung adenocarcinoma transferring mechanism.

The invention discloses application of human amniotic mesenchymal stem cells in preparation of a preparation for treating a myocardial ischemia reperfusion injury generated after cardiopulmonary bypass.In the myocardial ischemia reperfusion process after the cardiopulmonary bypass, the human amniotic mesenchymal stem cells can effectively prevent myocardial cells from being injured in myocardial ischemia reperfusion, obviously improve the cardiac functions, lower the levels of myocardial injury specific marker protein lactic dehydrogenase, creatine kinase isoenzyme and troponin I, lower the levels of a plasma inflammatory factor interleukin-8 and a tumor mecrosis factor-alpha, increase the content of the plasma inflammatory factor interleukin-10, obviously improve pathological changes of the myocardial tissue, reduce myocardial cell apoptosis, lower the expression level of cell apoptosis promoting protein, increase the expression quantity of anti-apoptoasis protein and can protect the functions of myocardial cell mitochondria.By preparing the human amniotic mesenchymal stem cells into an injection for treatment on the myocardial ischemia reperfusion injury generated after the cardiopulmonary bypass, the cardiac functions can be effectively protected, and postoperative complications of the cardiopulmonary bypass are relieved.

The invention belongs to the field of biological technology, and in particular relates to a method for regulating the expression, quantity and activity of heat shock protein 70 and its application. Utilizing the present invention can also regulate tumor tissue and intracellular transcription factor NF-κB and its activity, death receptor DR4 and DR5 expression and activity, JNK and c-Jun phosphorylation and activity, p53 protein expression and activity, pro-apoptosis Molecule Bax, Bid, t-Bid, capsase 3, capsase 8, capsase 9 expression and pro-apoptotic activity, anti-apoptotic protein c-FLIP and Bcl-2 expression and activity, promote tumor tissue and cell apoptosis. The present invention also relates to the application of the above-mentioned method in the preparation of medicines used in combination with apoptosis-inducing medicines.

The invention relates to the application of icariin in the preparation of a medicine for preventing and treating Alzheimer's disease. According to the invention, experiments such as a Morris water maze experiment, a Western blot experiment, an HE staining method and the like are carried out in an SAMP8 model mouse; it is proved that learning and memory disorder of SAMP8 mice can be reversed afterintragastric administration of ICA, icariin can down-regulate expression of BACE1 so as to reduce deposition of cytotoxic A beta 1-42. Besides, icariin can improve cognitive defects by increasing theexpression of anti-apoptotic protein Bcl-2, reducing the expression of pro-apoptotic protein Bax and remarkably increasing the ratio of Bcl-2 to Bax, so that neuronal apoptosis is inhibited, and neurons are protected. The invention provides further evidences for the clinical curative effect of icariin on Alzheimer's disease.

The present invention relates to a polypeptide binding with tumor necrosis factor (TNF-alpha), and applications thereof. According to the present invention, the polypeptide and TNF-alpha have high affinity, and the polypeptide can be bound with the excess TNF-alpha to make the apoptosis promoting protein Bid in the apoptosis-related mitochondrion apoptosis pathway be down-regulated while make the anti-apoptosis protein Bcl-2 be up-regulated in the apoptosis-related mitochondrion apoptosis pathway so as to inhibit the apoptosis caused by TNF-alpha, such that the polypeptide can be used for preparation of TNF-alpha-related disease treating drugs. The present invention further provides a method for screening at the molecular and cellular level and researching the influence of the polypeptide antagonist on the TNF-alpha physiological effect, and applications thereof so as to provide the effective method for development of the low-cost anti-TNF-alpha drug.

The invention belongs to the technical field of medicine, and particularly discloses compound stybenpropol a and application thereof in improving atherosclerosis (AS). According to the invention, thenovel compound stybenprop a is extracted from benzoin, and research results show that in human umbilical vein endothelial cells HUVECs) injured by tumor necrosis factor (TNF-alpha), the stybenprop a can inhibit endothelial cell inflammatory damage by inhibiting TNF-alpha-induced NF-kappa b activation and nuclear translocation and enhancing expression of anti-apoptotic protein Bcl-2 so as to increase the level of nitric oxide secretion and reduce the levels of vascular adhesion molecules and pro-inflammatory factors, the compound stybenpropol a can significantly inhibit TNF-alpha-induced inflammatory injury and apoptosis of the HUVECs, provides a new choice and approach for the development of anti-atherosclerosis drugs and has a good application prospect.

In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

The present invention provides methods and combinations of methods for identifying agents that modulate the apoptotic state of a cell by binding to the hydrophobic groove of a Bcl-2 family member anti-apoptotic protein. In certain embodiments, the methods generally comprise the use of Bcl-2 family member proteins having one or more mutations in the hydrophobic groove that, relative to a corresponding protein lacking the mutation, affect, e.g., binding of desired agents or in vitro antimycin sensitivity without substantially altering tertiary protein structure. In these embodiments, the methods comprise the identification of agents that exhibit reduced binding affinities and / or other biological activities for the mutant proteins relative to the corresponding Bcl-2 family member lacking the mutation. In other embodiments, the methods generally comprise the detection of the ability of an agent to induce increased glucose uptake or lactate production in proportion to the level of expression of an anti-apoptotic Bcl-2 family member protein.

The present invention relates to the technical field of medicine, and specifically relates to a PUMA inhibitor, a method for preparation thereof, and a use thereof. The PUMA inhibitor is the compound as shown in (I) or a pharmaceutically acceptable salt thereof. The definitions of its substituent groups are as described in the description. The compound (I) or pharmaceutically acceptable salt thereof is capable of targeting a PUMA protein and has very good physicochemical properties, very good apoptosis resistance and radiation protection effects; it can selectively inhibit the competitive combined effect of a PUMA protein and a Bcl-2 apoptosis-resistant protein, block apoptosis, and effectively protects against bone marrow damage. The present invention provides a new idea for, and powerful proof of, the application of a PUMA-protein small molecule inhibitor in radiation-protection pharmaceuticals, and is likely to become a highly effective, low-toxicity, and stable clinical radiation-protection pharmaceutical.

In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

The invention belongs to the technical field of medicine, and specifically discloses a compound Stybenpropol A and its application in improving atherosclerosis (AS). The present invention extracts a novel compound Stybenpropol A from benzoin, and the research results show that in human umbilical vein endothelial cells (HUVECs) induced by tumor necrosis factor (TNF-α), Stybenpropol A can inhibit TNF-α-induced NF-κB activation and nuclear translocation and enhanced expression of anti-apoptotic protein Bcl-2, thereby inhibiting endothelial cell inflammatory injury, increasing nitric oxide secretion levels, reducing vascular adhesion molecules and pro-inflammatory factor levels, can significantly inhibit TNF- α-induced inflammatory injury and apoptosis of HUVECs provides a new option and approach for the development of anti-atherosclerotic drugs, and has a good application prospect.

The invention belongs to the field of medicinal chemistry and particularly relates to an application of asymmetric curcumine compounds to preparation of anti-gastric-cancer drugs. The compounds can effectively inhibit growth of gastric cancer cells BGC-823, SGC-7901 and MFC, inhibit formation of gastric cancer cell colonies, inhibit NF-kappaB signaling pathways in the gastric cancer cells, down-regulate expression of anti-apoptotic protein Bcl-2, up-regulate expression of apoptin Bax and induce gastric cancer cell apoptosis, wherein the active compound S06 can effectively enhance anti-gastric-cancer activity of irinotecan and can serve as a potential anti-gastric-cancer drug.