35 results about "TGF beta receptors" patented technology

This invention relates to compounds, compositions, and methods useful for modulating TGF-beta and/or TGF-betaR gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of TGF-beta and/or TGF-betaR gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of TGF-beta and/or TGF-betaR genes. Such small nucleic acid molecules are useful, for example, for treating, preventing, inhibiting, or reducing inflammatory, respiratory, autoimmune, and/or proliferative diseases, disorders, conditions, or traits in a cell, subject or organism and any other disease, condition, trait or indication that can respond to the level of TGF-beta and/or TGF-betaR in a cell or tissue; or alternately in providing long term hematopeitic reconstitution in a subject or organism.

Restenosis is inhibited through local delivery of anti-restenotic agents including angiotensin converting enzyme inhibitors; nicotine receptor agonists, agents that increase concentrations of nitric oxide, anti-angiogenic agents, agonists of the TGF-beta receptor; death domain receptor ligands; and thrombin inhibitors. In one embodiment of the invention, the localized delivery is effected through the use of a stent modified for delivery of the agent at the site of injury from balloon angioplasty.

Anti-cancer agents and/or transforming growth factor beta (TGF-beta or TGFβ) antagonists are disclosed, where the agents and/or antagonists include a therapeutically effective amount of a combination of therapeutically active portions of sRII and therapeutically active portions of sRIII or a fusion polypeptide or protein comprising therapeutically active portions of sRII and therapeutically active portions of sRIII. Methods for preventing, treating and/or ameliorating the symptoms of cancer are also disclosed based on administering an effective amount of a composition of this invention.

Novel hetarylaminoquinoline derivatives of formula (I)

wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

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 an immune effector cell expressing a chimeric protein and an application thereof, in particular to the immune effector cell of the chimeric protein expressing an extracellular domain containing a TGF-beta receptor and an intracellular signal domain of IL-2 family protein, a pharmaceutical composition comprising the same, and the application of the immunological effector cell or a pharmaceutical composition as described above for preparing a drug for preventing or treating a tumor or pathogenic microorganism infection. The immune effector cell expressing the chimeric protein is capable of transforming the stimulation of TGF-beta into a positive signal of IL-2, IL-7 or IL-21, inhibiting TGF-beta-induced Treg differentiation, and promoting the proliferation and survival of immune cells; also reduces the effect of TGF-beta on cell killing ability, and shows a better anti-tumor ability.

The invention provides a culture system for preparing an endoderm cell line and a method for preparing the endoderm cell line by the culture system. The culture system comprises a composition of a TGF-beta receptor antagonist, an RA receptor activator and a cAMP (cyclic adenosine monophosphate) activating agent, wherein the composition is free from exogenous transcription factors. By the aid of the culture system and the culture method, reprogramming for changing cell fate can be induced, and body cells are reprogrammed into the endoderm cell line.

The invention relates to application of STAT1 serving as ovarian cancer treatment target point. Experiments prove that the STAT1 directly combines with a TGF-beta receptor (ALK1, ALK5 and TbetaRII), proliferation, migration and invasion of ovarian cancer cells can be promoted after STAT1overexpression, and proliferation, migration and invasion of the ovarian cancer cells can be inhibited after STAT1 knocking-down. Therefore, STAT1 reduction processing is conducted on patients with high ovarian cancer STAT1 expressions, a potential treatment effect exists. An STAT1 signal path mutually acts with a TGF-beta1 signal path to influence the proliferation, migration and invasion capability of ovarian cancers. The STAT1 is a potential novel ovarian cancer treatment target point and has a great clinical application value.

The invention relates to novel 5-cyano-thienopyridines of the formula (I) where R1, R2, and R3 have the meanings designated in Claim 1. Said 5-cyano-thienopyridines are inhibitors of TGF-beta receptor kinase and may be used, among other things, for the treatment of tumors.

The invention discloses a product for inhibiting and/or preventing influenza virus secondary bacterial infection. The invention provides an application of a TGF-beta signaling pathway inhibitor, namely an application of a TGF-beta signaling pathway inhibitor in preparation of a product for inhibiting and/or preventing influenza virus secondary bacterial infection. The TGF-beta signaling pathway inhibitor is at least one of the following inhibitors: an anti-TGF-beta monoclonal antibody, a soluble TGF-beta receptor, a TGF-beta antisense oligonucleotide, an inhibitor for inhibiting TGF-beta expression or inhibiting activity, a small-molecule inhibitor of a TGF-beta receptor and a small-molecule inhibitor of a TGF-beta signaling pathway downstream factor. By research results of a key role of TGF-beta in A-type influenza virus secondary bacterial infection, an impact factor for inhibiting TGF-beta signaling pathway or regulating TGF-beta is brought forward, and the effect of preventing settling and infection of bacteria at respiratory tract due to influenza virus infection is achieved. The product of the invention has the advantage of early-stage, high-efficiency and wide-spectrum blocking of bacterial adhesion.

The invention comprises a fusion protein as sensor for TGF-beta receptor activity, a method for detecting receptor activity and to screening compounds for modulators of receptor activity. The fusion protein comprises a type I TGF-beta receptor, a circularly permutated fluorescent protein moiety (cpFP) and an activation state specific receptor binding domain, binding specifically to either the activated or inactive form of the TGF-beta receptor. An activation specific interaction between the receptor and the activation state specific receptor binding domain modulates the fluorescence of the cpFP inserted in between. Thus, activation of the receptor can be detected directly by a change in fluorescence of the cpFP.

The invention discloses use of corilagin in preparation of anti-myocardial fibrosis medicines, belonging to the technical field of biological medicine. By constructing an in-vivo myocardial fibrosis model induced by a mouse aortic ligation operation and an in-vitro myocardial fibrosis model of transforming growth factor (TGF)-beta-induced rat suckling CFs for performing experimental study, the results show that the corilagin can regulate macrophage polarization so as to inhibit inflammation, also can down-regulate an interleukin-4 (IL-4) receptor so as to avoid excessive production of TGF-beta, and inhibits the expression of a TGF-beta receptor so as to reduce the activation of cardiac fibroblasts, thereby reducing collagen content and relieving myocardial fibrosis. The corilagin providedby the invention can reduce the myocardial fibrosis caused by long-term stress load, protect heart tissues and inhibit or delay deterioration of heart functions; the corilagin has a significant effectin the aspect of anti-myocardial fibrosis, is little in side effects, and can be used for preparing the anti-myocardial fibrosis medicines.

Novel triazole derivatives are inhibitors of TGF-beta receptor I kinase, for the treatment of tumours.

The present invention addresses the problem of providing a novel means whereby cells showing a function more closely similar to the function of intestinal epithelial cells of a living body can be easily and efficiently prepared. According to the present invention, differentiation of pluripotent stem cells into intestinal epithelial cells is induced by: (1) a step for differentiating the pluripotent stem cells into intestinal stem cell-like cells; and (2) a step for differentiating the intestinal stem cell-like cells obtained in step (1) into intestinal epithelial cell-like cells with the combined use of an MEK1 inhibitor, a DNA methylation inhibitor, a TGF Beta receptor inhibitor, EGF and a cAMP activator.

The invention discloses a small-molecular compound combination and a method for inducing differentiated cells to prepare osteoblasts by using the small-molecular compound combination. The small-molecular compound combination includes a first-stage small-molecular compound and a second-stage small-molecular compound used in a staged manner according to time sequence, wherein the first-stage small-molecular compound includes TGF-beta receptor inhibitors, WNT/beta-catenin agonists and cAMP agonists; the second-stage small-molecular compound includes lysine deacetylases inhibitors, TGF-beta receptor inhibitors, PKC inhibitors, WNT/beta-catenin agonists and cAMP agonists. Through phased induction of the small-molecular compounds, the differentiated cells can be differentiated into the osteoblasts, precision quality control can be achieved in each step, and standardization operation and large-scale production are facilitated. The method provided by the invention has wide donor sources, a patient himself can be used as a donor, and the osteoblasts needed for basic research, clinical treatment, or tissue engineering production can be obtained in a relatively short period of time.

The invention relates to the technical field of skin anti-aging nursing articles, in particular to an essence for promoting subcutaneous fat regeneration and a preparation process thereof. The essencecomprises the following components in percentage by mass: 0.01-1.00 percent of SIS3, 0.01-1.00 percent of SB431542, 0.05-1.5 percent of sodium hyaluronate, 0.5 percent of pyrrolidone carboxylate acidsalt, 0.01-1 percent of olive oil,1-5 percent of glycerol, 0.05-2.00 percent of Sepigel305 and the balance of deionized water, wherein the sum of components is 100 percent; SIS3 is a novel specific Smad3 inhibitor, which can inhibit phosphorylation suppression TGF-beta and activin signals of Smad3, SB-431542is a transforming growth factor beta receptor (TGF-beta receptor) inhibitor, SIS3 and SB 431542 are all fat-soluble, molecular weights are all less than 800 and can easily penetrate through skin cuticle to enter a basal layer and a dermis layer of skin. The essence is convenient to use, the use effect is good, and the anti-aging ability of skin is greatly improced.

The invention relates to a TGF-Beta receptor II isoform, fusion peptide, methods of treatment and methods in vitro. ATGF-p receptor II isoform, fusion peptide, methods of treatment and methods in vitro An isoform of the TGF beta receptor II comprising a sequence of about of 80 amino acids and lacking a transmembrane domain. A fusion peptide is provided comprising an isoform of the TGF beta II receptor fused to a ligand, wherein a vector comprising the fusion peptide is used to treat cancer and/or hepatic fibrosis. A method of treating hepatic fibrosis or cancer diseases, comprising the step ofadministering to a mammal in need thereof a vector bearing a polynucleotide sequence set forth in SEQ ID No.2. A fusion peptide is provided comprising an isoform of the TGF beta II receptor fused toa ligand, wherein a vector comprising the fusion peptide is used to treat cancer and/or hepatic fibrosis. An antibody binding the soluble isoform of the TGF beta II receptor is provided. The antibodybinds the amino acid sequence shown in SEQ ID No. 12 and is used in in vitro methods.

The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

Novel thienopyrimidines of formula (I), in which R1, R2, and X have the meanings indicated in claim 1, are TGF-beta receptor kinase inhibitors and can be used for the treatment of tumors, among other things.