14 results about "Matriptase" patented technology

Among the various aspects of the present disclosure are compounds that are useful for inhibiting one or more proteases including various serine proteases such as Hepatocyte Growth Factor Activator (HGFA), and the type II transmembrane serine proteases (TTSPs) including matriptase, hepsin, and TMPRSS2. The present invention also relates to various methods of using the inhibitor compounds to treat and / or prevent infections and their symptoms / complications, including those caused by coronaviruses and influenza viruses, conditions associated with inflammation, various other malignancies, pre-malignant conditions, and / or cancer.

To provide methods of identifying new substrates for proteases and methods of using these substrates in a variety of therapeutic, diagnostic and prophylactic indications.SOLUTION: The invention relates generally to: polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator (uPA); activatable antibodies and other large molecules that include the cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator; and methods of making these polypeptides that include the cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator, and methods of use in a variety of therapeutic, diagnostic and prophylactic indications.SELECTED DRAWING: Figure 4A

The present disclosure generally relates to a matriptase-cleavable substrate comprising the amino acid sequence: X1X2X3X4X5X6 (SEQ ID NO:1), wherein X1 and X2 are independently selected from any amino acid residue; X3 is R or K; X4 is selected from R, S, or G; X5 is R or K; and X6 is selected from S, R, or K.

The present invention relates to matriptase antibodies and immunoconjugates of matriptase antibodies with cytotoxic agents and the use thereof for killing or inhibiting the growth of matriptase-expressing cancer cells, such as those of multiple myeloma and breast cancers. In particular, immunoconjugates comprising a matriptase monoclonal antibody and anticancer agents such as auristatin, including monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF) are introduced, which have potent antitumor activity in vivo. Moreover, importantly; there was no weight loss or other evidence of toxicity in the animals, indicating that no significant free drug was released into the circulation from the conjugate. The present invention also provides compositions comprising these new immunoconjugates and use of them for treatment of malignancies comprising cells that express matriptase. In addition, administration of a matriptase antibody or immunoconjugates of a matriptase antibody and a cytotoxic agent in combination with administration of an immunomodulatory agent, such as thalidomide or an analog thereof, provides a more effective treatment of these cancers.

To provide an agent for reducing iron overload in patients having conditions such as beta-thalassaemia and myelodysplastic syndrome (MDS).SOLUTION: Antibodies to enzyme matriptase-2 (MTP-2) are presented. Inhibiting MTP-2 reduces uptake of dietary iron and reduces release of iron from cellular stores in the body. Inhibitors of MTP-2 (such as antibodies to a serine protease domain) can be used to treat iron overload, which is a feature of diseases such as beta-thalassaemia and which otherwise leads to toxic accumulation of iron. Combination of an MTP-2 inhibitor with an activin receptor ligand trap, or with erythropoeitin, provides additional therapeutic effects.SELECTED DRAWING: Figure 1

The present invention relates to a matriptase-2 (MT2) inhibitor, a TMPRSS6 inhibitor, a ferroportin blocker, or a hepcidin enhancer. In particular, the present invention relates to the use of compounds capable of reducing at least one of the following: systemic iron levels, transferrin saturation (Tsat), non-transferrin-bound iron (NTBI), and unstable plasma iron (LPI). This may occur by inhibiting the expression of a target gene, where the target gene may be a transmembrane protease, serine 6 (TMPRSS6). Furthermore, the present invention relates to compositions comprising the above compounds, and methods of using such compounds and / or compositions. Such use may include therapeutic use, for example, to reduce iron overload and prevent iron-related toxicity, before, during, or after chemotherapy pretreatment, stem cell transplantation, and engraftment.

Antibodies to the enzyme matriptase-2 (MTP-2) are presented. Inhibiting MTP-2 reduces uptake of dietary iron and reduces the release of iron from cellular stores in the body. Inhibitors of MTP-2 (such as antibodies to the serine protease domain) can be used to treat iron overload, which is a feature of diseases such as beta-thalassaemia and which otherwise leads to toxic accumulation of iron. Combination of an MTP-2 inhibitor with an activin receptor ligand trap, or with erythropoietin, provides additional therapeutic effects.

Provided is a method of treating or alleviating one or more pathologies associated with β- thalassemia in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of an anti-matriptase-2 antibody or antigen-binding fragment thereof. The one or more pathologies may be insoluble liver iron stores: α-globin precipitates in ery throid cells; reactive oxidized species formation; apoptosis of erythroid cells; reticulocytosis; or a combination thereof.

The present invention generally relates to compounds that are useful for inhibiting one or more trypsin-like S1 serine proteases, HGFA, matriptase, hepsin, KLK5 and / or TMPRSS2 as well as cysteine proteases including trypsin-like cysteine proteases (e.g. Cathepsin B). The present invention also relates to various methods of using the inhibitor compounds to treat or prevent viral infections, including those caused by coronaviruses and influenza, conditions associated with KLK5, various malignancies, pre-malignant conditions, and cancer.

A kind of metal matrix protease responsive polyphenol functionalized hydrogel and preparation method thereof.The present application belongs to the technical field of medicine, discloses a kind of metal matrix protease (MMPs) responsive polyphenol functionalized hydrogel and preparation method and application thereof.The present application prepares polyphenol functionalized hydrogel by film dispersion method.The method preparation process is simple, low in cost, good in stability, high in repeatability.TM / PT / Cel-Cu can solve the problems of poor water solubility and low bioavailability of Cel-Cu on one hand;On the other hand, by adding tea polyphenols, the stability and viscosity of the hydrogel are enhanced.The hydrogel preparation process is simple, fast, easy to scale up and industrialized production, and has good development prospect in clinical application transformation.

The invention belongs to the technical field of biological medicine, and particularly discloses a sponge patch as well as a preparation method and application thereof. The platelet vesicles are combined with absorbable gelatin, collagen or collagen peptide sponge, and the formation of keratin and the activation of inflammatory cells are promoted by virtue of a thrombin cascade effect after platelet activation and a neutrophil anti-inflammatory axis effect, so that conditions are provided for cell proliferation and migration, fibroblast proliferation and matrix deposition processes in the middle and later periods of healing; according to the present invention, with the application of the compound, the intercellular messenger effect is performed, the intercellular regulation is amplified, the functional proteins (CD47, CD55 and GPVI) on the platelets are retained, and the blood coagulation cascade reaction and the endothelial tissue repair are promoted; besides, the absorbable gelatin sponge is of a compact porous structure, is rich in a large amount of collagen, can neutralize excessive matrix protease on damaged wounds as a natural extracellular matrix, has an RGD amino acid sequence, and can promote cell adhesion, reduce inflammatory response, up-regulate growth factor level and accelerate wound healing.

The present invention relates to a Matriptase-2 (MT2) inhibitor, a TMPRSS6 inhibitor, an iron transporter blocking agent, or a hepcidin enhancer. In particular, the present invention relates to the use of compounds capable of reducing at least one of systemic iron levels, transferrin saturation (Tsat), non-transferrin binding iron (NTBI), and labile plasma iron (LPI). This can be accomplished by inhibiting the expression of a target gene, wherein the target gene can be transmembrane protease serine 6 (TMPRSS6). Further, the invention relates to compositions comprising said compounds and to methods of using such compounds and / or compositions. Uses may include therapeutic uses, such as for reducing iron overload and preventing iron-related toxicity before, during or after chemotherapy pretreatment, stem cell transplantation and colonization.

To provide a method for identifying a new substrate for a protease, and a method for using the substrate in various therapeutic, diagnostic and preventive applications.SOLUTION: The present invention relates generally to polypeptides comprising a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator (uPA), activatable antibodies and other large molecules comprising a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator, and methods of making and using these polypeptides comprising a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator in a variety of therapeutic, diagnostic, and prophylactic indications.SELECTED DRAWING: Figure 4A