45 results about "Cathepsin L" patented technology

The present invention relates to novel α-keto carbonyl calpain inhibitors for the treatment of neurodegenerative diseases and neuromuscular diseases including Duchenne Muscular Dystrophy, Becker Muscular Dystrophy and other muscular dystrophies. Disuse atrophy and general muscle wasting can also be treated. Diseases of the eye, in particular cataract, can be treated as well. Generally all conditions where elevated levels of calpains are involved can be treated. The compounds of the invention may also inhibit other thiol proteases such as cathepsin B, cathepsin H, cathepsin L, papain or the like. Multicatalytic Protease (MCP) also known as proteasome may also be inhibited and the compounds can therefore be used to treat cell proliferative diseases such as cancer, psoriasis, and restenosis. The compounds of the present invention are also inhibitors of cell damage by oxidative stress through free radicals and can be used to treat mitochondrial disorders and neurodegenerative diseases, where elevated levels of oxidative stress are involved.

The instant invention is drawn to methods useful for the treatment or the prevention of a viral infection. The methods include administering at least one compound that is an inhibitor of cathepsin L to an individual. The methods are particularly useful in individuals infected with, or at risk of infection with, SARS virus or Ebola virus. The invention also includes methods of identifying potential therapeutics for use in the methods of treatment or prevention of a viral infection.

Compositions which specifically block cathepsin L function in podocytes, compositions which protect cytoskeletal adaptor protein (CD2AP) for degradation, compositions which modulate expression or function of cytoskeletal adaptor protein (CD2AP), protect against renal diseases or disorders. Methods of treatment in vivo involve use of one or more compositions.

The present invention relates to a method for treating tissue damage caused by ischemia in a patient which comprises administering to said patient a therapeutically effective amount of a compound which is an inhibitor of cathepsin B or cathepsin L, but which is not as an effective inhibitor of calpain relative to cathepsin B or cathepsin L or both and which compound is a peptidyl diazomethyl ketone.

The present invention provides means for identifying or classifying breast tumors based on the levels of nuclear cathepsin-L (CTSL) and nuclear p53 binding protein (53BP1), and methods of treating thereof.

The present invention relates to the field of biomarkers and, more specifically, to biomarkers useful in diagnosing aggressive prostate cancer. In specific embodiments, a method for diagnosing aggressive prostate cancer in a patient comprises (a) measuring the levels of one or more biomarkers in a sample collected from the patient; and (b) comparing the levels of the one or more biomarkers with predefined levels of the same biomarkers that correlate to a patient having aggressive prostate cancer and predefined levels of the same biomarkers that correlate to a patient not having aggressive prostate cancer, wherein a correlation to one of the predefined levels provides the diagnosis. In a specific embodiment, the one or more biomarkers may comprise cathepsin-L (CTSL), periostin, microfibrillar-associated protein 4 (MFAP4), collagen XII, neprilysin, clusterin, neutrophil gelatinase associated lipocalin (NGAL), epithelial cell activating molecule (EpCAM), prostate specific antigen (PSA), membrane metallo-endopeptidase (MME) and asporin (ASPN).

Methods and agents useful for modulating histone proteolysis, stem cell differentiation, and gene transcription and for treating cancer are disclosed. Antibodies or antigen binding fragments that selectively bind to histone-3 cleavage products and are useful for diagnosing cancer and monitoring a subject's response to cancer treatment are also disclosed.

This invention relates generally to the treatment of cathepsin or dynamin mediated diseases, such as proteinuria, cancer, and cognitive disease and related products. Diagnostic and other assays are also provided, as well as methods for podocyte cell gene transfer.

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful.

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful.

The invention relates to the field of medicinal chemistry, particularly to a cathepsin inhibitor, a preparation method and applications thereof, more particularly to a tumor-associated cathepsin L inhibitor and a tumor-associated cathepsin D inhibitor, and a preparation method of the tumor-associated cathepsin L inhibitor and the tumor-associated cathepsin D inhibitor. Specifically the present invention further relates to a novel peptoid compound or a pharmaceutically acceptable salt thereof, a solvate, a pharmaceutical composition and a pharmaceutical preparation, a preparation method of thecompound, and applications of the peptoid compound or the pharmaceutically acceptable salt thereof, the solvate, the pharmaceutical composition and the pharmaceutical preparation in preparation of antitumor drugs, wherein the structure formula of the compound is defined in the specification, and R1, R2 are defined in the claims and the specification. The formula (I) is defined in the specification.

The disclosure provides methods and compositions useful for inhibiting virus requiring membrane fusion for viral entry, specifically for inhibiting severe acute respiratory syndrome coronavirus (SARS-CoV), Ebola virus (EBOV), Hendra (HeV) and Nipah (NIV) viruses by targeting Cathepsin-L (CatL) cleavages sites in the viruses' glycoproteins.

Biaryl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

The invention discloses a soybean protein hydrolyzate, a preparation method and applications thereof. The preparation method comprises: adding cathepsin L to soybean protein, adjusting the pH value to 5.5-8.5, stirring for 20-60 min at a room temperature, and carrying out a reaction for 2-24 h under a water bath condition of 35-42 DEG C so as to obtain the soybean protein hydrolyzate. According to the present invention, the soybean protein cathepsin L hydrolyzate can effectively improve the expression amounts of COL1A1 gene, COL1A2 gene and KPRP gene, can effectively increase the collagen I content in skin while enhance the protective function of skin, and can finally achieve effects of skin aging alleviating, skin protection improving and correspondingly improved skin moisturizing so as to achieve the purpose of skin care; with the estrogen-like effect of the soybeans, a lot of effects can be provided for the maintaining of the health of the skin; through the synergetic effect of a variety of factors and other unknown mechanisms, the soybean protein hydrolyzate of the present invention can effectively maintain the skin, and can alleviate the symptoms of various skin diseases.

The invention discloses a novel application of compound solidago decurrens spray extract dry powder in pharmacy, and finds that when the concentration of the compound solidago decurrens spray extract dry powder is 1mg / mL, the inhibition rate of the compound solidago decurrens spray extract dry powder on a new coronavirus drug target Cathepsin L protease reaches 55.6%; when inhibition rate IC50 of the compound on HIV protease is 0.38 mg / mL, and the compound can be independently used or compounded with other drugs to be used for drugs for preventing and treating novel coronavirus pneumonia and antiviral drugs.

The invention discloses application of ganodermanondiol using endonuclear cathepsin L as a target spot in pharmacy. Through in-vitro cancer cell proliferation resistance experiments and cell death andcell cycle experiments of the ganodermanondiol, it is proven that the ganodermanondiol reduces a truncated CUX1 factor (active form) by inhibiting the colorectal cancer endonuclear CL activity, thenexpression of Cyclin E2 is reduced, finally, colorectal cancer cells stay in an S phase of the cell cycle, and thus the effect of inhibiting cancer cell growth is achieved. Therefore, the ganodermanondiol can be used for preventing or curing colorectal cancer-related diseases including rectal cancer, colon cancer and related diseases, caused by rectal cancer or colon cancer, of constipation, hematochezia, abdominal pain, abdominal cramps, intestinal cancer cell infiltration and migration, and the like, and thus the ganodermanondiol is suitable for being popularized and applied.

The invention relates to a method for extracting myosin of noto-pleural muscles of freshwater fish, which belongs to the technical field of aquatic products. The method comprises the following steps: firstly, putting live fish into a pass box filled with fresh water and standing for 1-2 hours; rapidly taking the noto-pleural muscles of the live fish; washing fish dices by ice water; rinsing by a buffering solution; and finally, preparing a myosin solution. According to the method, the influences of cathepsin L are eliminated when the myosin of the noto-pleural muscles of aquaculture fish so as to obtain the high-purity myosin of fish.

Human cathepsin L inhibitors and probes containing a vinyl sulfonate ester moiety are described. The inhibitors are highly potent (low nM affinity), selective, and cell permeable, and can inhibit ultra-low concentration of active cathepsin L. The developed probes are highly sensitive and can detect an ultra-low amount of probe-labeled active cathespin L.

The invention provides a preparation method and application of high-gel-strength minced meat products of aquatic products. According to the invention, in the preparation of minced fish or minced shrimp gel products, by a specific high-pressure CO2 non-thermal processing treatment method, cathepsin L which causes degradation of minced fish gel can be effectively passivated so as to improve gel strength of the minced fish or minced shrimp products and improve storage stability of the products; moreover, the process adopted by the invention is simple, energy-saving and environmental-friendly, andthe high-gel-strength minced fish or minced shrimp products can be produced; and special flavors and nutritional ingredients of the minced meat products can be kept.

The present invention discloses a new application of compound solidarum spray extract dry powder in pharmacy. The present invention finds that compound solidarum spray extract dry powder at 1 mg / mL can inhibit the new coronavirus drug target Cathepsin L protease by 55.6%. ; the inhibition rate of HIV protease is IC 50 =0.38mg / mL can be used alone or in combination with other drugs for the prevention and treatment of new coronavirus pneumonia drugs and antiviral drugs.

This present disclosure is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin L, cathepsin K, and / or cathepsin B, will be therapeutically useful. Formula I: or a solvate or pharmaceutically acceptable salt thereof. Each of R1-R10 are independently selected from the group consisting of: hydrogen, alkoxy, halo, hydroxy, phosphate, phosphate salts, disodium phosphate, diphosphate dimer, diphosphate dimer salt, and sodium diphosphate dimer with at least one of R1-R10 is a phosphate or diphosphate dimer group.

The invention relates to a hydrazinonitrile cathepsin K inhibitor, and an application thereof in preparation of osteoarthritis treatment drugs, and belongs to the technical field of cathepsin inhibitors. The inhibitor contains a novel P3 group with different orientations, has a nano-mole concentration level inhibition effect on cathepsin K outside cells, has hundreds-of-times or above selectivity to cathepsin K, cathepsin S and cathepsin B, and also has hundreds-of-times or above selectivity to highly homologous cathepsin K and cathepsin L. Culture is carried out under the following two conditions: (1) cell passage and (2) ascorbic acid and beta-glycerophosphoric acid stimulation with primary chondrocytes as a model. Results of gelatin zymography and quantitative fluorescence assay tests show that the expression level of the cathepsin K under every one of the above two conditions is increased; and the activity of the cathepsin K is reduced after the novel inhibitor is added. The inhibitor also has a good inhibition effect in the cells, and has a very good inhibition effect on the cathepsin K.

The invention relates to a protein marker for sicca syndrome in saliva and application of the protein marker. Particularly, the invention relates to application of a protein identification reagent inpreparation of a reagent for diagnosing the sicca syndrome in a subject. Protin is selected from a combination of acylamino acid release enzyme, 1,4-glucose formyl transfer enzyme, Calumenin, C-C motif chemotatic factor ligand 28, activation-induced cytidine deaminase, alpha collagen 1 chain, carboxypeptidase D, carboxypeptidase E, cysteine proteinase inhibitor C, cathepsin L, DnaJ heat shock protein family (Hsp40) member C3, furan paired basic amino acid lyase, HtrA serine peptidase 1, kallikrein correlated peptidase 11, trypsin 3, proteasome subunit-4, proteasome subunit 9, antichymotrypsinand vimentin.

The invention relates to a method for extracting freshwater fish dorsal muscle myosin, which belongs to the technical field of aquatic products. The steps of the method of the present invention are as follows: first put the live fish into a turnover box equipped with fresh water and let it stand for 1 to 2 hours; quickly take the dorsal muscle of the live fish; rinse the diced fish with ice water; rinse with buffer solution; finally prepare Obtain myosin solution. The present invention obtains higher-purity fish myosin by eliminating the influence of cathepsin L when extracting domestic fish dorsal muscle myosin.

The invention discloses a colloidal gold test strip for detecting a lamb fasciola hepatica infection circulating antigen, and the prepared lamb fasciola hepatica infection colloidal gold test strip can be used for detecting the lamb fasciola hepatica infection circulating antigen and has the advantages of simplicity in operation, rapidness in detection, convenience in carrying and the like in the aspect of use. The detection result is visual, easy to understand and convenient to interpret, and the kit can be used for detecting early infection of fasciola hepatica, can distinguish current infection from previous infection, and is suitable for on-site detection of clinical samples. The anti-fasciola hepatica cathepsin L monoclonal antibody ensures the specificity of the detection method. The rabbit anti-fasciola hepatica cathepsin L polyclonal antibody improves the sensitivity of the detection method.

Human cathepsin L inhibitors and probes containing a vinyl sulfonate ester moiety are described. The inhibitors are highly potent (low nM affinity), selective, and cell permeable, and can inhibit ultra-low concentration of active cathepsin L. The developed probes are highly sensitive and can detect an ultra-low amount of probe-labeled active cathespin L.

The invention relates to a protein marker for sicca syndrome in saliva and application of the protein marker. Particularly, the invention relates to application of a protein identification reagent inpreparation of a reagent for diagnosing the sicca syndrome in a subject. Protin is selected from a combination of acylamino acid release enzyme, 1,4-glucose formyl transfer enzyme, Calumenin, C-C motif chemotatic factor ligand 28, activation-induced cytidine deaminase, alpha collagen 1 chain, carboxypeptidase D, carboxypeptidase E, cysteine proteinase inhibitor C, cathepsin L, DnaJ heat shock protein family (Hsp40) member C3, furan paired basic amino acid lyase, HtrA serine peptidase 1, kallikrein correlated peptidase 11, trypsin 3, proteasome subunit-4, proteasome subunit 9, antichymotrypsinand vimentin.

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and / or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma.