21 results about "Cysteine protease" patented technology

The present invention relates to the interaction of the protein HMCN1 (hemicentin 1 or fibulin 6) as a substrate of the protease ADAMTS12 (a disintegrin and metalloproteinase with thrombospondin motif 12 protein) in the pathogenesis of chronic kidney and heart diseases, and in particular chronic renal insufficiency and renal fibrosis, and heart failure and cardiac fibrosis, respectively. The present invention further relates to methods for identifying compounds that bind to and / or inhibit the protease ADAMTS12, as well as pharmaceutical compositions for use in the treatment of kidney diseases, in particular pharmaceutical compositions comprising active substances that inhibit the cleavage and digestion of hemicentin 1 by the metalloprotease ADAMTS12 or the interaction of hemicentin 1 with ADAMTS12.

The present invention provides a probe compound for labeling a cysteine protease based on activity. The compound targets the protease through a specific targeting element. The compound also includes a detectable element, such as a fluorescent label, a radioactive label, or a chelator. In some cases, the compound also includes a quenching element that is released upon reaction with the protease. The present invention also provides compositions comprising the compound, as well as methods of using the compound, such as labeling a protease in an animal and visualizing a tumor in an animal.

The present invention discloses a scomber japonicus dark muscle enzymolysis antibacterial peptide, its preparation method and use. The characteristics are that the amino acid sequence of the antibacterial peptide is Arg-Ser-Cys-His and / or Lys-Ser-Cys-Gly. The steps of its preparation method are as follows: Add deionized water with a mass 2-4 times that of the fish meat to the defatted scomber japonicus dark muscle and adjust the pH to 7-11, then add trypsin and bacillus licheniformis protease for enzymolysis, then incubate to inactivate the enzyme and centrifuge, and take the supernatant to obtain the crude enzymolysis solution; Add C-terminal endo-double enzyme cysteine protease ArgC and serine protease LysC to the crude enzymolysis solution for enzymolysis, incubate to inactivate the enzyme and centrifuge to obtain the upper enzymolysis clear solution, then filter it with an ultrafiltration system to obtain an enzymolysis solution of 1-3 kDa, collect the filtrate and freeze-dry it, and the powder is the scomber japonicus dark muscle enzymolysis antibacterial peptide. The advantages are high extraction efficiency and significant inhibitory effects on both Gram-positive bacteria and Gram-negative bacteria.

This invention discloses the application of a Trichinella spiralis cysteine ​​protease inhibitor in acute myocardial infarction and subsequent ventricular remodeling, belonging to the field of medicinal chemistry. This invention provides a drug that can prevent, alleviate, and / or treat acute myocardial infarction and subsequent ventricular remodeling. The active ingredient of this drug is the Trichinella spiralis cysteine ​​protease inhibitor cystatin, abbreviated as rTs-Cys. rTs-Cys can effectively delay acute myocardial infarction and inflammatory response in mice, reduce the infarct area, improve cardiac function deterioration, and reverse organ pathological damage, providing a new approach for the clinical treatment of acute myocardial infarction and subsequent ventricular remodeling.

A recombinant TEV protease, a preparation method therefor, and use thereof, relating to the technical field of biology. Specifically provided are four recombinant TEV proteases derived from a cysteine protease of tobacco etch virus. In each of the four recombinant TEV proteases, the N-terminus is fused with an 8His-CL7-GGS tag, and the C-terminus is fused with a polyarginine tag. Compared to a wild-type TEV protease, the provided four recombinant TEV proteases not only can overcome defects such as self-cleavage, poor solubility, and low activity during expression and purification of the wild-type TEV protease, but also have improved protein yield 5-6 times higher than that of the wild-type TEV enzyme, and enzyme activity 10-20 times higher than that of the wild-type TEV protease. In addition, the engineered TEV protease mutants also possess higher thermal stability with a Tm value 10-30 °C higher than that of the wild-type TEV protease, exhibit better protein stability, have broader application conditions, and are more suitable for large-scale production and industrial use.

The invention provides application of a small molecule compound in preparation of a product for inhibiting 3C-like cysteine protease, and belongs to the technical field of biological medicine. The small molecule compound is one or more of Gedatolisib, EGFR-IN-8, Akt inhibitor VIII, Bavlogalutamide, lifrafenib, TAM-IN-2, GSK1904529A and IKK 16, and the molecular weight of the small molecule compound is more than or equal to 100,000, the molecular weight of the small molecule compound is more than or equal to 100,000, the molecular weight of the small molecule compound is more than or equal to 100,000, the molecular weight of the small molecule compound is more than or equal to 100,000, and the molecular weight of the small molecule compound is more than or equal to 100,000. The small molecule compound provided by the invention has a remarkable inhibition effect on 3C-like cysteine protease, provides more choices for preparing a 3C-like cysteine protease inhibitor, and also provides a thought for developing antiviral drugs in the future.

The invention relates generally to cleavable polypeptides, method of producing a cleavable moiety (CM) containing polypeptide by culturing a cell under conditions that lead to expression of the polypeptide, methods of manufacturing a cleavable moiety (CM) containing polypeptide by culturing a cell comprising a nucleic acid construct that encodes the cleavable polypeptide to express the cleavable polypeptide, and recovering the cleavable polypeptide, nucleic acids encoding the cleavable polypeptides, and vectors including the nucleic acids encoding the cleavable polypeptides.

The invention discloses a biomimetic catalyst based on an MOF material, a preparation method of the biomimetic catalyst and application of the biomimetic catalyst in peptide synthesis. According to the method, firstly, a novel functional ligand is designed and synthesized, and the ligand integrates nucleophilic sulfydryl, proton transfer imidazolyl and skeleton connection carboxyl and can simulate a'catalytic triad 'of an enzyme active center. Then, the ligand, metal salt and terephthalic acid are co-assembled through a solvothermal method, and the bionic MOF material is prepared. The material has regular nanopore channels and high stability, and can accurately simulate the catalytic mechanism of cysteine protease. The catalyst is used for catalyzing peptide synthesis reaction, amino-acid ester condensation can be efficiently catalyzed to form peptide bonds under the mild and green conditions without chemical coupling agents, the conversion rate is high, the catalyst is easy to recycle, the inherent defects of a traditional chemical synthesis method and an enzyme method are overcome, and a new strategy is provided for green peptide synthesis.

Provided herein are compounds having a structure of formula (I) or formula (II):or a pharmaceutically acceptable salt, solvate, or hydrate thereof, useful in treating or preventing coronavirus infection. In some embodiments, the coronavirus infection is COVID-19 (SARS-COV-19). Also provided are compositions comprising the compounds, as well methods of using the compounds to treat or prevent coronavirus infection.

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.

The present invention relates generally to polypeptides comprising at least a first cleavable moiety (CM1) as a substrate for at least one matrix metalloproteinase (MMP) and at least a second cleavable moiety (CM2) as a substrate for at least one serine protease (SP) or at least one cysteine protease (CP); to activatable antibodies and other larger molecules comprising these polypeptides comprising at least CM1 as a substrate for at least one MMP protease and at least CM2 as a substrate for at least one SP protease or at least one cysteine protease (CP); the present invention relates to polypeptides comprising at least CM1 as a substrate for at least one MMP protease and at least CM2 as a substrate for at least one SP protease or at least one cysteine protease (CP), and to methods of making and using these polypeptides in a variety of therapeutic, diagnostic and prophylactic indications.

The invention relates generally to cleavable polypeptides, method of producing a cleavable moiety (CM) containing polypeptide by culturing a cell under conditions that lead to expression of the polypeptide, methods of manufacturing a cleavable moiety (CM) containing polypeptide by culturing a cell comprising a nucleic acid construct that encodes the cleavable polypeptide to express the cleavable polypeptide, and recovering the cleavable polypeptide, nucleic acids encoding the cleavable polypeptides, and vectors including the nucleic acids encoding the cleavable polypeptides.

The present invention provides activity-based probe compounds for labeling cysteine proteases. The compounds target proteases through specific target elements. The compounds also include a detectable element, such as a fluorescent label, a radiolabel or a chelating agent. In some cases, the compound also includes a quenching element that is released upon reaction with the protease. The invention also provides compositions comprising the compounds, and methods of using the compounds, such as labeling proteases in an animal body and visualizing a tumor in an animal body.

The invention relates generally to cleavable polypeptides, method of producing a cleavable moiety (CM) containing polypeptide by culturing a cell under conditions that lead to expression of the polypeptide, methods of manufacturing a cleavable moiety (CM) containing polypeptide by culturing a cell comprising a nucleic acid construct that encodes the cleavable polypeptide to express the cleavable polypeptide, and recovering the cleavable polypeptide, nucleic acids encoding the cleavable polypeptides, and vectors including the nucleic acids encoding the cleavable polypeptides.

To provide an isolated polypeptide comprising a tandem substrate, an activatable antibody that specifically binds to a target and a production method therefor, and methods for using these in a variety of therapeutic, diagnostic and prophylactic indications.SOLUTION: The invention provides polypeptides that include at least a first cleavable moiety (CM1) that is a substrate for at least one matrix metalloprotease (MMP) and at least a second cleavable moiety (CM2) that is a substrate for at least one serine protease (SP) or at least one cysteine protease (CP).SELECTED DRAWING: Figure 1

The present invention relates to anti-coronavirus compounds. The present invention includes a method for preventing and / or treating coronavirus infection by inhibiting cysteine proteases in viruses, in particular SARS-COV-2. Also provided are compositions / pharmaceutical compositions for preventing and / or treating coronavirus infection comprising any of the compounds, pharmaceutically acceptable salts thereof or mixtures thereof, and uses of the compounds.

The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.

Provided herein are fusion proteins comprising antigens (e.g., cancer neoantigens) conjugated to localization domains and / or self-proteins through an amino acid linker sequence that is preferentially cleaved by S-cathepsin, and methods of use thereof.

The invention relates to an application of Aloxistatin in preparation of a medicine for resisting virus infection, in particular to an application of Aloxistatin in preparation of a medicine for treating Orthopoxvirus virus infection or related diseases caused by Orthopoxvirus viruses, and particularly relates to an application of Aloxistatin in preparation of a medicine for treating Orthopoxvirus virus infection or related diseases caused by Orthopoxvirus viruses. Aloxistatin can significantly inhibit the activity of cysteine protease I7L of poxvirus, has potential ability to treat related diseases caused by orthopoxvirus such as monkey poxvirus, pox virus or vaccinia virus, and provides an effective drug use strategy for treating major infectious diseases caused by orthopoxvirus such as monkey poxvirus.