19 results about "TMPRSS2" 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.

The invention discloses a TMPRSS2 protein inhibitor efficacy prediction calculation method. A scoring function is constructed through a logP value, a virtual docking score and living cell inhibitor effect data to predict a drug inhibition effect. The method specifically comprises the following steps: constructing a TMPRSS2 overexpression cell model to screen drugs; the cell viability of various potential inhibitors is detected, and high-toxicity inhibitors are eliminated through a CCK-8 experiment; using flow cytometry to detect the cell average fluorescence intensity through a TMPRSS2 fluorescent probe to evaluate the enzyme activity influence of the inhibitor, and calculating the IC30 value; measuring the logP value of an effective inhibitor, and predicting the binding capacity of the effective inhibitor and TMPRSS2 by using Schrodinger software to obtain a virtual docking score; and analyzing the relationship among the IC30 value, the logP value and the virtual docking score, and constructing a scoring function to predict the drug effect. According to the method, the drug effect prediction can be simply, conveniently and quickly carried out, the drug screening consumption is reduced, and the drug screening period is shortened.

The present invention includes antibodies or antigen-binding fragments thereof that specifically bind to TMPRSS2, and methods of using such antibodies and fragments to treat or prevent viral infection (eg, influenza virus infection). [Selected Figure] Figure 2

Provided herein are methods related to treating or delaying progression of cancer in an individual. In some embodiments, the methods comprise detecting one or more TMPRSS2-ERG gene rearrangements in one or more samples from an individual having prostate cancer; and administering to the individual an effective amount of a treatment that comprises an anti-cancer agent.

Provided are a composition for diagnosing Down syndrome, a kit including the composition, a diagnostic method, and a method of providing information for diagnosing Down syndrome, the composition including an agent for measuring a methylation level of any one gene selected from the group consisting of MXRA8, MIB2, KIF26B, SP5, ZIC4, ENPEP, PITX2, SH3BP2, SEPP1, FLJ32255, SHROOM1, LINC00574, LOC154449, PRRT4, TMEM176B, MNX1, LOC101928483, EGFL7, NACC2, C9orf69, TLX1, FGF8, TACC2, CPXM2, NKX6-2, TLXINB, IQSEC3, PCDH8, F7, SOX9, PNMAL2, THBD, MAPK81P2, KLHDC7B, GPR143, IGHMBP2, MRGPRD, CHODL, NCAM2, CYYR1, GRIK1, OLIG2, CLIC6, SIM2, HLCS, MX2, MX1, TMPRSS2, SLC37A1, PDE9A, CBS, CRYAA, C21orf2, TRPM2, TSPEAR, LINC00162, SSR4P1, SLC19A1, LOC100129027, MCM3AP, YBEY, PRMT2, and ITSN1. Thus, Down syndrome can be diagnosed early with high accuracy, and the disclosure is expected to be applied as key a technology in the field of Down syndrome diagnosis.

The present invention relates to a multi-level virtual screening method based on molecular docking and the use of the compounds screened therefrom in the preparation of anti-lung cancer drugs. By analyzing the types of small molecule compounds obtained by the first screening, ginsenoside compounds are selected as the second screening library; the ginsenoside compound library is then selected as the second screening ligand, and virtual screening is performed again to obtain the docking score results of TMPRSS2 and ginsenoside compounds, obtain the top five compounds, and perform molecular docking and activity research. The present invention uses multi-level virtual screening to build a secondary virtual screening ligand library, enriching the variety of ligands of this type while reducing the number of compounds in the ligand library. While effectively improving the accuracy of virtual screening, it reduces the number of experimental screening compounds, shortens the R&D cycle, and saves costs.

Antibodies and antigen-binding fragments thereof that specifically bind to TMPRSS2 and methods of using such antibodies and fragments to treat or prevent viral infection (e.g., coronavirus infection or influenza virus infection) are provided.SOLUTION: Provided are neutralizing human antigen-binding proteins, e.g., antibodies or antigen-binding fragments thereof, that specifically bind to human H1, comprising: (a) CDR - H2, CDR - H3, and CDR - L1 of an immunoglobin heavy chain comprising specific amino acid sequences; and / or (b) CDR - L2, CDR - L3, and CDR - TMPRSS2 of an immunoglobin light chain comprising specific amino acid sequences.SELECTED DRAWING: None

To provide a TMPRSS2 inhibiting agent and an antiviral composition exhibiting excellent antiviral action.SOLUTION: The TMPRSS2 inhibiting agent contains at least one selected from a Platycodon root extract and cinnamon bark powder. The antiviral composition contains an extract from a plant or a plant powder as an active ingredient. The antiviral composition can be expected to exhibit an antiviral action by inhibiting the activity of TMPRSS2.SELECTED DRAWING: None

The invention belongs to the technical field of biological pharmacy, and particularly relates to an oligopeptide compound with anti-influenza virus activity and related application thereof. The oligopeptide compound provided by the invention has a structure as shown in a general formula I. The oligopeptide compound provided by the invention plays a role in inhibiting influenza virus by inhibiting the activity of TMPRSS2, and further plays a role in resisting influenza virus.

The invention relates to a Vero cell line capable of stably expressing TMPRSS2 as well as a construction method and application of the Vero cell line, and belongs to the technical field of biology. The invention provides a Vero cell line capable of stably expressing TMPRSS2. The cell line contains a TMPRSS2 coding gene which is integrated into a Rosa26 site of a cell genome of the cell line. The construction method of the cell line comprises the following steps: firstly, connecting an open reading frame cDNA sequence for coding TMPRSS2 with a donor vector carrying an attB site, then co-transfecting the donor vector and a Bxb1 expression vector into a Vero cell line, and carrying out antibiotic pressurized screening to obtain the stably expressed cell line. The cell line provided by the invention provides reliable candidate stromal cells for influenza virus cells independent of pancreatin culture, and has good application value for separation of influenza viruses and development of novel influenza vaccines.

The present invention includes antibodies, or antigen-binding fragments thereof, that specifically bind to TMPRSS2 and methods of using such antibodies and fragments to treat or prevent viral infections (e.g., influenza virus infections).

The invention relates to a method of post-surgical risk stratification of a prostate cancer subject, comprising determining a transmembrane protease, serine 2-ETS-related gene (TMPRSS2-ERG) fusion status in a biological sample obtained from the subject, determining a gene expression profile for each of one or more phosphodiesterase 4D variants in a biological sample obtained from the subject, determining an expression based risk score for the subject based on the gene expression profile for a selected phosphodiesterase 4D variant, and determining a post-surgical prognostic risk score for the subject based on the expression based risk score and post-surgical clinical variables of the subject, wherein the selected phosphodiesterase 4D variant is selected depending on the TM-PRSS2-ERG fusion status. This may allow for an improved stratification of the subject in a post-surgical setting that may result in better post-surgical, secondary treatment decisions.

The invention provides application of TMPRSS2 or a TMPRSS2-containing biological material in preparation of a virus proliferation promoting agent, and belongs to the technical field of virus replication. The amino acid sequence of the TMPRSS2 is as shown in SEQ ID NO. 2. The TMPRSS2 or a TMPRSS2-containing biological material is converted into an active enzyme with strong trypsin-like activity through a self-activation mechanism, and multi-cycle replication of enveloped viruses can be promoted even in the absence of trypsin. The recombinant LLC-MK2 cell for expressing the TMPRSS2, disclosed by the invention, can stably express the TMPRSS2 after continuous passage for 20 times. The recombinant LLC-MK2 cell supports the research and culture of the TMPRSS2-dependent mediated activated membrane fusion virus, promotes the in-vitro virus reproduction, improves the separation efficiency, is convenient to operate, and provides a method for improving the virus titer, expanding the virus yield and improving the in-vitro adaptability of clinical strains.

The present invention discloses compounds that target ubiquitination degradation of TMPRSS2 protein, as well as preparation methods and applications thereof. The compounds of the present invention are represented by general formula (I) or (II), wherein the E3 ligand is a ligand of the E3 ligase VHL or CRBN, and Linker is a linking group. The compounds of the present invention can target and degrade TMPRSS2 protein, exhibit good inhibitory effects on various tumor cell lines, and have low toxicity to normal cells. The preparation method of the compounds of the present invention is simple to operate and requires mild conditions. The resulting compounds have TMPRSS2 protein degradation activity and significant anti-tumor effects. Pharmacologically or physiologically acceptable salts thereof can be used to prepare anti-tumor drugs.

In alternative embodiments, provided is a protease-responsive and surface-potential-tunable peptide-conjugated AIEgens (EGTP) for TMPRSS2 selective imaging and accurate inhibitor screening, where EGTP comprises four segments: the first is a polyglutamic acid (Glu, E for short in EGTP) that increases the solubility, blocks the positive charges and cell-penetrating ability of PyTPE; the second comprises a spacer trimylglycine (GGG, G) designed to enhance probe flexibility and reduce steric hindrance for TMPRSS2-substrate interactions; the third component second comprises a TMPRSS2-responsive peptide (QAR, T), which can be cleaved by TMPRSS2 after QAR sequence; and the fourth second comprises a positive charged AIEgens (PyTPE, P). In alternative embodiments, provided are main protease (Mpro)-responsive and modular-peptide-conjugated probes for the selective imaging and inhibition of SARS-CoV-2 infected cells via enzyme-instructed self-assembly and aggregation-induced emission.

This invention relates to methods for selecting patients having prostate cancer for treatment with a PARP inhibitor, such as talazoparib, or a pharmaceutically acceptable salt thereof, and an androgen receptor inhibitor, such as enzalutamide, or a pharmaceutically acceptable salt thereof, comprising: i) determining an ERG gene alteration status, wherein the ERG gene alteration is a TMPRSS2-ERG gene fusion / rearrangement, and / or determining an RB1 gene alteration status, from a biological sample of the prostate cancer from the subject; and ii) selecting patients with the TMPRSS2-ERG gene fusion / rearrangement and / or the RB1 gene alteration for treatment.

The application relates to an aromatic formyl compound, a preparation method and application thereof, a structural formula of the aromatic formyl compound is shown as formula I, the aromatic formyl compound or a medicinal salt thereof provided by the application has good TMPRSS2 enzyme inhibiting activity, and provides a research basis for further development of antiviral drugs.

A composition for decomposition of trypsin or TMPRSS2 containing, as an active ingredient, bacteria having 00502 protein or a protein having 30% or more sequence identity with the amino acid sequence of 00502 protein and having trypsin binding ability or bacteria having 00509 protein or a protein having 30% or more sequence identity with the amino acid sequence of 00509 protein and having trypsin binding ability.

This invention discloses an extract of Phyllanthus emblica, its preparation method, and its application, relating to the field of traditional Chinese medicine technology. The preparation method of the Phyllanthus emblica extract includes the following steps: S1. Extracting Phyllanthus emblica with a solvent to obtain an extract; S2. Centrifuging the extract, collecting the supernatant, then filtering it through a membrane to obtain a filtrate with a molecular weight below 1000D, concentrating it, and drying it to obtain the Phyllanthus emblica extract. This invention uses membrane separation technology to prepare an Phyllanthus emblica extract that inhibits coronavirus main protease (Mpro / 3Clpro), transmembrane serine protease 2 (Tmprss2), and neuraminidase (NA).