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31 results about "Caspase activity" patented technology

Caspase-3 is activated in the apoptotic cell both by extrinsic (death ligand) and intrinsic (mitochondrial) pathways. The zymogen feature of caspase-3 is necessary because if unregulated, caspase activity would kill cells indiscriminately.

Dimeric small molecule potentiators of apoptosis

Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Dimeric small molecule potentiators of apoptosis

Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Protease specific cleavable luciferases and methods of use thereof

Provided are methods and compositions useful in detecting protease activity in a sample, as well as methods of identifying agents that modulate protease activity. The methods and compositions provide a modified luciferase polynucleotide sequence and a luciferase polypeptide containing protease recognition sequences, wherein cleavage of the recognition sequence by a protease inhibits luciferase activity. Further provided are methods and compositions for detecting and modulating caspase activity and apoptosis.
Owner:MILLIPORE CORP

Visualization and quantitation of cellular cytotoxicity using cell-permeable fluorogenic protease substrates and caspase activity indicator markers

This invention provides a non-radioactive assay to monitor and quantify the target-cell killing activities mediated by cytotoxic T lymphocytes (CTLs). This assay is predicated on the discovery that apoptosis pathway activation and, in particular, granzyme B activity, provides a measure of cytotoxic effector cell activity. In one embodiment, measurement of CTL-induced granzyme B activation in target cells is achieved through detection of the specific cleavage of fluorogenic granzyme B substrates. This assay reliably detects antigen-specific CTL killing of target cells, and provides a more sensitive, more informative and safer alternative to the standard 51Cr-release assay most often used to quantify CTL responses. The assay can be used to study CTL-mediated killing of primary host target cells of different cell lineages, and enables the study of antigen-specific cellular immune responses in real time at the single-cell level. As such, the assay can provide a valuable tool for studies of infectious disease pathogenesis and development of new vaccines and immunotherapies.
Owner:ONCOIMMUNIN

GLP-1 and FGF21 combinations for treatment of diabetes type 2

The invention relates to the use of a Fibroblast Growth Factor 21 (FGF21 ) compound and a Glucagon-Like Peptide 1 (GLP-1 ) compound in combination for the preparation of a medicament for the treatment of diabetes, more in particular type 2 diabetes, as well as pharmaceutical compositions comprising certain FGF21 and GLP-1 compounds in combination, together with a pharmaceutically acceptable carrier. The combination has a significant effect on parameters of relevance for diabetes type 2, viz. on the viability of [beta] cells ex vivo in the presence of free fatty acids, on caspase activity of [beta] cells ex vivo (a measure of cell apoptosis), and a blood glucose lowering effect on db / db mice in vivo.
Owner:NOVO NORDISK AS

Chimeric pro-caspases and methods of using same

The present invention relates to a chimeric pro-caspase, which contains a pro-caspase domain and an oligomerizing domain. The invention also relates to an antibody that reacts specifically with a chimeric pro-caspase. In addition, the invention further relates to a polynucleotide encoding a chimeric pro-caspase, and to nucleotide sequences, which can hybridize specifically with a polynucleotide encoding a chimeric pro-caspase. The present invention also relates to a method of inducing apoptosis in a cell by providing a chimeric pro-caspase in the cell, wherein the chimeric pro-caspase includes a pro-caspase domain and an oligomerizing domain, whereby the chimeric pro-caspase forms an oligomer in the cell, thereby activating caspase activity of the chimeric pro-caspase and inducing apoptosis in the cell. The present invention further relates to a method of reducing the severity of a pathologic condition in a subject, by providing cells of the subject that are involved in the pathologic condition with a chimeric pro-caspase comprising a pro-caspase domain and an oligomerizing domain, whereby the chimeric pro-caspase forms an oligomer in the cells, thereby activating caspase activity of the chimeric pro-caspase, inducing apoptosis in the cells, and reducing the severity of the pathologic condition in the subject.
Owner:CALIFORNIA INST OF TECH

Visualization and quantitation of cellular cytotoxicity using cell-permeable fluorogenic protease substrates and caspase activity indicator markers

This invention provides a non-radioactive assay to monitor and quantify the target-cell killing activities mediated by cytotoxic T lymphocytes (CTLs). This assay is predicated on the discovery that apoptosis pathway activation and, in particular, granzyme B activity, provides a measure of cytotoxic effector cell activity. In one embodiment, measurement of CTL-induced granzyme B activation in target cells is achieved through detection of the specific cleavage of fluorogenic granzyme B substrates. This assay reliably detects antigen-specific CTL killing of target cells, and provides a more sensitive, more informative and safer alternative to the standard 51Cr-release assay most often used to quantify CTL responses. The assay can be used to study CTL-mediated killing of primary host target cells of different cell lineages, and enables the study of antigen-specific cellular immune responses in real time at the single-cell level. As such, the assay can provide a valuable tool for studies of infectious disease pathogenesis and development of new vaccines and immunotherapies.
Owner:ONCOIMMUNIN

Inhibitors of caspases

The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), or interferon-γ-(“IFN-γ”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis-, and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
Owner:VERTEX PHARMA INC

Irreversible caspase-3 inhibitors as active site probes

The present invention encompasses a compound of Formula (I) useful as caspase active site probes. These probes can be used to determine whether a caspase has been activated, in cells or in tissues of animal models of various pathologies. Furthermore, through competition based assays, these caspase active site probes can be used to calculate the percentage of occupancy of active caspases by other, unlabeled inhibitors.
Owner:MERCK FROSST CANADA INC

Caspase biosensor, application thereof and detection method of caspase activity

The invention discloses a caspase biosensor, application thereof and a detection method of caspase activity. The caspase biosensor comprises a magnetic bead, a detection probe, an annular template, DNA polymerase and a secondary primer, wherein the surface of the magnetic bead is coated with streptavidin; the detection probe comprises a peptide substrate structural domain and a DNA primer structural domain which are connected, the peptide substrate structural domain is an amino acid sequence, and the DNA primer structural domain is a single-stranded DNA sequence; the peptide substrate structural domain contains a specific site, the specific site can be recognized and cut by caspase, the specific site and a connecting site are separated by n amino acids, the connecting site is a joint of the peptide substrate structural domain and the DNA primer structural domain, the peptide substrate structural domain is connected with biotin, the specific site is positioned between the biotin and theconnecting site, and n is a natural number smaller than 10; and the DNA primer structural domain can be matched with the annular template, the DNA polymerase and the secondary primer for a branch rolling circle amplification reaction.
Owner:SHANDONG NORMAL UNIV

Peptides modulating caspase activation

The present invention provides structures of small molecules capable of modulating apoptotic cell death. More specifically, the structures relate to the structures of apoptotic active sites of mammalian alpha-fetoprotein (AFP) and albumin. Peptides mimicking the active site contain two sequences, Arg-Gly-Asp and Asp-X-X-Asp, wherein X means any amino acid. These sequences are needed in the same molecule for causing a wide range of biological activities. The peptides can be utilized to suppress apoptotic pathways by inhibiting the cytochrome c-mediated caspaseactivation. Thus, the peptides can be used to inhibit effects of apoptosis induced by oxidative stress, drugs, cytokines, Fas-ligand, alpha-fetoprotein, used to prevent apoptosis in culturing cells, in organ transplantation, in immunological autoimmune disorders and immunodeficiency syndrom induced by viral infection, or to diminish side cytotoxic effects after chemotherapy and radiation therapy.
Owner:鲍里斯·爱德华多维奇·塔图洛夫

Method of treating solid tumors and leukemias using combination therapy of vitamin D and anti-metabolic nucleoside analogs

The present invention relates to a method of inhibiting solid tumor cell or leukemia cell proliferation by first administering to a solid tumor cell or leukemia cell either vitamin D or a derivative thereof and subsequently administering at least one anti-metabolic nucleoside analog to the solid tumor cell or the leukemia cell. Also disclosed is a method of treating a cancerous condition. Methods of down regulating a p-AKt survival signaling pathway and modulating activity of a pro-apoptotic caspases is also disclosed.
Owner:ROSWELL PARK CANCER INST

Visualization and quantitiation of cellular cytotoxicity using cell-permeable fluorogenic protease substrates and caspase activity indicator markers

This invention provides a non-radioactive assay to monitor and quantify the target-cell killing activities mediated by cytotoxic T lymphocytes (CTLs). This assay is predicated on the discovery that apoptosis pathway activation and, in particular, caspase activity, provides a measure of cytotoxic effector cell activity. In one embodiment, measurement of CTL-induced caspase activation in target cells is achieved through detection of the specific cleavage of fluorogenic caspase substrates. This assay reliably detects antigen-specific CTL killing of target cells, and provides a more sensitive, more informative and safer alternative to the standard 51Cr-release assay most often used to quantify CTL responses. The assay can be used to study CTL-mediated killing of primary host target cells of different cell lineages, and enables the study of antigen-specific cellular immune responses in real time at the single-cell level. As such, the assay can provide a valuable tool for studies of infectious disease pathogenesis and development of new vaccines and immunotherapies.
Owner:ONCOIMMUNIN

Methods and compositions for use in the diagnosis and treatment of chronic immune disease

Methods and compositions are provided for use in the diagnosis and treatment of a host suffering from a chronic immune disease. In the diagnostic methods of the subject invention, a host derived sample, typically PBMC or a derivative thereof, is assayed for the presence of low molecular weight fragments of RNase L, typically in conjunction with an evaluation of caspase activity. The results of this assay are then employed to diagnose and / or characterize a chronic immune disease in the host. In the treatment methods of the subject invention, an effective amount of agent capable of enhancing RNase L homodimer activity in the host, e.g., in host PBMC, is administered to the host. Also provided are methods for identifying agents having RNase L cleavage-inhibitory activity or RNase L fragment antagonist activity.
Owner:R E D LAB

Isatin derivatives for use as in vivo imaging agents

The present invention provides isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising said derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing said derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity.
Owner:IMPERIAL INNOVATIONS LTD +1

Caspase inhibitor

InactiveUS20090149436A1Inhibit caspase activityOrganic active ingredientsBiocideCaspase inhibitorsDisease
The present invention provides a caspase inhibitor containing a cobalt porphyrin complex compound or cobalt choline complex compound as an active ingredient. The caspase inhibitor of the present invention can strongly and specifically inhibit the caspase activity. In addition, the caspase inhibitor / cobalt porphyrin complex compound or cobalt choline complex compound of the present invention is useful as a pharmaceutical agent for the prophylaxis or treatment of various diseases relating to apoptosis.
Owner:ASTELLAS PHARMA INC

Methods for detecting membrane derived caspase activity and modulators thereof

The present invention provides methods for detecting membrane-derived apoptotic activity. In one embodiment, the present invention provides methods of identifying membrane-derived caspase activity. In another embodiment, drug discovery methods are provided for screening compounds that inhibit or enhance the activity of membrane-derived caspases. In these various embodiments, heavy membrane fractions are used in the screening methods described herein.
Owner:IDUN PHARMA INC

Application of musculus growth inhibin for preparing anticarcinogen

An application of myostatin in preparing the orally taken antineoplastic medicines for treating prostatic cancer, cencer of uterine cervix, lung cancer, liver cancer, etc is disclosed.
Owner:THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI

Plasma derived from human umbilical cord blood for the treatment of neurodegenerative disorders

A method of treating neurodegenerative diseases using hUCB plasma is presented herein. hUCB plasma attenuated the hyperactive response (Group III) and potentiated the normal response in Group I ALS patients, but did not alter that of the non-responders to PHA (Group II). The elevated activity of caspase 3 / 7 observed in the MNCs from ALS patients was significantly reduced by hUCB plasma treatment. The ability of hUCB plasma to modulate the mitogen cell response and reduce caspase activity suggest that the use of hUCB plasma alone, or with stem cells, may prove useful as a therapeutic in ALS patients. hUCB plasma was shown to increase therapeutic efficacy of MNCs as well as decrease apoptosis of MNCs. The cytokine profile of hUCB plasma supports its usefulness as a sole therapeutic as well as an additive to MNCs.
Owner:UNIV OF SOUTH FLORIDA +1

Screening assays for agents that alter inhibitor of apoptosis (IAP) protein regulation of caspase activity

The present invention relates to an action between an inhibitor of apoptosis (IAP) protein and members of the caspase family of cell death proteases, for example, an interaction of the X chromosome linked IAP (XIAP) and caspase-3, caspase-7 or caspase-9, wherein the IAP regulates the activity of the caspases. The invention provides screening assays for identifying agents that alter the specific association of an IAP such as XIAP, c-IAP-1 or c-IAP-2 and a caspase such as caspase-3 or caspase-7. The invention also provides screening assays for identifying agents that alter the specific association of an IAP such as XIAP, c-IAP-1 or c-IAP-2 and a pro-caspase such as pro-caspase-9. In addition, the invention also provides methods for identifying agents that modulate the activity of a caspase in the presence of an IAP and that regulate the activation of a pro-caspase by an IAP. The invention further provides methods of reducing the severity of a pathologic condition in an individual by administering to the individual an agent that alters the caspase inhibitory activity of an IAP. In addition, the invention provides methods of modulating the ability of a population of cells to survive ex vivo by contacting the cells with an agent that alters the caspase inhibitory activity of an IAP in the cells.
Owner:SANFORD BURNHAM MEDICAL RES INST

Plasma derived from human umbilical cord blood for the treatment of neurodegenerative disorders

Amyotrophic lateral sclerosis (ALS) is a progressive neurodegenerative disease characterized by degeneration of motor neurons in the spinal cord and brain. Increasing evidence shows autoimmune mechanisms likely promote disease progression. Human umbilical cord blood (hUCB) derived plasma is rich in cytokines and growth factors that are required for growth and survival of cells during hematopoiesis. hUCB plasma attenuated the hyperactive response (Group III) and potentiated the normal response in Group I ALS patients, but did not alter that of the non-responders to PHA (Group II). The elevated activity of caspase 3 / 7 observed in the MNCs from ALS patients was significantly reduced by hUCB plasma treatment. The ability of hUCB plasma to modulate the mitogen cell response and reduce caspase activity suggest that the use of hUCB plasma alone, or with stem cells, may prove useful as a therapeutic in ALS patients.
Owner:SANERON CCEL THERAPEUTICS +1

Excision enzyme III-driven three-dimensional DNA nano machine and application thereof

The invention provides an excision enzyme III-driven three-dimensional DNA nano machine and application thereof. The three-dimensional DNA nano machine comprises a signal probe and nanogold structure and a detection probe, the signal probe comprises a signal probe sequence and fluorescent molecules, the detection probe comprises a caspase recognition site and a DNA trigger chain, and the DNA trigger chain and the signal probe sequence are complementary; the detection probe is split in the presence of caspase to release a structure containing a DNA trigger chain, the DNA trigger chain in the structure is hybridized with the signal probe to form double-chain DNA, the double-chain DNA can be recognized and digested by excision enzyme III and releases fluorescent molecules in the signal probe, and the DNA trigger chain immediately recovers a single chain and continues to be hybridized with other signal probes, therefore, the cyclic release of the fluorescent molecules is realized. The machine can be used for simultaneously detecting the activities of various caspase, is high in detection sensitivity, and can also be used for screening caspase inhibitors.
Owner:SHANDONG NORMAL UNIV

Application of musculus growth inhibin for preparing anticarcinogen

An application of myostatin in preparing the orally taken antineoplastic medicines for treating prostatic cancer, cencer of uterine cervix, lung cancer, liver cancer, etc is disclosed.
Owner:THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI

Method of screening inhibitor of caspase activity by lipopolysaccharide

Provided are a method of screening an inhibitor of caspase activity by lipopolysaccharide and a method of screening a therapeutic agent for inflammatory diseases or sepsis using the same. Accordingly, it is possible to develop a caspase-4-specific inhibitor.
Owner:KOREA INST OF SCI & TECH

Exonuclease III-driven three-dimensional DNA nanomachines and their applications

The present application provides an exonuclease III-driven three-dimensional DNA nanomachine and its application. The three-dimensional DNA nanomachine includes a signal probe@nano-gold structure and a detection probe, and the signal probe includes a signal probe sequence and a fluorescence Molecules, the detection probe contains a caspase recognition site and a DNA trigger strand, and the DNA trigger strand is complementary to the signal probe sequence; the detection probe is cleaved in the presence of caspase to release the DNA trigger strand containing the DNA trigger strand. structure, the DNA trigger strand in this structure hybridizes with the signal probe to form double-stranded DNA, the double-stranded DNA can be recognized and digested by exonuclease III, and the fluorescent molecules in the signal probe are released. Continue to hybridize with other signaling probes to achieve cyclic release of fluorescent molecules. The invention can realize the simultaneous detection of multiple caspase activities with high detection sensitivity, and can also be used for screening caspase inhibitors.
Owner:SHANDONG NORMAL UNIV

Novel Protein Highly Producing Recombinant Animal Cell, Method for Preparing the Same, and Method for Mass-Producing Protein Using the Same

InactiveUS20090099338A1Improve survivabilityConsiderable cost downFactor VIIFibrinogenBiotechnologyApoptosis
A gene encoding a production amount-potentiating factor is introduced into an animal cell to transform the cell. Alternatively, a protein production gene and the gene encoding the production amount-potentiating factor are introduced into the animal cell to transform the cell. Herein, as the production amount potentiating factor, there is used a factor having caspase activity inhibiting activity and / or protein biosynthesis activity potentiating action, for example, baculovirus P35. Further, the animal cell is cultured by a culturing method under a condition that apoptosis is not induced, so that a protein is mass-produced.
Owner:JURIDICAL FOUND THE CHEMO SERO THERAPEUTIC RES INST
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