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82 results about "Plasminogen Activator Inhibitors" patented technology

Gene expression profiling of uterine serous papillary carcinomas and ovarian serous papillary tumors

InactiveUS20050037389A1Different responseAccelerated differential diagnosisSugar derivativesMicrobiological testing/measurementPapillary carcinomaEndometrial epithelium
Oligonucleotide microarrays were used to profile and compare gene expression patterns between uterine serous papillary carcinoma and ovarian serous papillary carcinoma or normal endometrial epithelial cells. mRNA fingerprints readily distinguish the more biologically aggressive and chemotherapy resistant USPC from OSPC or NEC. Plasminogen activator inhibitor is the most highly up-regulated gene in OSPC relative to USPC, whereas the c-erbB2 gene product (HER-2 / neu) is strikingly overexpressed in USPC relative to OSPC and may therefore represent a novel diagnostic and therapeutic marker for this highly aggressive subset of endometrial tumors.
Owner:THE BOARD OF TRUSTEES OF THE UNIV OF ARKANSAS

Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.
Owner:EASTERN MICHIGAN UNIVERSITY +1

Peptide Inhibition of Lung Epithelial Apoptosis and Pulmonary Fibrosis

During lung injury, p53 expression increases, inducing plasminogen activator inhibitor-1 (PAI-1) while inhibiting expression of urokinase-type plasminogen activator (uPA) and its receptor (uPAR), resulting in apoptosis of lung epithelial cells (LECs). In the bleomycin lung injury model, p53 and PAI-1 are induced while uPA and uPAR are inhibited. A 20 residue peptide DGIWKASFTTFTVTKYWFYR termed PP-1 (the Cav-1 scaffolding domain) or peptide NYHYLESSMTALYTLGH, termed PP-2, protected LECs from bleomycin-induced apoptosis in vitro and in vivo and prevented subsequent pulmonary fibrosis by attenuating lung epitheilial damage. Pharmaceutical compositions, peptide multimers and deliverable polypeptides comprising the above peptides are dislcosed. The peptides and functional variants, peptide multimers, cell-targeted polyepeptides and pharmaceutical compositions are used in methods for inhibiting apoptosis of injured or damaged lung epithelial cells and for treating acute lung injury and consequent pulmonary fibrosis.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Modified plasminogen inhibitor type-1 and methods based thereon

The present invention is based upon the discovery that modified plasminogen activator inhibitor type-I (PAI-1) in which two or more amino acid residues that do not contain a sulfliydryl group have been replaced with amino acid residues that contain a sulfhydryl group and, therefore, forms intramolecular disulfide bonds, have increased in vivo half-life. Also disclosed are the modified PAI-1 proteins, derivatives and analogs thereof, specific antibodies, nucleic acid molecules and host cells. Methods for producing modified PAI-1, derivatives and analogs are also provided. The invention further relates to Therapeutics, pharmaceutical compositions and method of using the composition for treatment. The invention may be used to inhibit angiogenesis in a subject, thereby treating diseases or conditions associated with undesired angiogenesis and cell proliferation. Such conditions include psoriasis, chronic inflammation, tumor invasion and metastasis invention are useful for the treatment, prophylaxis, management and amelioration of cardiovascular diseases such as, but not limited to those that are related to hyerfibrinolysis, hemophilia, and vessel leakage syndrome.
Owner:UNIVERSITY OF TOLEDO

Hemostatic compositions, devices and methods

A hemostatic composition which comprises at least one procoagulant metal ion, such as silver (I) or mercury (II), and at least one procoagulant biopolymer, such as collagen, thrombin, prothrombin, fibrin, fibrinogen, heparinase, Factor VIIa, Factor VIII, Factor IXa, Factor Xa, Factor XII, von Willebrand Factor, a selectin, a procoagulant venom, a plasminogen activator inhibitor, glycoprotein IIb-IIIa, a protease, or plasma. The composition in the form of a paste, dough, glue, liquid, lyophilized powder or foam, may be provided, for application to a wound. A hemostatic device is also described which comprises a hemostatic composition as described above. The device may be in the form of, for example, a plug, bandage, gauze, cloth, tampon, membrane or sponge. Methods are also provided for prophylaxis or treatment of bleeding at a site by application to the site of the composition or device as described.
Owner:RUTGERS THE STATE UNIV

Use of Urokinase Type Plasminogen Activator Inhibitors for the Treatment of Corneal Disorders

The invention concerns the use of inhibitors of the urokinase type of plasminogen activator (uPA) appearing in the anterior segment of the eye, for the treatment and prevention of corneal ulcers and other disorders. The invention further concerns pharmaceutical compositions, comprising inhibitors of uPA, preferably eye drops and eye ointments. The pharmaceutical compositions according to the invention preferably comprise PAI-2 protein or a derivative thereof retaining uPA-inhibiting capacity, or a tripeptide aldehyde inhibitor, preferably the D-Phe-Pro-Arg-aldehyde (Ald-1). The PAI-2 protein, used according to the invention, is preferably produced through bacterial expression, as a fusion protein.
Owner:UNIVERSITY OF DEBRECEN

Plasminogen Activator Inhibitor-1 Inhibitor

ActiveUS20120022080A1Enhanced inhibitory effectPreventing and treating thrombosisBiocideSenses disorderPai 1 activityDisease
The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.
Owner:RENASCI

Peptide inhibition of lung epithelial apoptosis and pulmonary fibrosis

During lung injury, p53 expression increases, inducing plasminogen activator inhibitor-1 (PAI-1) while inhibiting expression of urokinase-type plasminogen activator (uPA) and its receptor (uPAR), resulting in apoptosis of lung epithelial cells (LECs). In the bleomycin lung injury model, p53 and PAI-1 are induced while uPA and uPAR are inhibited. A 20 residue peptide DGIWKASFTTFTVTKYWFYR termed PP-1 (the Cav-1 scaffolding domain) or peptide NYHYLESSMTALYTLGH, termed PP-2, protected LECs from bleomycin-induced apoptosis in vitro and in vivo and prevented subsequent pulmonary fibrosis by attenuating lung epitheilial damage. Pharmaceutical compositions, peptide multimers and deliverable polypeptides comprising the above peptides are dislcosed. The peptides and functional variants, peptide multimers, cell-targeted polyepeptides and pharmaceutical compositions are used in methods for inhibiting apoptosis of injured or damaged lung epithelial cells and for treating acute lung injury and consequent pulmonary fibrosis.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Plasminogen activator inhibitor-1 inhibitor

The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof.Each symbol is defined as those in the specification.
Owner:RENASCI

Plasminogen activator inhibitor-1 inhibitors and methods of use thereof

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or disorder associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to prevent or reduce thrombosis and fibrosis, to promote thrombolysis, and to modulate lipid metabolism and treat diseases or disorders associated with elevated PAI-1, cholesterol, or lipid levels.
Owner:EASTERN MICHIGAN UNIVERSITY +1

Modified plasminogen activator inhibitor type-1 and methods based thereon

The present invention is based upon the discovery that modified plasminogen activator inhibitor type-I (PAI-1) in which two or more amino acid residues that do not contain a sulfhydryl group have been replaced with amino acid residues that contain a sulfhydryl group and, therefore, forms intramolecular disulfide bonds, have increased in vivo half-life. Also disclosed are the modified PAI-1 proteins, derivatives and analogs thereof, specific antibodies, nucleic acid molecules and host cells. Methods for producing modified PAI-1, derivatives and analogs are also provided. The invention further relates to Therapeutics, pharmaceutical compositions and method of using the composition for treatment. The invention may be used to inhibit angiogenesis in a subject, thereby treating diseases or conditions associated with undesired angiogenesis and cell proliferation. Such conditions include psoriasis, chronic inflammation, tumor invasion and metastasis and conditions in which angiogenesis is pathogenic. The modifide PAI-1 molecules of the present invention are useful for the treatment, prophylaxis, management and amelioration of cardiovascular diseases such as, but not limited to those that are related to hyperfibrinolysis, hemophilia, and vessel leakage syndrome.
Owner:UNIVERSITY OF TOLEDO

Peptides derived from plasminogen activator inhibitor-1 and uses thereof

The present invention relates to isolated 18-mer peptides corresponding to amino acid residues 369-386 of human plasminogen activator inhibitor 1 (PAI-1) and fragments thereof, compositions that include such peptides, and uses of such compositions for treating thromboembolic diseases and pathological conditions associated with neurological damage.
Owner:D PHARMA LTD

Modified plasminogen activator inhibitor type-1 molecule and methods based thereon

InactiveUS20100184667A1Reduce cancer cell growthInhibit primaryPeptide/protein ingredientsMuscular disorderUrokinase Plasminogen ActivatorVitronectin
The present invention relates to a modified plasminogen activator inhibitor type-1 (PAI-1) molecule that displays CN an increased in vivo half-life of the active form of PAI-1, but is deficient in one or more functional activities as compared to the wild-type PAI-1 protein. The modified PAI-1 molecule that displays an increased half-life further displays at least one of the following funtional characteristics: (i) decreased binding activity to at least one of the following molecules: urokinase plasminogen activator (uPA), tissue plasminogen activator (tPA) and vitronectin (Vn); and (ii) decreased specific activity against at least one of the following molecules: uPA, tPA and Vn. The invention further relates to pharmaceutical compositions comprising modified PAI-1 molecules and methods of using these pharmaceutical compositions for treatment.
Owner:UNIVERSITY OF TOLEDO

5-phenyl-3-pyridazinone derivative

To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and / or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I):and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and / or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.
Owner:KOWA CO LTD

Food-grade recombined lactococcal lactis capable of producing conjugated linoleic acid as well as construction method and application thereof

The invention discloses food-grade recombined lactococcal lactis capable of producing conjugated linoleic acid as well as a construction method and an application thereof. The method for constructing the recombined lactococcal lactis comprises the step of introducing an encoding gene of a protein PAI (Plasminogen Activator Inhibitor) into lactococcal lactis serving as host bacteria to obtain the recombined lactococcal lactis, the conversion rate of the trans-10, cis-12 conjugated linoleic acid of which is higher than that of the host bacteria, wherein the protain PAI is a protein (a) composed of amino acid sequences shown in SEQ IN No. 2 or a protein (b) which is formed by replacing the amino acid sequences shown in SEQ IN No. 2 with one or several amino acid residues and / or deleting and / or adding the amino acid sequences shown in SEQ IN No. 2 and has the activity of linoleate isomerase, or is derived from the protein (1) and has the activity of linoleate isomerase. The food-grade recombined lactococcal lactis disclosed by the invention can produce t10c12-CLA, and the content of the t10c12-CLA accounts for 15.19-23.91% of the total quantity of thallus fatty acids.
Owner:CHINA AGRI UNIV

Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.
Owner:EASTERN MICHIGAN UNIVERSITY +1

Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.
Owner:RGT UNIV OF MICHIGAN +1

Gene expression profiling of uterine serous papillary carcinomas and ovarian serous papillary tumors

InactiveUS7659062B2Different responseEasy to identifySugar derivativesMicrobiological testing/measurementPapillary carcinomaEndometrial epithelium
Oligonucleotide microarrays were used to profile and compare gene expression patterns between uterine serous papillary carcinoma and ovarian serous papillary carcinoma or normal endometrial epithelial cells. mRNA fingerprints readily distinguish the more biologically aggressive and chemotherapy resistant USPC from OSPC or NEC. Plasminogen activator inhibitor is the most highly up-regulated gene in OSPC relative to USPC, whereas the c-erbB2 gene product (HER-2 / neu) is strikingly overexpressed in USPC relative to OSPC and may therefore represent a novel diagnostic and therapeutic marker for this highly aggressive subset of endometrial tumors.
Owner:THE BOARD OF TRUSTEES OF THE UNIV OF ARKANSAS

Inhibitor of plasminogen activator inhibitor-1

The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula.Each symbol is defined as those in the specification.
Owner:RENASCI

Chimeric truncated and mutant variant of tissue plasminogen activator (t-pa) resistant to plasminogen activator inhibitor-1

The various embodiments herein provide a chimeric truncated and mutant variant of a tissue plasminogen activator (t-pa) and a method for preparing the same. According to an embodiment herein, the mutant variant comprises a signal sequence domain, followed by a chimeric tetrapeptide, followed by a tripeptide, followed by a kringle 2 domain, followed by a serine protease domain and a substituted amino acids at position 128-131. The substituted amino acids are AAAA (SEQ ID NO: 3) amino acids. The chimeric tetrapeptide is Gly-His-Arg-Pro (SEQ ID NO: 1). The chimeric tetrapeptide is at a position of 36 to 39 amino acid of the mutant variant. The tripeptide is Ser-Tyr-Glu. According to an embodiment herein, a chimeric truncated and mutant variant of a tissue plasminogen activator comprises a native t-pa deleted with Finger domain, a Growth Factor domain and a Kringle 1 domain, a chimeric tetrapeptide and a substituted amino acids at a position of 128-131.
Owner:MAHBOUDI FEREIDOUN +3

Antibodies to Plasminogen Activator Inhibitor-1 (PAI-1) and Uses Thereof

ActiveUS20160200831A1Convenient treatmentRestoring plasmin generationDigestive systemAntibody ingredientsPai 1 activityIn vivo
The invention provides antibodies that specifically bind to Plasminogen Activator Inhibitor type-1 (PAI-1), The invention also provides pharmaceutical compositions, as well as nucleic acids encoding anti-PAI-1 antibodies, recombinant expression vectors and host cells for making such antibodies, or fragments thereof. Methods of using antibodies to modulate PAI-1 activity or detect PAI-1, either in vitro or in vivo, are also provided. The disclosure further provides methods of making antibodies that specifically bind to PAI-1 in the active conformational state.
Owner:SANOFI SA

Modified plasminogen activator inhibitor type-1 molecule and methods based thereon

The present invention relates to a modified plasminogen activator inhibitor type-1 (PAI-1) molecule that displays an increased in vivo half-life of the active form of PAI-1, but is deficient in one or more functional activities as compared to the wild-type PAI-1 protein. The modified PAI-1 molecule that displays an increased half-life further displays at least one of the following functional characteristics: (i) decreased binding activity to at least one of the following molecules: urokinase plasminogen activator (uPA), tissue plasminogen activator (tPA) and vitronectin (Vn); and (ii) decreased specific activity against at least one of the following molecules: uPA, tPA and Vn. The invention further relates to pharmaceutical compositions comprising modified PAI-1 molecules and methods of using these pharmaceutical compositions for treatment.
Owner:UNIVERSITY OF TOLEDO

Brain associated inhibitor of tissue-type plasminogen activator

The present invention relates to a novel BAIT protein which is a member of serpin superfamily which is expressed primarily in brain tissue. In particular, isolated nucleic acid molecules are provided encoding the human and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of BAIT activity. Also provided are diagnostic methods for detecting nervous system-related disorders and therapeutic methods for treating nervous system-related disorders. Additionally, the present invention is related to methods of treating patients with BAIT polynucleotides or polypeptides, wherein said patients have had a stroke.
Owner:HUMAN GENOME SCI INC +1

Biomarkers of vascular disease

A biomarker panel including a four-panel test for clotting that detects soluble fibrin (SF), thrombin-antithrombin complex (TAT), antithrombin III (ATIII), and plasminogen activator inhibitor (PAI-1). A biomarker panel including a three-panel test for glycocalyx integrity that detects syndecan-1 (SDC1), heparan sulfate (HS), and hyaluronidase (HAD). A biomarker panel including a test that detects a biomarker chosen from soluble fibrin (SF), thrombin-antithrombin complex (TAT), antithrombin III (ATIII), plasminogen activator inhibitor (PAI-1), syndecan-1 (SDC1), heparan sulfate (HS), hyaluronidase (HAD), and combinations thereof. A kit including a biomarker panel, instructions for use, materials to take and apply samples to the panel, and descriptions of biomarker levels and their meaning. Methods of detecting the presence of vascular disease, determining the stage of vascular disease, monitoring the progress of vascular disease treatments, and monitoring the efficacy of drugs during drug development.
Owner:ARTEREZ INC

Anti-blood stasis syndrome application of scirpusin component C in common burreed rhizome

ActiveCN109172577ASignificant anti-blood stasis effectImprove liver indexOrganic active ingredientsBlood disorderScirpusin CSerum ige
The invention discloses application of a scirpusin component C in common burreed rhizome in synthesis of anti-blood stasis syndrome drugs. The invention first proves that the scirpusin C has an obvious anti-blood stasis drug effect, and can be used for preparing a medicine for treating the blood stasis syndrome. Pharmacological experiments prove that the scirpusin C is capable of obviously reducing the levels of thromboxane B2 (TXB2), fibrinogen (FIB), active plasminogen activator inhibitor (PAI-1) and endothelin 1 (ET-1) in serum of blood stasis model mice and improving the thymus index (TI),spleen index (SI) and hepatic index (HI) of the mice, and has high clinical application value and development prospects in the aspect of treating the blood stasis syndrome.
Owner:GUANGDONG PHARMA UNIV

Prophylactic or therapeutic agent for pulmonary fibrosis

Disclosed is a compound which has an inhibitory activity on plasminogen activator inhibitor-1 (PAI-1) and has a propanedioic acid structure represented by formula (1) [wherein R1 and R2 independently represent a hydrogen atom or a linear or branched alkyl group having 1 to 4 carbon atoms; R3 represents a cyclohexyl group or a phenyl group (provide that the phenyl group may be substituted by a substituent selected from a linear or branched alkyl group having 1 to 4 carbon atoms, a linear or branched alkoxy group having 1 to 4 carbon atoms, and a halogen atom); R4 represents a linear or branched alkyl group having 1 to 6 carbon atoms or a phenyl group (provide that the phenyl group may be substituted by a substituent selected from a linear or branched alkyl group having 1 to 4 carbon atoms, a linear or branched alkoxy group having 1 to 4 carbon atoms, and a halogen atom); and n represents an integer of 1 to 8]. The compound is useful as a prophylactic or therapeutic agent for pulmonary fibrosis.
Owner:SHIZUOKA KAFUEIN INDSSHIYO
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