Abstract: The present invention provides compositions and methods useful for regulating fertilization and for use as a contraceptive based on the discovery herein of an oocyte specific protein, SAS1R (Sperm Acrosomal SLLP1 Receptor), which is a sperm protein receptor. Six SAS1R variants, including the full length SAS1R, were identified. mSLLP1 and SAS1R co-localized to oocytes and to acrosomes of acrosome-reacted sperm. Interactions between mSLLP1 and SAS1R were demonstrated by far-western analysis, in a yeast two-hybrid system under stringent selection conditions, and by immunoprecipitation of SAS1R by anti-mSLLP1 as well as the converse. Purified recombinant SAS1R was found to have protease activity, to inhibit fertilization in-vitro, and to induce an immune response in females.

Abstract: The invention discloses 5-lipoxygenase inhibitory product prepared from botanical sources. More specifically, the invention describes 5-lipoxygenase inhibitory extracts or bio-enriched extracts or fractions of Aphanamixis polystachya, methods of making 5-lipoxygenase inhibitory extract, and methods of treating and/or preventing disease conditions mediated by 5-lipoxygenase by using the said extract. The invention further discloses pharmaceutical or nutraceitical or dietary compositions containing therapeutically effective amounts of the extracts of Aphanamixis polystachya in combination with other known anti-inflammatory agents useful for oral, parenteral and topical administration.

Abstract: The present invention relates to anti-angiogenic polypeptides derived from the non catalytic C-terminal hemopexin-like domain of the metalloproteinase MMP-2. The invention also provides pharmaceutical compositions comprising said anti-angiogenic polypeptides and methods for using said polypeptide for treating angiogenic diseases, and in particular for treating cancer.

Abstract: The present invention relates to new pyrazolinone scavengers of free radicals, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Compositions including topical formulations comprising secreted products obtained from the culture medium of human umbilical cord stem cells and particular combinations of components therefrom are provided for treatment of various dermatological conditions, such as adverse consequences of aging, wrinkling, altered pigmentation, altered viscoelasticity, and altered thickness, among others. Methods for using the compositions and topical formulations for treating adverse or undesirable dermatological conditions are also provided, as well as preventing the appearance of undesirable dermatological conditions.

Abstract: The invention provides isolated nucleic acids molecules, designated 27875, 22025, 27420, 16319, 55092 and 10218 nucleic acid molecules. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing 27875, 22025, 27420, 16319, 55092 and 10218 nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a 27875, 22025, 27420, 16319, 55092 and 10218 gene has been introduced or disrupted. The invention still further provides isolated 27875, 22025, 27420, 17906, 16319, 55092 or 10218 proteins, fusion proteins, antigenic peptides and anti-27875, 22025, 27420, 17906, 16319, 55092 or 10218 antibodies. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: Certain embodiments disclosed herein relate to compositions, methods, devices, systems, and products regarding frozen particles. In certain embodiments, the frozen particles include materials at low temperatures. In certain embodiments, the frozen particles provide vehicles for delivery of particular agents. In certain embodiments, the frozen particles are administered to at least one biological tissue.

Abstract: What is described is a use of an antidepressant compound, preferably belonging to the class of selective serotonin reuptake inhibitors (SSRI), for regenerating the integumentary system and/or for stimulating the growth, the original trophism and/or original pigmentation of the corresponding cutaneous appendages, particularly body hair and/or head hair, in mammals. For this purpose, the antidepressant can be formulated in a cosmetic preparation, a pharmaceutical composition, a medical device, or in the form of a culture medium, alone or in combination with a further active ingredient such as a proteolytic enzyme and/or a vitamin.

Abstract: The invention is directed to methods of treating patients suffering from Peyronie's disease, methods of identifying patients suffering from Peyronie's disease and a computer program for identifying patients suffering from Peyronie's disease.

Abstract: The present invention relates to a combination of pharmaceutical compositions adapted for oral administration one of which comprises a pharmaceutically active ingredient being acid resistant, and the other of which comprises a pharmaceutically active ingredient being acid labile. Said combination is in the form of a kit of parts which is administered in such way as to use food intake to optimize absorption of both the acid labile and the acid resistant active ingredient. Consequently, the kit of parts of the present invention when administered according to the invention provides improved bioavailability of both the acid-resistant and acid-labile active ingredient.

Abstract: Multi-drug resistant superbugs are a persistent problem in modern health care. LysK is a staphylococcal bacteriophage endolysin from the phage K. It is a peptidoglycan hydrolase enzyme that can lyse many staphylococcal strains and thus is a potent antimicrobial against S. aureus, including MRSA. Lysostaphin is a bacteriocin secreted by S. simulans to kill S. aureus, and has been shown to also be a potent antimicrobial for many antibiotic resistant strains of S. aureus. This study describes optimal reaction conditions for the recombinant His-tagged LysK protein, compares its MIC and antimicrobial activity to lysostaphin and demonstrates synergy when the two are used in combination against the MRSA USA300.

Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The effect of the action of collagenase in treating lesions containing collagen or mixed fibrin clots (e.g., burns or ulcers) is improved by applying collagenase to the wound in combination with an organogel and a phosphatidylcholine, of which lecithin is a readily available source, particularly when the collagenase is first mixed and stored with that choline and an organic solvent and is subsequently mixed with a second individually stored formulation comprising a gel-forming agent and water, the two formulations individually having satisfactory shelf lives and the resultant mixture being applied to the lesion promptly after being formed.

Abstract: This invention relates to methods for treating or preventing an infarction by administering to a patient in need thereof a compound capable of suppressing the expression or activity of the von Willebrand Factor (VWF). Thus, the invention relates to the use of a pharmaceutically effective amount of a VWF inhibitor, such as ADAMTS13, for the preparation of a medicament for treating conditions known to involve infarction to reduce or eliminate the symptoms and effect of an infarction.

Abstract: The present invention relates to a method of treatment of an inflammatory disease, in particular sepsis, in particular sepsis caused by gram-positive bacteria, wherein the method comprises the step of administering to a subject in need thereof a sufficient amount of bacterial cell wall degrading enzymes. The present invention relates further to pharmaceutical compositions comprising bacterial cell wall degrading enzymes.

Abstract: The present invention relates to a disintegrin and metalloproteinase containing thrombospondin 1-like domains (ADAMTS) and in particular to a novel ADAMTS13 protease and to nucleic acids encoding ADAMTS13 proteases. The present invention encompasses both native and recombinant wild-type forms of ADAMTS13, as well as mutant and variant forms including fragments, some of which posses altered characteristics relative to the wild-type ADAMTS13. The present invention also relates to methods of using ADAMTS13, including for treatment of TTP. The present invention also relates to methods for screening for the presence of TTP. The present invention further relates to methods for developing anticoagulant drugs based upon ADAMTS13.

Abstract: The present invention relates to a disintegrin and metalloproteinase containing thrombospondin 1-like domains (ADAMTS) and in particular to a novel ADAMTS13 protease and to nucleic acids encoding ADAMTS13 proteases. The present invention encompasses both native and recombinant wild-type forms of ADAMTS13, as well as mutant and variant forms including fragments, some of which posses altered characteristics relative to the wild-type ADAMTS13. The present invention also relates to methods of using ADAMTS13, including for treatment of TTP. The present invention also relates to methods for screening for the presence of TTP. The present invention further relates to methods for developing anticoagulant drugs based upon ADAMTS13.

Abstract: Tissue engineering devices and methods are provided for the reconstruction, repair, augmentation, or replacement of a luminal organ or tissue structure involving the use of a biodegradable polymer matrix conforming to a portion of a laminarly arranged luminal organ, the processing of autologous, allogeneic or xenogeneic tissue comprising multiple cell populations to obtain a minced tissue composition, the seeding of the matrix with the composition, and the implanting of the seeded polymer matrix into a patient.

Abstract: The present invention features mammalian expression systems with improved production yields, and method of using these systems to produce desired proteins. In one embodiment, the expression systems of the present invention comprise genetically-engineered mammalian host cells cultured in a medium that contains an effective amount of heparin or heparin-like molecules. The presence of heparin or heparin-like molecules significantly increases protein production by the cultured cells. The present invention also features the use of constitutively-active components of FGFR-I-mediated signal transduction pathways to improve protein production by cultured mammalian cells. Co-expression of such a component with a protein of interest markedly increases the production yield of the protein of interest.

Abstract: The present inventors discovered for the first time that intestinal inflammation could be efficiently suppressed by suppressing the production or accumulation of chondroitin sulfate proteoglycans. Specifically, inflammation in the large intestine can be suppressed by using siRNA to suppress the expression of versican, which is one of the chondroitin sulfate proteoglycans. Compounds used as siRNA, such as nucleic acids, can be used as effective agents for suppressing intestinal inflammation. Furthermore, the above finding also suggests that such intestinal inflammation-suppressing agents can be found by screening for compounds that suppress the production or accumulation of chondroitin sulfate proteoglycans.

Abstract: A pharmaceutical composition is disclosed. In at least one embodiment, a pharmaceutical drug is linked via a peptide linker to an iron-binding agent, for example an iron-binding protein, with the iron-binding agent in turn being bound to an iron-containing magnetic particle. The peptide linker has a protease recognition sequence, i.e. it may be cleaved at said protease recognition sequence by a protease, thereby enabling the pharmaceutical drug to be released locally. The pharmaceutical composition is suitable for magnetic drug targeting.

Abstract: A composition for in vitro use as a culture medium or in vivo use as a pharmaceutical composition or a medical device, capable of accelerating the differentiation of stem cells into cells with a chondrocytic phenotype and of restoring the original trophism of chondrocytes, is described. The composition comprises, in combination, at least one proteolytic enzyme, at least one growth factor and at least one from a sugar, an amino acid, a vitamin factor, a vitamin, a nucleotide and a nucleoside, in a physiologically acceptable carrier or diluent. A method of differentiating stem cells in cells having a chondrocytic phenotype, the cells obtained by the method and their uses, for example in human or animal cell therapy, for example by CBMP (Cellular Based Medicinal products) are also described.

Abstract: Thrombin-conjugated nanoparticles, wherein said nanoparticles comprise one or more organic and/or inorganic compounds and process for preparing the same are provided. The thrombin-conjugated nanoparticles are suitable for use in the preparation of fibrin-based biological sealant.

Abstract: There is provided an anti-microbial composition comprising a cationic peptide and a glycineglycine endopeptidase. The composition has been found to be synergistic against bacteria, especially Gram positive bacteria such as Staphylococcus aureus MSSA or MRSA. In one embodiment the composition comprises ranalexin, dermaseptin, magainin or mixtures thereof together with lysostaphin. The composition is useful for treating surfaces, including a wound surface in a patient or surfaces of an object (e.g. surgical instrument) or room.

Abstract: The invention relates to the discovery that collagenase injections are effective in lyse the collagenous adhesions in the shoulder and treat the disorder, adhesive capsulitis. As such, the invention relates to methods of treating or preventing adhesive capsulitis, or frozen shoulder, in a patient in need of such treatment comprising injecting or otherwise delivering an effective amount of collagenase to the collagenous adhesions in the shoulder. The invention also relates to the use of collagenase in the manufacture of a medicament to treat adhesive capsulitis.

Abstract: The present invention relates to a skin cosmetic composition containing enzyme and amino acid. More particularly, the skin cosmetic composition according to the invention contains enzyme and amino acid, and thus safely improves stratum corneum thickening resulting from the progression of skin aging, improves skin drying occurring during keratin removal, and shows excellent skin moisturizing and whitening effects.

Abstract: The present invention relates to a disintegrin and metalloproteinase containing thrombospondin 1-like domains (ADAMTS) and in particular to a novel ADAMTS13 protease and to nucleic acids encoding ADAMTS13 proteases. The present invention encompasses both native and recombinant wild-type forms of ADAMTS13, as well as mutant and variant forms including fragments, some of which posses altered characteristics relative to the wild-type ADAMTS13. The present invention also relates to methods of using ADAMTS13, including for treatment of TTP. The present invention also relates to methods for screening for the presence of TTP. The present invention further relates to methods for developing anticoagulant drugs based upon ADAMTS13.

Abstract: The use of a collagenase containing formulation for degrading collagen within an occlusive atherosclerotic plaque in a chronic fibrotic occlusion, chronically occluded animal tube or cavity. A medical-related apparatus is provided comprising a medical-related device having provided thereto a therapeutic amount of a collagen degrading composition comprising a proteiolytic enzyme containing formulation A method is provided for treating chronically occluded animal tubes and cavities by administering a therapeutic effective amount of a proteolytic enzyme-containing formulation adjacent to an occluding atherosclerotic plaque, waiting for a pre-angioplasty waiting period, followed by crossing the plaque with an angioplasty guide wire.

Abstract: The invention relates to vWF cleaving entities having a molecular weight of 180 kD, 170 kD, 160 kD, 120 kD or 110 kD and an N-terminal amino acid sequence of AAGGILHLELLV, vWF cleaving complexes and methods for their production.

Abstract: Devices, systems and methods for compressing, cutting, incising, reconfiguring, remodeling, attaching, repositioning, supporting, dislocating or altering the composition of tissues or anatomical structures to alter their positional or force relationship to other tissues or anatomical structures. In some applications, the invention may be used to used to improve patency or fluid flow through a body lumen or cavity (e.g., to limit constriction of the urethra by an enlarged prostate gland).

Abstract: The invention provides methods for treating a an obstructed biological conduit that include administering to the conduit an agent that can degrade extracellular matrix of obstructing tissue. Particular methods include delivery of an enzyme or a mixture of several enzymes to the area or region of obstruction wherein the enzyme(s) have the capability to degrade extracellular matrix components within the obstruction thereby restoring the normal flow of transported fluid through the conduit. The invention also includes prophylactically dilating a section of conduit to minimize the risk of obstruction formation.

Abstract: Methods for treatment by collagenase injections are provided, which are effective in dissolving and lysing a collagenase septa network to treat carpal tunnel, plantar fasciitis and lateral epicondylitis conditions. The methods treat such conditions by injecting or otherwise delivering purified collagenase to the afflicted region of the patient, as well as use of collagenase for manufacture of a medicament for such conditions.

Abstract: The invention relates to compositions for debriding damaged skin comprising at least one enzymatic debriding agent and at least one antiseptic compound comprising heavy metal ions. The present invention further relates to kit and methods for topical debridement of damaged skin, particularly of burned skin.

Abstract: The present invention relates to compositions and products comprising at least one proteolytic enzyme adapted to promoting the restoration of original trophism of the integumentary apparatus, the original pigmentation and stimulating the growth thereof and, particularly, improving the viability of the pilifer follicles, even in scar tissue areas.

Abstract: Elucidation of the crystal structure of an ADAM10 substrate-recognition and proteinase-positioning module comprising the protein cysteine-rich and disintegrin domains, and detailed functional analysis revealed that an acidic pocket within the cysteine-rich domain forms a substrate-recognition site. The binding of this pocket to receptor/ligand complexes facilitates effective ligand cleavage, which is prevented when critical residues within the pocket are changed. This provides use of the surface pocket within the extracellular domain of ADAM10, and the corresponding structure in related proteases such as ADAM17, as a target for structure-based computational and high-throughput screens for small-molecule substrate-specific inhibitors or monoclonal antibodies that inhibit ADAM protease cleavage of ephrins and other ADAM10 or ADAM17 substrates.

Abstract: A class of novel agents that are able to modify nociceptive afferent function is provided. The agents may inhibit the release of neurotransmitters from discrete populations of neurones and thereby reduce or preferably prevent the transmission of afferent pain signals from peripheral to central pain fibers. They comprise a galactose-binding lectin linked to a derivative of a clostridial neurotoxin. The derivative of the clostridial neurotoxin comprises the L-chain, or a fragment thereof, which includes the active proteolytic enzyme domain of the light (L) chain, linked to a molecule or domain with membrane translocating activity. The agents may be used in or as pharmaceuticals for the treatment of pain, particular chronic pain.

Abstract: A pharmaceutical composition having thrombolytic, anti-inflammatory and cytoprotective properties is described. The composition contains active proteases attached to a gel or to a mixture of a gel with a water-soluble polymer, said attachment being achieved with the help of radiation, preferably with the help of gamma-radiation or a flow of accelerated electrons. As the proteases the composition contains proteases which are stable at a temperature of up to 70° C., preferably at 30-40° C., for instance such as subtilysine, trypsin, chemotrypsin, papain or streptokinase. The gel is preferably polyethylene glycol gel, dextran gel, or polyglycane gel, and the water-soluble polymer is polyethylene glycol, polyvinyl alcohol, dextran or polyglycane. The method of preparing said composition and its use are also disclosed. The composition has a broad range of application, and can be used in cardiology, nephrology, surgery, rheumatology, gynecology and gastroenterology.

Abstract: The present invention provides polymeric compositions, devices, and methods for repair of vascular injury, particularly endothelial injury and impaired vascular repair, such as from intracranial aneurysms and carotid atherosclerosis. The invention particularly provides polymers incorporating signaling factors useful for recruiting circulating vascular progenitor cells. The polymers can be used alone or as a coating for various devices for placement at sites of vascular injury to promote repair by the body's natural systems.

Abstract: The use of a collagenase containing formulation for degrading collagen within an occlusive atherosclerotic plaque in a chronic fibrotic occlusion, chronically occluded animal tube or cavity. A medical-related apparatus is provided comprising a medical-related device having provided thereto a therapeutic amount of a collagen degrading composition comprising a proteiolytic enzyme containing formulation. A method is provided for treating chronically occluded animal tubes and cavities by administering a therapeutic effective amount of a proteolytic enzyme-containing formulation adjacent to an occluding atherosclerotic plaque, waiting for a pre-angioplasty waiting period, followed by crossing the plaque with an angioplasty guide wire.

Abstract: The present invention concerns new compositions containing hyaluronic acid or the derivatives thereof in association with the proteolytic enzyme collagenase (and relative pharmaceutical formulations) for the preparation of a dressing for topical treatment of various kinds of wounds, burns of varying depth, pressure sores, vascular ulcers and diabetic foot ulcers as well as for the treatment of hypertrophic and keloid scars.

Abstract: Disclosed herein are methods of using extracellular matrix digesting enzymes and neurotoxins, such as a Clostridial neurotoxins, to treat various medical conditions, such as overactive bladder, benign prostatic hyperplasia, hyperhidrosis, and cholecystitis for example.

Abstract: Disclosed herein are methods of using extracellular matrix digesting enzymes and neurotoxins, such as a Clostridial neurotoxins, to treat various medical conditions, such as overactive bladder, benign prostatic hyperplasia, hyperhidrosis, for example.

Abstract: The present disclosure relates to methods, compositions and articles of manufacture useful for the treatment of Bacillus anthracis and B. cereus bacteria and spores, and related conditions. The disclosure further relates to methods and compositions for the identification of a phage associated lytic enzyme to rapidly and specifically detect and kill Bacillus anthracis and other bacteria. Related articles of manufacture, methods of degrading spores and methods of treatment of infections or bacteria populations of, or subjects exposed to or at risk for exposure to, Bacillus anthracis are also provided.

Abstract: The object of the present invention is to increase PHEX activity to improve the osteogenic process in a mammal where this process has been diminished due to pathology or a condition that require osteogenesis. Osteocalcin is an endogenous inhibitor of the PHEX activity. Therefore, the identification of a substance capable of potentiating PHEX activity by preventing the inhibitory action of endogenous inhibitors will improve osteogenesis. Since PHEX is generally associated with the growth plane of bone or teeth and the absence of osteocalcin is associated with increased bone mass, potentiation of PHEX activity can promote bone growth. Increased PHEX activity can also be obtained by administration of the enzyme itself.

Abstract: The invention relates to a slimming cosmetic composition comprising, by way of an active agent, at least one inhibitor of metalloproteinases ?2 and/or ?9 or a plant extract containing said metalloproteinase inhibitor. The invention also relates to the use of an inhibitor of metalloproteinases ?2 and/or ?9 or a plant extract containing said inhibitor in a slimming cosmetic product. The invention further relates to the cosmetic use of an inhibitor of metalloproteinases ?2 and/or ?9 or a plant extract containing said inhibitor as an agent that prevents adipocyte differentiation for the preparation of a slimming composition.

Abstract: The present invention provides a method of using locally administered collagenase as a non-invasive means of enhancing cell release from the cartilage or fibrocartilage tissues adjacent to a disease or injury site. The subsequent migration of cells from these tissues into the lesion or wound, followed by deposition of the appropriate extracellular matrix, results in closure of the lesion or fusion of a tissue gap.

Abstract: The present invention provides a polymerizable antimicrobial composition and a method for using the same. The polymerizable antimicrobial composition of the invention comprises an antimicrobial compound, a linker, and a polymerizable function group.

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract: Frozen and lyophilized compositions for a metalloproteinase fibrinolytic agent (fibrolase or NAT), a method for preparing the lyophilized composition, and a kit and method for reconstituting the lyophilized composition are described herein.