Abstract: New Lactococcus lactis strains, NRRL B-50571 and NRRL B-50572, and a bacterial preparation containing the same, have the ability to produce bioactive peptides that reduce blood pressure, lower LDL-cholesterol (bad cholesterol) and present antioxidant properties for better cardiovascular health. These biologically active peptides may be produced within the food for the production of a food product, such as a functional food, or they may be produced from protein sources and subsequently added to a food as part of the formulation or as part of a food supplement or a pharmaceutical preparation.

Abstract: The invention is directed to an anti ageing skin care composition, more in particular a cosmetic anti aging skin care composition. The anti ageing skin care composition of the invention comprise, in a physiologically acceptable medium, (i) at least one peptide from Laminin-1 that is able to promote synthesis of Laminin-5; (ii) at least one peptide capable of at least partially inhibiting neuronal exocytosis; and (iii) at least one tripeptide producing a rapid and strong stimulation of collagen synthesis. The compositions of the present invention are effective in reducing existing wrinkles and/or preventing the formation of new wrinkles.

Abstract: The invention refers to multibasic, N-terminally modified tetrapeptide mimetics with a C-terminal P1-arginine mimetic, methods for their production and use for therapy and prophylaxis of diseases, caused by bacterial pathogens or viruses, as well as for therapy and prophylaxis of diabetes, arteriosclerosis, cancer, Alzheimer's or the onset of obesity, as well as the use of these compounds as inhibitors of the proprotein convertases which cleave behind basic P1 residues, especially for inhibition of the protease furin.

Abstract: Methods are described and related devices, compositions, and systems, in which a caged compound is administered to a biological environment, the caged compound being caged with a long wavelength absorber, the long wavelength being a wavelength greater than or equal to 750 nm; and irradiating the biological environment to excite the long wavelength absorber with light at a wavelength in a range from 900-1100 nm, thus decaging the compound.

Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of ca

Abstract: Novel peptidomimetics exhibiting affinity for opioid receptors, possessing general formula show on FIG. 1, for gastrointestinal or peripheral administration in the form of a pill, infusion, injection or implant in the treatment of peripheral opioids side effects, particularly constipation or/and respiratory depression.

Abstract: This invention pertains to the discovery that pentagastrin, when administered in conjunction with a proton pump inhibitor (PPI) is synergistic with the PPI and significantly increases the efficacy of the PPI in reducing/mitigating excess gastric acid secretion.

Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.

Abstract: The present invention provides novel peptides that inhibit and/or reduce the opening of mammalian tight junctions, i.e. peptide tight junction antagonists. The present invention also provides methods for the treatment of excessive or undesirable permeability of a tissue by administering to a subject suffering from such a condition a composition comprising a peptide tight junction antagonist of the invention.

Abstract: The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).

Abstract: The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.

Abstract: The present invention relates to novel Motoneuronotrophic Factors (MNTF) peptides and analogs thereof, including compositions capable of promoting the growth and viability of neurons. MNTF peptides between two and six amino acids in length are provided, as well as analogs of these MNTF peptides that are modified by covalent attachment to another moiety. Other embodiments are described herein.

Abstract: The disclosure relates to methods for treating a subject suffering from a burn injury or associated complications by administering to the subject an effective amount of an aromatic-cationic peptide. For example, a burn injury may be associated with distant pathophysiological effects, such as hypermetabolism, skeletal muscle dysfunction, and organ damage. The disclosure also relates to methods for protecting a subject from a burn injury by administering an effective amount of an aromatic-cationic peptide to a subject at risk of a burn injury.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: Patients inflicted with various clustering chronic diseases require treatment with multiple drugs having distinct mechanisms of action. Accordingly, patients with multiple conditions suffer from cumulative side effects of multiple drugs as well as drug-drug interactions. Embodiments, agents, compounds or drugs of the present invention, such as sesquiterpenes, e.g., Zerumbone, replace an equal or larger number of approved drugs during patient treatment. Examples of disorders prevented or ameliorated by administration of the formulations of this invention include but are not limited to inflammatory diseases that may be, oncological, genetic, ischemic, infectious, neurological, hematological, ophthalmological, rheumatoid, orthopedic, neurological, hematological, kidney, vascular, dermatological, gynecological, or obstetric.

Abstract: The present disclosure relates to nutritional compositions comprising a protein equivalent source, wherein 20% to 80% of the protein equivalent source includes a peptide component comprising SEQ ID NO 4, SEQ ID NO 13, SEQ ID NO 17, SEQ ID NO 21, SEQ ID NO 24, SEQ ID NO 30, SEQ ID NO 31, SEQ ID NO 32, SEQ ID NO 51, SEQ ID NO 57, SEQ ID NO 60, and SEQ ID NO 63, and 20% to 80% of the protein equivalent source comprises an intact protein, a partially hydrolyzed protein, or combinations thereof. The disclosure further relates to methods of reducing the inflammatory response and/or production of proinflammatory cytokines, i.e. Interleukin-17, by providing said nutritional compositions to a target subject.

Abstract: The present disclosure provides a method for suppressing a proinflammatory response by administering a composition comprising peptides selected from a casein hydrolysate. Such a composition may reduce the levels of proinflammatory cytokines and may be a treatment for inflammatory disease, especially type 1 diabetes. Preferably, the hydrolysate consists of peptides with a molecular weight of more than 500 Da.

Abstract: The present disclosure relates to nutritional compositions including a protein equivalent source that includes a peptide component comprising selected peptides. The protein equivalent source may further include intact protein, hydrolyzed protein, including partially hydrolyzed protein, or combinations thereof. The disclosure further relates to methods of promoting healthy body weight in a target subject by stimulating adiponectin levels by providing the nutritional compositions disclosed herein to a target subject, which includes a pediatric subject.

Abstract: The present disclosure provides a method for reducing the risk of autoimmune disease by administering a composition comprising peptides selected from a casein hydrolysate. Such a composition, may reduce the symptoms of autoimmune disease and may be a treatment for autoimmune disease, especially type 1 diabetes. Preferably, the hydrolysate consists of peptides with a molecular weight of more than 500 Da.

Abstract: The disclosure provides for one or more peptoids, methods of manufacture thereof, and methods of use thereof, including the use of one more peptoids in neutralizing the anticoagulant activity of heparin.

Abstract: The invention provides ultra-small peptide inhibitors that are capable of preventing amyloid formation/amyloidosis.

Abstract: The disclosure provides for one or more peptoids, methods of manufacture thereof, and methods of use thereof, including the use of one more peptoids in neutralizing the anticoagulant activity of heparin.

Abstract: A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy g

Abstract: The present invention describes new compounds (e.g.

Abstract: Apoptotic processes induced by infection of, or injury to, fetal and placental tissues have been implicated in preterm delivery. Thus, modulation of apoptotis constitutes a strategy for improving pregnancy outcome in women with intrauterine infections. Caspase inhibitors, including the pancaspase inhibitor Z-VAD-FMK, can be used to prevent apoptosis and, thus, prevent preterm delivery. Accordingly, compositions and methods comprising caspase inhibitors for prevention of preterm delivery are provided.

Abstract: The present invention relates to a stabilized vitamin C derivative with a peptide molecule linked to vitamin C or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a composition containing the same.

Abstract: A method of treatment is disclosed, comprising administering a composition of Cyclodextrin and one or more of a natural molecule or fragment thereof in at least one carrier to a patient in need of treatment, wherein the natural molecule is non-acetylated, non-Esterified, and non-fatty acid attached.

Abstract: The invention is directed to the cosmetic use of tetrapeptides according to formula (I) R1-Val-Leu-Leu-Lys-R2 (I) wherein R1 is linked to the NH2-terminal group of the peptide and is chosen from the group consisting of —H, a linear saturated or unsaturated or branched saturated or unsaturated acyl group having 1 to 24 carbon atoms, which may be functionalized by a —OH, —SH, —COOH or —CONH2 group wherein R2 is the terminal carboxylic group of the peptide either as —COOR3 or —CO—NH2, and wherein R3 is chosen from the group consisting of —H, a linear saturated or unsaturated or branched saturated or unsaturated alkyl group having 1 to 24 carbon atoms, which may be functionalized by a —OH, —SH, —COOH or —CONH2 group. The invention is also directed to the respective tetrapeptides and cosmetic compositions containing these.

Abstract: There is provided a lipid peptide that is capable of forming a hydrogel with an extremely small amount thereof over a liquid property range from acidic to alkaline, and a hydrogel having high environmental suitability, biocompatibility and biodegradability. A lipid peptide represented by Formula (1): where R1 represents an aliphatic group having 9 to 23 carbon atoms; R2, R3, R4 and R5 independently represent a hydrogen atom, an alkyl group having 1 to 7 carbon atom(s) which optionally has a branched chain having 1 to 3 carbon atom(s), a phenylmethyl group, a phenylethyl group or a —(CH2)n—X group, and at least one of R2, R3, R4 and R5 represents a —(CH2)n—X group; n represents the number of 1 to 4; X represents a guanidino group, a —CONH2 group or a 5-membered ring, a 6-membered ring or a fused heterocyclic ring composed of a 5-membered ring and a 6-membered ring which optionally have 1 to 3 nitrogen atom(s); and m represents 1 or 2, and a hydrogel comprising the lipid peptide.

Abstract: The invention relates to peptide derivatives of general formula (I): R1-AA1-AA2-R3-AA4-R2??(I) their stereoisomers, mixtures thereof, and their cosmetically or pharmaceutically acceptable salts, a method for obtaining them, cosmetic or pharmaceutical compositions containing them and their use for the treatment, care and/or cleansing of those conditions, disorders and/or pathologies of the skin, mucosae, scalp and/or nails resulting from microorganism proliferation or being at risk of microorganism proliferation.

Abstract: Disclosed is a general methodology to create nanofibers of therapeutic molecules that have a dual role, as both the delivery vehicle and the drug itself. It is shown that with proper molecular design, the integration of enzymatic reaction and self-assembly provides a powerful method to create molecular hydrogels of clinically-used therapeutics without compromising their bioactivities. In addition, the results disclosed herein demonstrate enzyme-instructed self-assembly as a facile strategy for generating the supramolecular hydrogels of molecules that inherently have poor solubility in water. For example, by covalently connecting paclitaxel with a motif that is prone to self-assemble, a hydrogel of paclitaxel can be formed without compromising the activity of the paclitaxel.

Abstract: Methods for treating cutaneous inflammation, are described. Also described is a method for inhibiting the mucous release into airways of a patient, a method for blocking IgE activation of an immune cell, a method for stabilizing the cell membrane of an immune cell, thereby preventing their further involvement in the increased inflammatory response to an IgE antigen challenge, and a method for inhibiting the migration of T-cells. Such methods involve administering to said patient a therapeutically effective amount of a peptide having the formula f-Met-Leu-X, wherein X is selected from the group consisting of Tyr, Tyr-Phe, Phe-Phe and Phe-Tyr.

Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

Abstract: Provided herein is technology relating to theranostic agents and particularly, but not exclusively, to compositions comprising cell-specific theranostic agents and associated methods and systems for using the cell-specific theranostic agents to treat subjects.

Abstract: Potent compounds having combined antioxidant, anti-inflammatory, anti-radiation and metal chelating properties are described. Short peptides having these properties, and methods and uses of such short peptides in clinical and cosmetic applications are described.

Abstract: The present invention relates to the use of a composition comprising at least one cell membrane fraction or parts thereof, for the reduction of lipolytic activity and/or to retard fat digestion, suppress appetite, body weight and/or lower blood lipids. The invention also relates to the use of said hydrophobic peptide in a pharmaceutical as well as a food composition and methods of treating a mammal with said composition.

Abstract: Sparingly water-soluble agents can be formulated as cyclodextrin complexes, however, these water-soluble drug-cyclodextrin complexes dissociate when the complex is administered into patients. The dilution of the complex in the patient leads to the drug being released from the complex, so the drug is not effectively targeted. In contrast, drugs encapsulated in the aqueous core of a lipid vesicles are not released when the liposome is diluted in blood. This invention describes compositions and methods whereby cyclodextrin or polyanionic beta-cyclodextrin drug-complexes are mixed with a preformed liposome containing the amine salts of an acidic compound. This results in the drug cyclodextrin complex being transferred into the liposome where it is stably retained. The liposome-encapsulated drug can then be injected into a patient.

Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).

Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).

Abstract: The present invention relates to a neurotrophic peptide having an amino acid sequence of VGDGGLFEKKL (SEQ ID NO:1) and alternatively comprising an adamantyl group at the C- and/or N-terminal end. The neurotrophic peptide can rescue cognition, correct impairments in neural cell proliferation and synaptic plasticity, and thus address the cognitive defects associated with Down syndrome.

Abstract: The present invention relates to a neurotrophic peptide having an amino acid sequence of VGDGGLFEKKL (SEQ ID NO: 1) and alternatively comprising an adamantyl group at the C-and/or N-terminal end. The neurotrophic peptide can rescue cognition, correct impairments in neural cell proliferation and synaptic plasticity, and thus address the cognitive defects associated with Alzheimer's disease.

Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.

Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Abstract: The invention described herein relates to methods of treating emphysema and COPD with a GHK tripeptide. The invention further relates to methods of determining the state of the lungs using biomarkers described herein.

Abstract: The present invention relates to a nanoparticle having a linker connected to a long alkane or alkene chain, and a method for preparing the nanoparticle. The alkyl chain of C10-30 introduced with a ligand of the present invention can be coated on a hydrophobic nanoparticle through a noncovalent bond, enabling easy introduction of various ligands to the nanoparticle, and the nanoparticle having various functional groups prepared using the method can be applied to fluorescent detection, MRI, raman spectroscopy, optical detection, PET, SPECT, or gamma image device, and the ligand of the visualization agents can be modified to be used for new vessels detection, cancer cell detection, immunocyte detection, hepatocyte detection, cell death detection, and gene detection.

Abstract: Provided herein are compositions and related methods useful for prevention or mitigation of ionizing radiation-induced esophagitis. The compositions comprise compounds comprising a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent or mitigate esophageal damage caused by radiation.

Abstract: The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs 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 invention proposes the combination of reduced glutathione in a liposome (liposomal reduced glutathione) with a specified concentration of reduced glutathione within the liposome for the oral administration of a therapeutically effective amount to ameliorate the progression of vascular disease, including atherosclerosis, diabetes, hypertension, narrowing of arteries leading to decreased blood flow, ischemic events, and the formation of blood clots, abnormal platelet aggregation, and thrombotic events, by reducing the amount and effect of oxidized cholesterol, oxidized HDL and oxidized LDL. The invention also proposes combining liposomal encapsulated glutathione with ACE inhibitors in order to improve the effect of lowering not only cholesterol but also the oxidized cholesterol as well as oxidized HDL and oxidized LDL. The invention also proposes combining liposomal encapsulated glutathione with lisinopril in particular.

Abstract: Methods are provided for selecting a new therapeutic indication for at least one first pharmaceutical comprising the steps of: generating a drug-side effect (SE) association for said at least one first pharmaceutical; generating a disease-side effect (SE) association for at least one disease or disorder and at least one second pharmaceutical intended for treatment of said at least one disease or disorder; determining an association strength between the drug-side effect (SE) association and the disease-side effect (SE) association; selecting said at least one disease or disorder as a new therapeutic indication for said at least one first pharmaceutical if said at least one first pharmaceutical induces at least one side effect which is the same as at least one side effect induced by at least one second pharmaceutical intended for treatment of said at least one disease or disorder.

Abstract: The present invention provides peptide-based peroxidase inhibitors having the formula AA1-AA2-AA3, wherein AA1 is a positively charged, negatively charged or neutral amino acid, AA2 is a redox active amino acid, and AA3 is an amino acid possessing a reducing potential such that AA3 is capable of undergoing a redox reaction with a radical of amino acid AA2 or a retro or retro-inverso analog thereof. The result of such a combination is a highly effective inhibitor of peroxidase activity that has potent anti-inflammatory properties in widely diverse models of vascular disease and injury. Exemplary tripeptides effectively inhibit peroxidase mediated LDL oxidation, increase vasodilation in SCD mice, inhibit eosinophil infiltration and collagen deposition in asthma mice, inhibit acute lung injury, and decrease ischemic injury of the heart.