Abstract: The present invention relates to peptide derivatives, wherein glutathione-like peptides are connected to benzoic acid derivatives, and a cosmetic composition comprising the same. The peptide derivatives according to the present invention have excellent tyrosinase inhibition and anti-oxidative activities to show excellent skin whitening effect, biocompatibility without skin stimulation, and stability during long-term storage. Therefore, they can be effectively used for a cosmetic composition for skin whitening.

Abstract: Methods and compositions for inhibition of platelet cell aggregation are described. In particular, compositions comprising cell permeant RGT peptides, such as RGT bound to a lipid moiety are provided. Compositions may be used in the treatment and prevention of clot related diseases such as stroke and myocardial infarction.

Abstract: The present invention concerns a peptide of the general formula (I): R1-(AA)nX1—X2—X3-Pro-X4—X5—X7-(AA)p-R2, capable of activating the synthesis of proteins of the family of aquaporins. The present invention also concerns a cosmetic, nutraceutical or pharmaceutical composition, comprising a peptide of general formula (I) as active principle. The invention also relates to the use of this new active principle in a cosmetic or nutraceutical composition, intended to improve the moisturizing and the barrier function of the epidermis and intended to stimulate cutaneous regeneration. The invention also relates to the use of this new active principle to realize a pharmaceutical composition, and in particular a dermatological composition, intended to regulate and/or stimulate the activity of the aquaporins and to thus treat the pathological dryness of the skin or mucosa.

Abstract: The present invention relates, in part, to agents for binding and/or inactivating native ghrelin. These agents include those that specifically bind and/or cleave octanoylated native ghrelin. Such agents include antibodies and enzymes. The agents also include those that can be used to generate antibodies that specifically hind and/or cleave octanoylated native ghrelin. Compositions that include the agents are also provided. Further provided are methods of producing and using the agents and compositions thereof. For instance, the agents and compositions can be used to reduce or eliminate the hunger response activity of octanoylated native ghrelin. Therefore, the agents, compositions and methods provided can be used to suppress appetite and/or treat obesity. In addition, the agents, compositions and methods can be used to treat any disease associated with or caused by ghrelin (e.g., Prader-Willi Syndrome).

Abstract: This invention relates to a conjugate molecule comprising at least one first portion (I) comprising a carrier sequence and at least one second portion (II) comprising at lest one antitumor drug molecule or a protease inhibitor molecule said conjugate molecule comprising D-enantiomeric amino acids in its portion (I). Furthermore, the invention relates to pharmaceutical compositions containing said conjugate molecule as well as to the use of said conjugate molecule for therapeutic treatment. Methods for improving cell permeability or water solubility are disclosed as well.

Abstract: This invention relates to agents capable of reducing the activity, amount or density of complement regulatory proteins (CRPs) on target cells. The invention also provides methods of identification of such agents, methods of making, and uses thereof.

Abstract: A novel method of treating and preventing viral infection is provided. In particular a method of blocking viral infection facilitated by a serine proteolytic (SP) activity is disclosed, which consists of administering to a subject suffering or about to suffer from viral infection a therapeutically effective amount of a compound having a serine protease inhibitory or serpin activity. Among compounds are ?1-antitrypsin (AAT), peptide derivatives from the carboxyterminal end of AAT, and man-made, synthetic compounds mimicking the action of such compounds. The preferred viral infections include retroviral infection such as human immunodeficiency virus (HIV) infection.

Abstract: A method of identifying a compound that modulates NCKX-mediated calcium ion exchange across a cell membrane, the method comprising the steps of providing an adherent cell, the cell membrane of which comprises a NCKX polypeptide or a functionally equivalent variant thereof, exposing the cell in suspension to a fluorescent calcium-sensitive dye, thereby causing intracellular uptake of the dye, settling the cell onto a solid support without allowing the cell to adhere to the solid support, exposing the cell to a test compound, exposing the cell to calcium and potassium ions, and measuring fluorescence from the intracellular calcium-sensitive dye after exposure of the cell to the test compound and the calcium and potassium ions, thereby to determine the rate and/or amount of calcium ion exchange across the cell membrane in the presence of the test compound.

Abstract: The invention relates to a novel organosilicon carrier system for biological agents that is produced via a simple, stable and reproducible preparation process that is capable of maintaining tertiary protein structure and biological activity of the proteins and/or other biological agents in the mixture, whereby the carrier system is obtainable by mixing one or more organosilicon compounds, selected from the group comprising organosilicon, sugar organosilicon, amino sugar organosilicon compounds, their derivatives, salts and/or the vesicles formed from them, with one or more biological agents, selected from the group comprising antigens, preantigens, antigen conjugates, antibodies, pre-antibodies, antibody conjugates, allergens, allergen extracts, nucleic acids, plasmids, proteins, peptides, pharmaceutical agents, immunologically active substances and/or cosmetics, in solution at a pH value between 7 and 8, preferably 7.

Abstract: The present invention relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, other than N-(phosphonomethyl)-glycine or N,N-bis(phosphonomethyl)-glycine. Also included is a composition including an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, and a cosmetically or pharmaceutically acceptable vehicle for topical or systemic administration to a mammalian subject, as well as a method of administering an effective amount of such a composition for alleviating or improving a condition, disorder, symptom or syndrome associated with at least one of a nervous, vascular, musculoskeletal or cutaneous system.

Abstract: Compounds having a diphenylmethane skeleton are superior in broad utility and stability, and are useful as a protecting reagent (anchor) of amino acid and/or peptide in the liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide(-CONHR)-type, and in organic synthetic reaction methods (particularly peptide liquid phase synthetic methods), and may be contained in a kit for peptide liquid phase synthesis.

Abstract: Lipopeptide compounds comprising a peptide having 2 to 100 amino acid residues, and having a lipophilic group attached to at least one terminus of the peptide or to at least one amino acid residue of the peptide, and salts and uses thereof. The lipophilic group may be attached to the N-terminus, C-terminus or both termini of the peptide. The lipophilic group may be attached to at least one interal amino acid residue (i.e., an amino acid residue that is not the N-terminus or the C-terminus amino acid residue of the peptide). The lipophilic group may be attached to either termini or both and at least one internal amino acid residue.

Abstract: Peptides comprising a cadherin cell adhesion recognition (CAR) sequence, and compositions comprising such peptides, are provided. Methods of using such peptides for modulating cadherin-mediated processes in a variety of therapeutic contexts are also provided. Methods are also provided for identifying compounds that are capable of modulating cadherin-mediated processes.

Abstract: The various embodiments herein provide a method for producing a carrier system for the encapsulation or entrapment of a bioactive agent. According to one embodiment herein, producing a carrier complex of a bioactive ingredient disposed within a carrier material, the method comprising the steps of: (a) providing a complexation zone supplied with an aqueous medium containing the carrier material; (b) simultaneously stirring and heating the aqueous medium; (c) adding the bioactive ingredient to the aqueous medium and maintaining the complexation zone under conditions of temperature effective to facilitate complexation of the bioactive ingredient by the carrier material; and (d) recovering from the complexation zone a carrier complex of the bioactive ingredient.

Abstract: This invention provides methods of inhibiting the onset or progression of a fibrotic disease (or pre-fibrotic pathology) in a mammal. The method involves administering oen or more peptides (e.g., class A amphipathic helical peptides, G* peptides, etc.) as described herein to a mammal in need thereof, in an amount effective to inhibit the onset and/or progression of the fibrotic disease (or pre-fibrotic condition) in the mammal.

Abstract: A cDNA molecule that encodes a protein designated Labyrinthin (Lab) isolated and its nucleotide sequence is determined. The protein, or peptides derived from the protein, are markers useful to define novel classes of cancers. Diagnostic assays for these cancers use antibodies to Lab or nucleotide probes that hybridize with the lab gene or a fragment therefrom. Vaccines useful either to prevent recurrence of cancers in subjects who test positive for Lab (or lab), or to prevent initial occurrence of cancer, use proteins or peptides derived from Lab. Expression of Lab via immunogenic assays is used to monitor effects of cancer treatments. Antisense molecules against lab are used in treatments. Sense molecules of lab are used to restore lost lab function in diseased normal cells, for example, gland cells.

Abstract: The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal N-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a ?-(methylamino)-thioester intermediate that spontaneously rearranges to form an amide bond. Furthermore, the invention relates to methods of converting N-methyl-thiazolidine to N-methyl-cysteine (SEQ ID NO: 1) of polypeptides and proteins. The invention also relates to methods of synthesizing peptide-thioester from peptide-acid fluoride.

Abstract: The present invention relates to new molecularly imprinted polymers which are suitable for the selective recognition of glutathione GSH and/or of an analog thereof, and in particular which are of use for the treatment of media comprising in particular a mixture of glutathione GSH, and/or of an analog thereof, with GSH adducts.

Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.

Abstract: The invention relates to a synthetic bifunctional non-antibody compound comprising one or more effector moieties and one or more binder moieties, wherein the effector moieties are operably linked to the binder moieties via a linker, the effector moieties are ligands to at least one pathogen pattern recognition receptor (PRR) and the binder moieties bind to a marker of a tumor cell.

Abstract: Disclosed herein are a materials such as a coating, an elastomer, an adhesive, a sealant, a textile finish, a wax, and a filler for such a material, wherein the material includes an enzyme such as an esterase (e.g., a lipolytic enzyme, a sulfuric ester hydrolase, an organophosphorus compound degradation enzyme), an enzyme that degrades a cell wall and/or a cell membrane component (e.g., a lysozyme, a lytic transgrycosylase, a peptidase), and/or a biocidal or biostatic peptide. Also disclosed herein are methods of decontaminating a surface comprising such a material from a chemical substrate of an enzyme such as a lipid or an organophosphorus compound, as well as reducing the growth of a microorganism on or within such a material.

Abstract: Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.

Abstract: A dechalcogenative method for the preparation of an allylic sulfide comprises contacting an activated chalcogenide of Formula (I) with a thiol of Formula (II) for a period of time sufficient to form an intermediate of Formula (III), and supplying sufficient activation energy to the intermediate of Formula (III), in a suitable solvent, preferably in the absence of a phosphine or other thiophile, to induce a [2,3]-sigmatropic rearrangement therein to form an allylic sulfide of Formula (IV), with concomitant loss of chalcogen Z, as set forth in the following reaction scheme, wherein X is an activating group selected from the group consisting of CN, S-pyridyl, S-heteroaryl, SO2-aryl, and SO3Y; Y is an alkali metal ion; Z is Se or S; R1, R2, R3, R4, and R5 are each independently H or a hydrocarbon moiety; and R is an organic moiety.

Abstract: Compositions comprising a tripeptide having the sequence XC1C2; wherein X is any amino acid such that XC1C2 is capable of binding a metal in a square planar orientation or square pyramidal orientation or both; and wherein C1 and C2 are the same or different; and wherein C1 and C2 individually are chosen from a cysteine and a cysteine-like nonnatural amino acid, as well as metal-XC1C2 complexes and methods for forming such complexes.

Abstract: A nanostructure composed of a plurality of peptides, each peptide containing at least one aromatic amino acid, whereby one or more of these peptides is end-capping modified, is disclosed. The nanostructure can take a tubular, fibrillar, planar or spherical shape, and can encapsulate, entrap or be coated by other materials. Methods of preparing the nanostructure, and devices and methods utilizing same are also disclosed.

Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.

Abstract: A molecular probe comprises two arsenic atoms and at least one cyanine based moiety. A method of producing a molecular probe includes providing a molecule having a first formula, treating the molecule with HgOAc, and subsequently transmetallizing with AsCl3. The As is liganded to ethanedithiol to produce a probe having a second formula. A method of labeling a peptide includes providing a peptide comprising a tag sequence and contacting the peptide with a biarsenical molecular probe. A complex is formed comprising the tag sequence and the molecular probe. A method of studying a peptide includes providing a mixture containing a peptide comprising a peptide tag sequence, adding a biarsenical probe to the mixture, and monitoring the fluorescence of the mixture.

Abstract: The present invention is directed to the use of the peptide compound Pyr-His-Pro-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pyr-His-Pro-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.

Abstract: A pharmaceutical or a foodstuff including as an active ingredient a peptide containing Tyr (Y), Phe (F), Trp (W), or His (H) and a hydrophobic amino acid adjacent thereto, or an analog thereof.

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

Abstract: The invention relates to carrier complexes and methods for delivering molecules to cells. The carrier complexes comprises a molecule and an aromatic cationic peptide in accordance with the invention. In one embodiment, the method for delivering a molecule to a cell comprises contacting the cell with a carrier complex. In another embodiment, the method for delivering a molecule to a cell comprises contacting the cell with a molecule and an aromatic cationic peptide.

Abstract: The present invention provides a peptide comprising amino acid sequences R I, F I and R I G C and containing 25 or fewer amino acid residues, and capable of transporting a functional molecule into a cell, and also into a nucleus, more efficiently than a previous PTD.

Abstract: The present invention provides polymeric linkers containing pyridyl disulfide moieties. Methods of making the polymeric linkers and methods of making conjugates using the same are also disclosed.

Abstract: The present invention relates to the use of compounds of the formula for treating obsessive compulsive neurosis.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: The present invention relates to the use of didepsipeptides of the general formula (I) and their salts in which the radicals have the meaning given in the description, and to new didepsipeptides and processes for their preparation.

Abstract: The present invention is directed towards an isomer, an enantiomer, a diastereoisomer, or a tautomer of a pyrrolidine compound represented by Formula I: in which the substituents R1, R1a, R2, R2a, R3, A and Q are defined herein; or a prodrug, or a salt thereof, and which bind to IAP BIR domains. In particular, the compounds are useful in treating proliferative disorders such as cancer.

Abstract: Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Subject of the present invention are new isotopic and isobaric tagged molecules, kits comprising them and methods of using them in mass spectrometry.

Abstract: This invention provides a composition having preventive and/or therapeutic effects on liver disease, which is highly effective, free of side effects, easily ingestible, and capable of long-term ingestion from the viewpoint of a cost and safety. This invention relates to a peptide having the amino acid sequence represented by the following formula: pyroGlu-(X)n-A, wherein X is the same or different and represents Gln or Asn; A represents Gln, Asn, Leu, Ile, or Val; and n is an integer from 0 to 2 or a salt thereof.

Abstract: The present invention is directed to the use of the peptide compound Pro-Leu-Gly-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pro-Leu-Gly-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.

Abstract: The present invention relates to IL-23 receptor antagonists and agonists. The use of IL-23 receptor antagonists in treating autoimmune and inflammatory disorders, as well as methods of identifying IL-23 receptor antagonists and agonists.

Abstract: The present invention relates to molecular probes of the formula (I) {L1-R1-L}n-A-CO—NH—R2-L2??(I) as defined herein that allow for the observation of the catalytic activity of a selected cathepsin in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.

Abstract: Substrates for thrombin and assays for determining the level of bioactive thrombin in a sample are disclosed, wherein the substrate has the general formula: A-X-Z-A? wherein one of either A or A? comprises a luminescent chelate and the other one of A or A? comprises a first partner of a binding pair, X forms a tri- or tetra-peptide, and Z comprises a linker.

Abstract: The present invention is directed to the use of the peptide compound Gly-Pro-Glu-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Gly-Pro-Glu-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.

Abstract: Disclosed are compositions and methods for inhibiting viral entry.

Abstract: One aspect of the present invention relates to compounds for delivering chemotherapeutic agents to cancerous cells to reduce discomfort and deleterious side effects associated with systemic administration of such agents. Another aspect of the invention relates to methods of treating a subject with cancer by administering a therapeutically effective amount of a chemotherapeutic agent that predominately targets cancerous cells over healthy cells. Additionally, one aspect of the present invention relates to methods of inhibiting the life-cycle of a cancerous cell, as well preparing a chemotherapeutic prodrug.

Abstract: The invention provides a method for radiofluorination of biological vectors such as peptides comprising reaction of a compound of formula (II): or a salt thereof with a source of [18F]-fluoride, to give a compound of formula (I): or a salt thereof.

Abstract: The present invention concerns compositions comprising and methods of identification and use of targeting peptides selective for cancer tissue, particularly prostate or ovarian cancer tissue. The method may comprise identifying endogenous mimeotopes of such peptides, such as GRP78, IL-11R? and hsp90. Antibodies against such targeting peptides or their mimeotopes may be used for detection, diagnosis and/or staging of prostate or ovarian cancer. In other embodiments, the compositions and methods concern a novel type of gene therapy vector, known as adeno-associated phage (AAP). AAP are of use for targeted delivery of therapeutic agents to particular tissues, organs or cell types, such as prostate or ovarian cancer. In still other embodiments, targeting peptides selective for low-grade lipomas may be used for detection, diagnosis and targeted delivery of therapeutic agents.