Abstract: The purpose of the present invention is to provide a cross-linked peptide containing a novel non-peptide cross-linked structure, and a method for synthesizing the same. A cross-linked peptide having a novel non-peptide cross-linked structure, a useful intermediate for synthesizing the cross-linked peptide, and a method for synthesizing the novel cross-linked peptide and the intermediate are provided. The cross-linked peptide is characterized by having an —NR— bond in the cross-linked structure. By using the method for synthesizing the cross-linked peptide, a cross-link can be freely designed and an change can be freely made to a cross-link.

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 invention provides small molecule mimics of the Smac peptide that are dimers or dimer-like compounds having two binding domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

Abstract: The invention provides an agent comprising an amino acid sequence for use in a method of diagnosis of a synucleinopathic disease.

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: Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention generally relates to methods and compositions for preventing or treating axonal and/or neuronal degeneration in a subject by administering a composition comprising a peptide that comprises the amino acid sequence Arginine-Glycine-Aspartate (RGD).

Abstract: The present invention is an inhibitor of the trypsin-like ?2/?2i sites of the proteasome. The inhibitor is characterized as being a peptide-based epoxyketone or vinyl sulfone that contains an arginine or 4-aminomethylene-L-phenylalanine at the C-terminus (i.e., at the P1 position). Methods for using the inhibitor to inhibit the activity of the ?2/?2i site of a proteasome and treat a proteasome-mediated disease or condition are also described.

Abstract: A topical composition for application to aging skin, comprising an effective amount of S-acyl glutathione derivative of formula (I) wherein R1 consists of an unsaturated or saturated C16 group and R2 is a hydrogen, aliphatic or aromatic acyl group; and a dermatologically acceptable carrier. Preferred compositions comprise about 1.0% to about 3.0% by weight of S-palmitoyl glutathione.

Abstract: Compositions that include vanadium or vanadyl chelated to an amino acid are disclosed, particularly vanadium or vanadyl chelated to creatine, arginine, citrulline, taurine, phenylalanine, glutamine, glutathione, leucine, or combinations thereof. In addition, compositions that included blended forms of such chelates and/or vanadyl sulfate and one or more unbound amino acids. Still further, the compositions disclosed may further include one or more additional proteins, amino acids, vitamins, minerals, or combinations thereof, which impart an additional nutritional and/or therapeutic benefit to the composition.

Abstract: The present invention relates to peptides derived from human HMG-CoA reductase of general formula (I): R1-(AA)n-X1-Gly-Lys-X2-(AA)p-R2, And of sequence SEQ ID No. 1 to SEQ ID No. 10. The present invention also relates to a cosmetic or pharmaceutical composition comprising at least one peptide of general formula (I), in a physiologically suitable medium. The present invention further relates to the use of this novel peptide as an active principle that activates human HMG-CoA reductase in a cosmetic composition intended to strengthen the barrier function of the skin and to stimulate epidermal differentiation. The invention further applies to a cosmetic treatment method intended to prevent and/or combat the external stresses and signs of cutaneous aging.

Abstract: The present invention relates to compounds of the formula (I) and in particular medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.

Abstract: The present invention provides a metastin derivative represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition containing it. The metastin derivative or a salt thereof is superior in blood stability, and has a cancer metastasis suppressive action or cancer growth suppressive action.

Abstract: The present invention relates to the use of a compound of the following formula (I), as an enzyme substrate for the detection of a peptidase activity or as a pH indicator: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or else V is N or N+R and U is CZ6; R is H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3, Z4 and Z5 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.

Abstract: The invention relates to peptides comprising part or all of a conserved element within a Center-of-Tree (COT) sequence derived from a family of polypeptides encoded by naturally occurring variants of HIV. The invention also relates to immunogenic compositions and vaccines comprising said peptides. The invention also relates to methods for the identification of HIV controller patients based on the detection of the T cells of the patient to mount a cytotoxic T cell response against said peptides and to methods for the identification of immunogenic peptides within a family of variant polypeptides.

Abstract: The present invention relates to a casein hydrolysate containing free amino acids and in vivo indigestible peptides having minimally suppressed in vivo enzymatic digestibility, and expected to express functions, such as hypotensive effect, in living organism, and to a method for preparing such a hydrolysate, and use thereof. The casein hydrolysate of the present invention contains free amino acids and peptides, such as in vivo indigestible peptides including Xaa-Pro and Xaa-Pro-Pro, obtained by hydrolyzing animal milk casein to have an average chain length of not longer than 2.1 in terms of the number of amino acid residues, and has ACE inhibitory activity or hypotensive effect.

Abstract: This invention relates to peptides activating dermatopontin in the skin. This invention also relates to a cosmetic composition including a dermatopontin-activating peptide, in a physiologically suitable medium. The invention also relates to the use of said composition to increase the expression of proteins of the extracellular matrix and to prevent the degradation of collagen and elastic fibers by UV radiation. The invention finally relates to cosmetic care methods intended to prevent and/or treat cutaneous signs of aging and photoaging, and in particular wrinkles, sagging, and loss of volume and elasticity of the skin.

Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

Abstract: A delivery system. The delivery system includes a carrier or an active compound and a glutathione or a glutathione derivative grafted thereon. The invention also provides a compound including a moiety comprising a vitamin E derivative or a phospholipid derivative, a polyethylene glycol (PEG) or a polyethylene glycol derivative bonded thereto, and a glutathione (GSH) or a glutathione derivative bonded to the polyethylene glycol or the polyethylene glycol derivative.

Abstract: The present application relates to an affinity material useful in antibody purification.

Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula I are presented: wherein Q is a portion of a polymethine bridge: Also included are bioconjugates of the compounds of Formula I, methods of labeling biomolecules with the compounds, and methods of imaging.

Abstract: The invention provides a peptide comprising or consisting of SEQ ID NO: 1 and variants thereof, particularly comprising of consisting of the sequence FTY, nucleic acids encoding said peptides and pharmaceutical and nutraceutical compositions comprising said peptide(s) and/or nucleic acids. Also provided is the use of such a peptide in therapy and in vitro methods of ACE-inhibition.

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 invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Disclosed are peptides for augmenting the expression of BDNF (brain-derived neurotrophic factor) and a pharmaceutical composition for the prevention and treatment of Alzheimer's disease or Parkinson's disease, comprising the same. The peptides can induce the expression of BDNF in dopamine-reactive human cells, pass easily through the blood-brain barrier thanks to their low molecular weights and are almost free of cytotoxicity. Thus, they are useful in the prevention and treatment of neuropathies such as Alzheimer's disease or Parkinson's disease.

Abstract: The invention discloses processes for preparing compounds comprising an ?-amino acid motif. The compounds are useful in e.g. the chemical ligation of peptides.

Abstract: The invention relates generally to peptides comprising one or more non-natural amino acids residues and their use in cosmetic and personal care compositions.

Abstract: The present invention provides peptides and peptide conjugates for treating inflammatory bowel diseases, including ulcerative colitis and Crohn's disease. The peptides are derived from annexin-1, can be acetylated or conjugated to fatty acids, may be linear or cyclic, and may comprise D amino acids. Pharmaceutical compositions and methods of use are also disclosed.

Abstract: Soothing cosmetic or pharmaceutical composition that includes at least one peptide as an active principle that activates human HMG-CoA reductase of general formula (I): R1-(AA)n-X1-Gly-Lys-X2-(AA)p-R2 and is chosen from among sequences SEQ ID NO: 1 to SEQ ID NO: 10, in a physiologically suitable medium is described. This novel peptide is designed to act as a soothing active principle capable of providing a solution to skin sensitivity in a cosmetic composition. The invention further applies to a cosmetic treatment method intended to combat skin irritations.

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 invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid of the formula H2NCHRCOOH, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.

Abstract: The present invention relates to depigmenting, lightening and/or whitening peptidic compounds of general formula (I) R1—X1—X2-Asp-Cys-Arg-X3—X4-(AA)p-R2. In addition, the present invention relates to, on the one hand, a cosmetic or pharmaceutical composition comprising at least one peptide of general formula (I), in a cosmetically or dermatologically acceptable medium and, on the other hand, its utilization to depigment, lighten and/or whiten the skin and prevent or treat hyperpigmentation blemishes as well as cutaneous signs due to photo-aging. Lastly, the invention applies to a cosmetic treatment method utilizing said peptidic compounds.

Abstract: The present invention relates to reagents and methods for [18F]-fluorination of biomolecules, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET).

Abstract: The present invention relates to peptidic compounds of general formula (I): R1—X1—X2-Asp-Cys-Arg-X3—X4-(AA)p-R2. In addition, the present invention relates to, on the one hand, a cosmetic or pharmaceutical composition comprising at least one peptide of general formula (I), in a cosmetically or pharmaceutically acceptable medium and, on the other hand, its utilization to prevent or treat the cutaneous signs of aging and photo-aging and to protect the skin from aggressions due to UV radiation. Lastly, the invention applies to a cosmetic treatment process intended to prevent and/or combat the cutaneous signs of aging and photo aging.

Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

Abstract: Antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, tubulysin analogs, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers.

Abstract: A microreactor for preparing a radiolabeled complex or a biomolecule conjugate comprises a microchannel for fluid flow, where the microchannel comprises a mixing portion comprising one or more passive mixing elements, and a reservoir for incubating a mixed fluid. The reservoir is in fluid communication with the microchannel and is disposed downstream of the mixing portion. A method of preparing a radiolabeled complex includes flowing a radiometal solution comprising a metallic radionuclide through a downstream mixing portion of a microchannel, where the downstream mixing portion includes one or more passive mixing elements, and flowing a ligand solution comprising a bifunctional chelator through the downstream mixing portion. The ligand solution and the radiometal solution are passively mixed while in the downstream mixing portion to initiate a chelation reaction between the metallic radionuclide and the bifunctional chelator. The chelation reaction is completed to form a radiolabeled complex.

Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the following formula (for convenience, collectively referred to herein as “PVA compounds”), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.

Abstract: The present invention provides methods and materials for use in increasing HSP20 activation in a biological system, for example by increasing phosphorylation of Ser16 of HSP20. In one aspect, the invention provides a method for increasing HSP20 activation in a biological system, comprising contacting the system with an antagonist capable of inhibiting PDE4 binding to HSP20, the antagonist comprising or consisting essentially of a fragment of PDE4 or an analogue thereof. In a further aspect the invention provides a method of screening for an agent able to increase activation of HSP20. A preferred antagonist has a C-terminal lysine residue.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Abstract: The invention relates to an antigenic structure that contains a tryptophan epitope, characterised in that said structure is made up of a tryptophan pattern W or a peptide of 3 or 4 amino acids comprising a pattern W, coupled with glutaraldehyde. The invention can he used for screening trypanosomiasis in humans or animals.

Abstract: The present invention provides a pharmaceutical or a food that comprises, as an active ingredient, at least one peptide selected from the group consisting of Val-Tyr-Leu-Pro-Arg, Tyr-Leu-Pro-Arg, and Leu-Pro-Arg, or an analog thereof.

Abstract: A composition useful as a PET and/or fluorescence imaging probe a compound a compound of Formula I, including salts, hydrates and solvates thereof: wherein R1-R7 may be independently selected from hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, X is selected from the group consisting of C and N; and A is selected of hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, alkyl, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, including phenyl and aminophenyl, and heteroaryl.

Abstract: The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.

Abstract: There is provided a hydrogelator 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 hydrogelator comprising a lipid peptide represented by Formula (1): (where R1 represents an aliphatic group having 9 to 21 carbon atoms; R2, R3 and R4 independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atom(s) which may have a branched chain having 1 or 2 carbon atom(s), a phenylmethyl group or a —(CH2)n—X group, and at least one of R2, R3 and R4 represents a —(CH2)n—X group; n represents the number of 1 to 4; X represents an amino group, 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 may have 1 to 3 nitrogen atom(s)) or a salt thereof, and a hydrogel comprising the hydrogelator.

Abstract: Provided herein are methods for using mitochondria-targeted electron scavengers as anti-inflammatory agents. The mitochondria-targeted electron scavenger comprises a free radical-scavenging group covalently linked to a mitochondria-targeting group derived from a hemigramicidin moiety. The mitochondria-targeted electron scavenger can be used to treat medical conditions associated with acute or chronic inflammation.

Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.

Abstract: In one or a plurality of embodiments, there is provided a target molecule of amylospheroid, which is expressed in mature neurons and to which the amylospheroid binds to induce death of cells. Further, in one or a plurality of embodiments, there is provided a method and a substance for inhibiting death of mature neurons induced by the amylospheroid. In one aspect, the present disclosure relates to a use of Na+/K+-ATPase ?3 as a binding target molecule of amylospheroid. In another aspect, the present disclosure relates to a method for suppressing death of mature neurons induced by the amylospheroid, including inhibiting protein-protein interaction between the amylospheroid and the Na+/K+-ATPase ?3, and the like.