Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1,R2,R3,R4,R5 and R6 are as described herein.

Abstract: The invention relates to novel compounds derived from amino acids of formula (I) and also to cosmetic or dermatological compositions containing them and to their use as agents for treating human perspiration in a cosmetic composition. The invention also relates to a cosmetic process for treating perspiration and possibly the body odour associated with human perspiration, especially underarm odour.

Abstract: The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities 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, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

Abstract: Provided is a pharmaceutical composition comprising, as an active ingredient, a quinoline or quinazoline derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof, which is effective in the prevention and treatment of a cancer, inflammation, autoimmune diseases or neurodegenerative disorders which are induced by the overexpression of inhibitor of apoptosis proteins (IAPs).

Abstract: Small molecule, peptidic hepatocyte growth factors mimics, which act as both mimetics and antagonists, have been generated. These molecules have been shown or predicted to have therapeutic potential for numerous pathologies including dementia, neurodegenerative disease, diabetes and metabolic syndrome, cancer, and defective wound healing.

Abstract: Described herein are the preparation and use of novel bromo-phosphonomethylphenylalanine amino acid derivatives (BrPmp) and BrPmp-containing peptides as specific, irreversible protein tyrosine phosphatase inhibitors, which are suitable for application in peptide synthesis. These derivatives are particularly advantageous since their synthesis is both easy and scalable, and they are suitable for peptide synthesis. The BrPmp derivatives described herein can be appropriately protected to allow for solid phase peptide synthesis (SPPS) and incorporation into peptides for preparation of protein tyrosine phosphatase inhibitors and inhibitor libraries. The peptides and peptide libraries can be used to identify new protein tyrosine phosphatase specific sequences and profile protein tyrosine phosphatase activity in cell lysates, diagnostic samples and biopsy samples.

Abstract: The present invention relates to peptides or fragments thereof, which peptides bind to mesenchymal stem cells. The present invention also relates to a method for identifying, isolating, specifically selecting and/or enriching mesenchymal stem cells, wherein the peptides, or fragments thereof, are employed for specifically binding to the mesenchymal stem cells. Also, the present invention relates to the use of the peptides of the invention, or fragments thereof, and of the mesenchymal stem cells isolated with the peptides of the invention, or fragments thereof, for treating, injuries and/or degenerated bone, cartilage or tissues.

Abstract: The present invention discloses compounds of formula I and II 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: A medical device includes a substrate having at least a portion thereof functionalized with at least one reactive member and a chemotactic agent functionalized with at least one complementary reactive member, wherein the at least one reactive member and the at least one complementary reactive member are covalently bonded, adhering the chemotactic agent to the substrate.

Abstract: The present disclosure provides targeting peptides and vectors containing a sequence that encodes targeting peptides that deliver agents to the brain.

Abstract: The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.

Abstract: The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes.

Abstract: The present invention concerns a peptide of the general formula (I): R1-(AA)n-X1—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: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract: The invention provides lipophilic conjugates comprising a peptide coupled to a fatty acid, the peptide comprising at least two positively charged amino acid residues, said peptide after conjugation to the fatty acid possessing antibacterial, antifungal, and/or anticancer activity higher than prior to conjugation. The lipophilic conjugates are suitable for treatment of infections caused by pathogenic organisms such as bacteria and fungi. The lipophilic conjugates are also suitable for sanitation, as disinfectants, or for food preservation.

Abstract: Disclosed are a novel therapeutic agent and a novel prophylactic agent for atherosclerosis, a blood cholesterol level-lowering agent, and a functional food or a food for specified health uses effective for the inhibition and/or prevention of aging of blood vessels or inflammation in blood vessels. Specifically disclosed are an inhibitor of the progression of atherosclerosis, a prophylactic agent for atherosclerosis, a blood cholesterol level-lowering agent, and a functional food and a food for specified health uses both effective for the inhibition and/or prevention of aging of blood vessels or inflammation in blood vessels, each of which comprises, as an active ingredient, a hydrolysis product of a collagen comprising at least one collagen tripeptide Gly-X-Y [wherein Gly-X-Y represents an amino acid sequence; and X and Y independently represent an amino acid residue other than Gly].

Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.

Abstract: Described herein are small peptide domains and consensus sequences that bind small target molecules of industrial importance, e.g., metals such as nickel, ? carotene, and isoflavones such as genistein. Also described are fusion proteins containing such binding domains fused to proteins or to peptide domains like GST or GBD that bind other ligands and can be used to immobilize the target binding domain on a support. One class of fusion proteins that is useful in industrial settings are fusions that contain concatemers of target binding domains, which increases the binding equivalents per molecule.

Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: This invention relates to a novel process for synthesizing the product ibodutant shown in the figure below, consisting of a small number of high-yield steps involving reagents and solvents with low environmental impact, characterized by the coupling of two portions, compounds (3) and (4), one of which (3) is synthesized by coupling of 6-methyl-2-benzo[b]thiophenecarboxylic acid (1) with 1-amino-alpha-alpha-cyclopentan carboxylic acid and subsequent cyclization with oxazolone, while the other, compound (4), is obtained from suitable highly selective functionalizations of 4-aminomethylpiperidine (2).

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: Peptides and conjugates thereof comprising one or more bioactive agents which can be coupled to a tissue via a transglutaminase and related methods.

Abstract: The present invention relates to peptides and antibodies which bind to melanoma inhibitory activity protein and the uses of such peptides and antibodies. The invention also relates to nucleic acids coding for such peptides or antibodies. The invention also relates to pharmaceutical compositions comprising such peptides or antibodies or such nucleic acids. The present invention also relates to small molecule compounds which bind to melanoma inhibitory activity protein and to uses of such small molecule compounds. Moreover, the present invention also relates to a method of preventing dimerization and/or aggregation of melanoma inhibitory activity (MIA) protein. The invention is based on the identification of the relevant sites of interaction of the MIA protein with the inhibitory peptides/antibodies.

Abstract: Disclosed is a protein hydrolysate having DPP-IV inhibiting activity, the hydrolysate being enriched in peptides having a length of 2-8 amino acids comprising at least one proline residue, an isolated peptide derivable from such a protein hydrolysate, or a mixture thereof, and the use of such protein hydrolysate or isolated peptide for the manufacture of a medicament, food supplement, beverage or food product for prophylaxis and/or treatment of a DPP-IV mediated condition, in particular chosen from the group of obesity, type 2 diabetes mellitus and an immunological disorder.

Abstract: The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6 or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24)alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or NH—; or XR5 with X?O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I).

Abstract: The present invention encompasses a method for screening for a kokumi-imparting substance by using the calcium receptor activity as an index, a composition containing a kokumi-imparting substance obtained by the screening method, a method for producing food or drink imparted with kokumi, and food or drink imparted with kokumi.

Abstract: The invention provides a method of reducing or preventing mitochondrial permeability transitioning. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2 a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.

Abstract: Compounds and compositions comprising a B-type natriuretic signal peptide fragment agent, and methods of use thereof, are provided for the treatment or prevention of cardiovascular diseases, disorders, and conditions.

Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Abstract: A low-fat food containing an amino acid or a peptide which is able to activate a calcium receptor, examples of which include ?-Glu-X-Gly, ?-Glu-Val-Y, ?-Glu-Ala, ?-Glu-Gly, ?-Glu-Cys, ?-Glu-Met, ?-Glu-Thr, ?-Glu-Val, ?-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, D-Cys, ?-Glu-Met(O), ?-Glu-?-Glu-Val, ?-Glu-Val-NH2, ?-Glu-Val-ol, ?-Glu-Ser, ?-Glu-Tau, ?-Glu-Cys(S-Me)(O), ?-Glu-Leu, ?-Glu-Ile, ?-Glu-t-Leu, ?-Glu-Cys(S-Me), etc, wherein X and Y are an amino acid or an amino acid derivative.

Abstract: A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemization, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerization.

Abstract: The invention relates to crystalline peptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.

Abstract: The invention provides a cationic lipid comprising: (i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor; (ii) a linking moiety of formula (5): —(HNR5)2NC(O)R3C(O)—??(5), wherein: each R5 is independently an optionally substituted C1-4 alkylene moiety; and R3 is an optionally substituted alkylene or alkenylene moiety; and (iii) two lipophilic moieties, wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.

Abstract: The invention provides a method of preparing a sirtuin complex. The invention also provides a method of detecting a sirtuin in a sample comprising use of the aforesaid sirtuin complex.

Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:

Abstract: The present invention provides an anti-hypertensive agent. The anti-hypertensive agent of the present invention contains, as an active ingredient, at least one peptide selected from the group consisting of peptides originally derived from globin proteolysate, each of which consists of one of the following amino acid sequences (1) to (6), or a globin proteolysate containing at least one of the peptides: (1) Val-Val-Tyr-Pro (SEQ ID: NO. 1); (2) Trp-Gly-Lys-Val-Asn (SEQ ID: NO. 2); (3) Trp-Gly-Lys-Val (SEQ ID: NO. 3); (4) Trp-Gly-Lys (SEQ ID: NO. 4); (5) Ala-Ala-Trp-Gly-Lys (SEQ ID: NO. 5); and (6) Phe-Glu-Ser (SEQ ID: NO. 6).

Abstract: The present invention pertains to the use of certain flavour enhancing compounds obtainable from an Allium species. In one embodiment, seeds from chives, leeks, ramson and other onions are used for conveying strong kokumi flavour enhancing effects on food products without imparting an onion or garlic-like off taste. These flavour enhancing compounds are also useful for the preparation of Amadori products, which are also used as kokumi flavour enhancing compounds.

Abstract: A composition for promoting lacrimal secretion which can be used safely and effectively in the lacrimal secretion promoting therapy, not in the conventional supplemental therapy of lacrimal fluid components is provided. The composition for promoting lacrimal secretion comprising a peptide derivative represented by the formula (I): and a contact lens which retains and/or contains the composition are provided.

Abstract: Novel dendrimeric peptide compounds are disclosed that have a formula represented by the following formula I: The compounds demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention and treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present peptides are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.

Abstract: Provided is a novel crystal of oxidized glutathione hexahydrate. Crystal of oxidized glutathione hexahydrate is produced by cooling an aqueous solution containing oxidized glutathione to 15° C. or lower to precipitate a crystal of oxidized glutathione hexahydrate.

Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

Abstract: The combined use—whether by adsorption or covalent linkage—of Melatonin adjacent any bone implant or graft, preferably any calcium- and oxide-containing artificial bone graft material, and more preferably a calcium aluminate composition. Alternatively, the bone graft or implant material may be used as a scaffold for tissue engineering.

Abstract: Compositions comprising certain tripeptides which are capable of binding a metal in a square planar orientation, a square pyramidal orientation, or both, are disclosed in processes for modulating tagged peptides or proteins. Such compositions and processes may be used for site-specific chiral inversion of amino acids, site-specific peptide cleavage, and protein purification, among other uses.

Abstract: The invention relates to the production of bioactive products that are derived from milk proteins for the production of bioactive milk products derived from milk proteins, particularly caseins. The 16 inventive peptides can be obtained chemically, biotechnologically or by means of enzymatic treatment from proteins containing same and give rise to peptides with an antimicrobial activity, an in vitro angiotensin converter inhibitor activity and/or antihypertensive activity and/or antioxidant activity. Said nutraceutical products are suitable for use in the food and pharmaceutical industries, both in the form of a hydrolyzate or bioactive peptides.

Abstract: The present invention includes methods of making and methods of using peptidomimetics compositions that mimic ?-helical BH3 sequences in cells. The peptidomimetics can be used to mimic ?-helical BH3 sequences and kill cancer cells.

Abstract: Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or ary1-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.

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.