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

Abstract: The invention concerns polypeptides of the general formula (I): A-(Xaa)n-Lys-X-Lys-B wherein: i) A is —NH2, NH3+, or NH-D (D is an acyl group being biotin or an alkyl chain (C2-C22)), H) B is H, O? OR1 or NR2R3 and R1, R2 and R3 independently either: H or an alkyl chain (C1-C24), iii) (Xaa)n is an amino acid chain including any amino acid natural or not, excluding arginine and lysine, iv) “n” is between 0-3, and v) X is either a chain of two any amino acids (Xaa1Xaa2), which may be the same or different, excluding arginine, lysine and excluding Xaa1Xaa2=Thr-Thr, Gly-His and Glu-His, or X is a spacer selected among beta-alanyl, 5-amino-valeroyl, 4-amino-cyclohexanoyl, 4-amino-butyroyl, 6-amino-caproyl and derivatives thereof. More particularly, the invention concerns polypeptides of formula (I) wherein “n” is 0 and with the formula: A-Lys-X-Lys-B; A, X and B being defined herein. Compositions containing at least one of said polypeptides and their use.

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 present invention relates to the use of a preparation comprising a substance that is capable of binding acetaldehyde, and to the use of a filter that is attached to a tobacco product to reduce tobacco and/or alcohol dependence.

Abstract: Compositions for regenerating tissue and wound repair, among other applications, are described.

Abstract: The present invention is directed to an isotopically labeled trapping agent, methods for detecting reactive metabolites and methods of identifying drug candidates. More specifically, the isotopically labeled trapping agent and methods for detecting reactive metabolites may be used to detect both “hard” and “soft” reactive metabolites, thereby eliminating false positives.

Abstract: The present invention concerns a monomeric or multimeric tripeptide molecule able of inhibiting Cripto signalling in embryonic stem cells, thereby enhancing dopamine specification and differentiation, after transplantation in animal models of Parkinson's disease, as well as reducing tumor formation, and uses thereof.

Abstract: The invention concerns the use of inhibitors of the urokinase type of plasminogen activator (uPA) appearing in the anterior segment of the eye, for the treatment and prevention of corneal ulcers and other disorders. The invention further concerns pharmaceutical compositions, comprising inhibitors of uPA, preferably eye drops and eye ointments. The pharmaceutical compositions according to the invention preferably comprise PAI-2 protein or a derivative thereof retaining uPA-inhibiting capacity, or a tripeptide aldehyde inhibitor, preferably the D-Phe-Pro-Arg-aldehyde (Ald-1). The PAI-2 protein, used according to the invention, is preferably produced through bacterial expression, as a fusion protein.

Abstract: The present invention provides a novel class of macrocyclic compounds, which are useful as cysteine protease inhibitors. Also provided are novel intermediates and methods of preparing the compounds. The invention also provides pharmaceutical compositions comprising the compounds. The compounds and compositions are useful in methods of treating or preventing one or more diseases associated with cysteine protease activity, particularly those associated with calpain activity.

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: A “one-step” process for production of peptides and other organic molecules which are both esters and also acetylated forms of the desired molecule. The ester may be a mono-ester, di-ester, or another poly-ester, complexed with a molecule for protecting the organic molecules in the digestive tract. The method allows simple adjustment of the delivery properties of the peptides produced, in particular adjustment or addition of lipiphilic tendencies. A therapeutic or nutrient made by this method comprises acetylated organic molecule esters, in particular an acetylated peptide ester or even an acetylated amino acid ester and demonstrates improved metabolic properties leading to increased efficiency for therapeutic and cosmetic purposes including oral, transdermal, sublingual, buccal, and topical administration.

Abstract: Degradable complexes comprising a polycation, a polyanion and a polynucleotide are useful for in vivo polynucleotide delivery applications.

Abstract: A biologically active peptide, of Formula (1) [X-L-?-Glu-Trp-Y], a novel pharmaceutical composition containing the peptide, a method for preparing the peptide and uses of the peptide are disclosed.

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

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: Provided are novel human tumor-specific antibodies as well as fragments, derivatives and variants thereof that recognize tumor-associated antigen NY-ESO-1. In addition, pharmaceutical compositions comprising such antibodies and mimics thereof in the treatment of tumors are described.

Abstract: This invention relates to a collagen polypeptide comprising a tripeptide motif having the formula (ProYaaGly)n, where Yaa is an O-methylated amino acid residue and “n” is the number of motif repeats. Preferred O-methylated amino acid residues at the Yaa position include (2S,4R)-4-methoxyproline. Other suitable amino acid residues at that position include O-mono or O-di-halogenated methylproline. Also, disclosed is a method of making a synthetic or a semi-synthetic collagen polypeptide molecule having increased stability relative to natural collagen. The strengthened collagen molecules are suitable for use in biomaterials for the medical field or in leather-related products prepared by the tanning industry.

Abstract: The present invention relates to the identification and use of bone morphogenetic protein (BMP)-binding domains of members of the repulsive guidance molecule (RGM) protein family, and polypeptide fragments and fusion proteins derived therefrom. The domains, i.e., peptide fragments and fusion proteins, according to the invention are suitable as agents for the active or passive immunization of individuals, or as diagnostic and therapeutic agents for use for diseases or medical conditions in whose origin or progression a member of the RGM family and a cellular receptor associated with this molecule, such as neogenin and/or BMP in particular, is involved. The invention further relates to monoclonal and polyclonal antibodies directed against the binding domains according to the invention, and against the polypeptides derived therefrom, and to methods for producing the polypeptides, fusion proteins, and antibodies according to the invention.

Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.

Abstract: The invention provides means and methods for inducing and/or enhancing immunogenic reproducibility and/or immunogenicity of a compound, comprising at least in part restricting the conformation of said compound. The conformation is preferably restricted by the formation of at least one internal bond within said compound. Protein mimics comprising an amino acid sequence bound to a scaffold and/or a carrier, wherein said amino acid sequence comprises at least one internal SS-bridge, are also herewith provided.

Abstract: The invention relates to a process for the preparation of cardiodilatin fragments, to highly purified cardiodilatin fragments, and to appropriate intermediates for the preparation of said fragments. Furthermore, the invention relates to highly purified cardiodilatin fragments which are free of peptide impurities and exhibit a single migration peak in capillary electrophoresis, as well as to appropriate processes for the preparation of same.

Abstract: A probe compound for protein tyrosine phosphatases (PTPs), as shown in Formula (I) is provided. In Formula (I), A1 and A2 represent amino acids. The amino acids include leucine, phenylalanine, glutamic acid, lysine, alanine, arginine, aspartic acid, asparagine, citrulline, cysteine, cystine, glutamine, glycine, histidine, hydroxyproline, isoleucine, methionine, proline, serine, threonine, tryptophan, valine or a combination thereof. The invention also provides probe compound precursors for protein tyrosine phosphatases (PTPs).

Abstract: The present invention features polypeptides, such as antibodies, and their use in the treatment and diagnosis of neoplasms.

Abstract: The invention is related to the medicinal means of correction of metabolic vascular syndrome and diseases, associated with disordered vascular wall permeability and capillaries fragility, and can be used as a means of enhancing capillaries resistance. There is proposed a peptide lysyl-glutamyl-asparagine acid of the general formula H-Lys-Glu-Asp-OH sequence 1 [SEQ ID NO:1], revealing biological activity and capable of enhancing capillaries resistance. There is also proposed a pharmaceutical composition enhancing capillaries resistance, containing effective amount of peptide lysyl-glutamyl-asparagine acid of the general formula H-Lys-Glu-Asp-OH sequence 1 [SEQ ID NO: 1] as its active base and pharmaceutically acceptable carrier. This pharmaceutical composition is in form for parenteral administration.

Abstract: The present invention provides ?4?1 integrin ligands that display high binding affinity, specificity, and stability. The ligands comprise a peptide having n independently selected amino acids, wherein at least one amino acid is an unnatural amino acid or a D-amino acid, and wherein n is an integer of from 3 to 20. Methods are provided for administering the ligands for treating cancer, inflammatory diseases, and autoimmune diseases. Also provided are methods for administering the ligands for imaging a tumor, organ, or tissue in a subject.

Abstract: The present invention provides HLA-DR (MHC class II) binding peptides derived from the ovarian/breast cancer associated antigens, Human Epidermal Growth Factor Receptor 2 (HER-2/neu), Carcinoembryonic Antigen (CEA), Insulin Growth Factor Binding Protein 2 (IGFBP-2), and Cyclin D1. The immunogenic peptides can be used in cancer vaccines.

Abstract: The present invention relates to novel compounds, particularly derivatives of boroarginine, boroornithine and borolysine that selectively modulate, regulate, and/or inhibit enteropeptidase. The invention also relates to compositions, particularly pharmaceutical compositions, as well as methods to treat excess weight, obesity and diseases associated with an abnormal fat metabolism.

Abstract: The invention provides a self-assembling peptide comprising (a) a first amino acid domain that mediates self-assembly, wherein the domain comprises alternating hydrophobic and hydrophilic amino acids that are complementary and structurally compatible and self-assemble into a macroscopic structure when present in unmodified form; and (b) a second amino acid domain that does not self-assemble in isolated form. In certain embodiments of the invention the second amino acid domain comprises a biologically active peptide motif, e.g., a peptide motif found in a naturally occurring protein, or a target site for an interaction with a biomolecule. In certain embodiments of the invention the naturally occurring protein is a component of the extracellular matrix, e.g., a component of the basement membrane. The invention further provides scaffolds comprising the self-assembling peptides and methods of using the scaffolds including for cell culture, tissue engineering, and tissue repair.

Abstract: A peptide of formula I (SEQ ID NO: 1): Lip-A-Gly-His-B-R (I) wherein: Lip is a lipoyl residue of R or S configuration; A is absent or is a lysine residue of configuration L or D; GIy is a glycine residue; His is a histidine residue of configuration L or D; B is a lysine residue of configuration L or D, or a lysine residue of configuration L or D in which the NH2 group of the side chain comprises a modification, wherein said modification is (i) a replacement with a hydrogen or (ii) a modification with a protecting group selected from the group consisting of acetyl, benzoyl, tosyl, sulfonyl benzene, benzyloxycarbonyle and palmitoyl; wherein R is O(Z) or N(Z?)(Z?), and wherein Z, Z? and Z? are independently of each other a hydrogen or a protecting group selected from the group consisting of methyl, ethyl, propyl, phenyl, hexyl, decyl and hexadecyl, or a racemate, an enantiomer or a diastereomer thereof, or a mixture thereof, or a salt thereof.

Abstract: Monodisperse macromolecular conjugate compositions of a peptidic carrier irreversibly or reversibly conjugated with one or more effectors and one or more therapeutic agents, wherein at least one effector or therapeutic agent is attached to a pendant reactive group on said peptidic carrier via a water-soluble polymer. Monodispersity is obtained through the use of orthogonal and separate conjugation reactions.

Abstract: The present invention relates to a peptide comprising amino acids according to Formula (I): ((X)l(Y)m)n wherein l, m and n are integers from 0 to 10; X and Y, which may be the same or different, are an amino acid selected from the group consisting of hydrophobic amino acids and/or cationic amino acids, for use as a medicaments.

Abstract: A solid phase peptide synthesis method for synthesizing a peptidyl contrast agent is disclosed. In one example, the method includes synthesizing an amino-chelator loaded resin, coupling of the amino-chelator loaded resin to the C-terminus and/or backbone of a peptide, cleaving the amino-chelator-peptide from a resin, and chelating a lanthanide metal to the amino-chelator-peptide.

Abstract: The invention which is the subject of the present application relates to a compound of structure I: A-B-C for use in the prophylaxis and/or treatment of a viral infection, and in particular for preventing and/or inhibiting viral replication, in which A is a quinoline or a quinoline-type group, B is a single amino acid or a peptide or polypeptide having a given amino acid sequence, C is an O-phenoxy group and the symbol “-” indicates that the entities A, B and C are chemically bonded within the compound I. According to a particular embodiment, said compound is a protease inhibitor, in particular a caspase inhibitor, and more particularly the inhibitor Q-VD-OPh (N-(2(quinolyl)valyl-aspartyl-(2,6-difluorophenoxy)methyl ketone), optionally in an O-methylated form.

Abstract: The invention relates to a PEGylated peptide-chromophore conjugate, which forms irregular micelles, for use in photodiagnostic and phototherapeutic applications. Methods for synthesizing and using the conjugates of the invention are also provided.

Abstract: Methods for inhibiting an inflammatory reaction in a mammal and pharmaceutical compositions are provided. The methods comprise administering to the mammal an effective amount of a peptide of the formula: X1-X2-X3 wherein X1 is selected from the group consisting of 2-amino-hexanoic acid; 2-amino-heptanoic acid; 2-amino-octanoic acid; cyclohexyl-substituted 2-amino-ethanoic acid, 2-amino-propanoic acid or 2-amino-butanoic acid and methionine; X2 is an acidic amino acid; and X3 is an aliphatic amino acid; or of a peptide of the formula: X4-X5 wherein X4 is an aromatic or aliphatic amino acid; and X5 is an acidic amino acid.

Abstract: The present invention provides novel peptides that facilitate the opening of mammalian tight junctions, i.e. tight junction agonists. The present invention also provides methods for the treatment of disease by administering to a subject suffering from the disease a composition comprising a peptide tight junction agonist of the invention in combination with a therapeutically effective amount of an active agent.

Abstract: The present invention provides, among other things, soluble derivatives of soluble polypeptides that incorporate membrane binding elements. Methods of making these soluble derivatives, and methods of using these soluble derivatives also are provided.

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

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: Processes for the synthesis and purification of a Gly-Gly-Val-Leu-Val-Gln-Pro-Gly octapeptide (SEQ ID NO 1).

Abstract: The present invention provides phenylalanine derivatives that inhibit SH2 domain binding with a phosphoprotein. These derivatives include compounds of the formula: W—Y-(AA)n-Z wherein n is 0 to 15; Y is a phenylalanyl radical having a phenyl ring, an amine end, and a carboxyl end, the phenyl ring having one or more substituents, e.g., hydroxyl, carboxyl, formyl, carboxyalkyl, carboxyalkyloxy, dicarboxyalkyl, dicarboxyalkyloxy, dicarboxyhaloalkyl, dicarboxyhaloalkyloxy, and phosphonoalkyl, or phosphonohaloalkyl; W is a moiety attached to the nitrogen of Y and is, e.g.

Abstract: The present invention is directed to the use of a class of peptide compounds for treating pain in trigeminal neuralgia.

Abstract: The present invention relates to the crystal structure of the insulin receptor ectodomain, to the nature of its N-linked glycans and to methods of using the crystal and related structural information to screen for and design compounds that interact with or modulate the insulin receptor and/or the closely-related insulin-like growth factor receptors or variants thereof.

Abstract: The present invention relates to homo- and hetero-dimer compounds formed by a disulfide, sulfinyl thio, or olefin bond between two monomers. A method of making a homo- or hetero-dimer compound is also disclosed. The present invention also relates to monomer compounds capable of forming homo- or hetero-dimer compounds, as well as oligomers formed via linkage of one or more dimers. Also disclosed are methods of inhibiting the activity of target RNA molecules, particularly those having a secondary structure that include a stem or stem-loop formation. Dimer compounds capable of inhibiting the activity of an HIV-I RNA frameshifting stem-loop and a (CUG)n expanded repeat stem-loop are disclosed, as are methods of treating diseases associated with these target RNA molecules. The dimer compounds can also be used for selectively detecting presence of the target RNA molecule in a sample.

Abstract: The present invention provides peptides which affect T-cells, presumably by action on the T-cell antigen receptor. The present invention further relates to the therapy of various inflammatory and autoimmune disease states involving the use of these peptides. Specifically, the peptides are useful in the treatment of disorders where T-cells are involved or recruited. In one aspect the peptides have the formula: R1-A-B-A-R2 in which A is a hydrophobic amino acid or a hydrophobic peptide sequence comprising between 2 and 10 amino acids B is a charged amino acid R1 is NH2 and R2 is COOH In another aspect the peptides have the formula: R1-A-B-C—R2 in which A is a peptide sequence of between 0 and 5 amino acids; B is cysteine; C is a peptide sequence of between 2 to 10 amino acids; R1 is NH2; and R2 is COOH.

Abstract: The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by a trouase enzyme such as Thimet oligopeptidase. Also disclosed are methods of making and using the prodrug compounds.

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: Conformationally constrained peptide mimetics in which a hydrogen bond interaction is replaced with a covalent hydrogen bond mimic are provided. Also provided are various methods of making these peptide mimetics.