Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Abstract: Diagnostic compositions and methods for imaging and/or assessing collagen are described. The diagnostic compositions can include collagen binding peptides.

Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

Abstract: Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula: —Ra—Y—Rb—(Z)x where Ra, Rb, Y, Z and x are as defined, and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.

Abstract: Peptides generated from a random library that are bound by a monoclonal antibody to Chlamydial glycolipid exoantigen (GLXA) and thus mimic this antigen are disclosed. Peptides that correspond to antigen-binding regions of an anti-idiotypic antibody (mAb2) specific for anti-GLXA antibody (Ab1) which act as molecular mimics of GLXA are also disclosed used as immunogens to induce broadly reactive genus-specific anti-chlamydial antibodies. These peptides and immunogenic DNA encoding the mAb2-like peptides, microparticle or nanoparticle formulations and other formulations of these peptides are disclosed as are methods for immunizing subjects to obtain genus-specific anti-chlamydial antibodies and to treat or prevent Chlamydia-associated or induced rheumatoid arthritis.

Abstract: Described herein are peptide targeting imaging agents. The peptides are covalently attached to the imaging agent and have a specific peptide sequence that enables the imaging agent to accumulate specifically in tumor tissues. Additionally, the imaging agents are readily excreted by the subject within a short period of time after administration to the subject. Methods for using the imaging agents are also described herein.

Abstract: Glycopeptide conjugates, and methods of making and using such conjugates are disclosed. Certain glycopeptide conjugates comprise tumor associated carbohydrate antigens and peptide epitopes. Certain glycopeptide conjugates comprise cyclic peptide scaffolds that display carbohydrate antigens in a clustered fashion. The immunogenicity of select glycopeptide conjugates is demonstrated.

Abstract: The invention relates to peptide derivatives (peptides and pseudo-peptides) and use thereof as vectors for molecules of interest. The invention also relates to conjugates containing a peptide derivative of the invention bound to a molecule of interest. The peptides and prodrug conjugates of the invention can be used to vectorise molecules of pharmaceutical or diagnostic interest, such as, for example, therapeutic molecules, imaging or diagnostic agents, or molecular probes, across cell membranes, and notably to promote their transport across the blood-brain barrier (BBB).

Abstract: The present invention relates generally to novel peptides and related compounds that have thrombopoietic activity. The compounds of the invention may be used to increase production of platelets or platelet precursors (e.g. megakaryocytes) in a mammal.

Abstract: Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.

Abstract: A complex of an echinocandin compound with a carbohydrate is described having improved thermal stability and water solubility. A process for making the echinocandin/carbohydrate complex is also described as well as the use of the complex in pharmaceutical formulations and treatments of fungal infections.

Abstract: The invention concerns the use of at least a synthetic compound comprising: a carrier molecule having at least a hydrocarbon chain comprising at least 10, advantageously at least 12, preferably at least 14 and not more than 300, advantageously not more than 100, preferably not more than 50, selected'among C, N, O, S, P and Si, and comprising at least two reactive functions, or capable of reacting, for grafting lateral arms on said chain, and at least two different epitopes carried by said lateral arms grafted on said carrier molecule, as standard or control for immunoassay of said biological molecules, in particular of polypeptides or proteins.

Abstract: At least one embodiment of the present invention relates to new cycloundecadepsipeptide compounds and to the use of said compounds as a medicament, in particular as antiviral agents, more particularly for preventing or treating Hepatitis C infections or HCV induced disorders.

Abstract: The present invention relates to a compound represented by formula (I): wherein R1 represents a hydrogen atom or the like; R2 and R3 represent a hydrogen atom or the like; R4 is a group represented by (II) R5 represents a phenyl group which may be substituted with a halogen or the like; m is an integer of from 1 to 3; and p is an integer of from 0 to 4; or a pharmaceutically acceptable salt thereof.

Abstract: Macrocyclic compounds of the formula in which R1, R3, V1, V2, X1, X2, Y, Z, Ar, AA and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16, 17 or 18, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them are presented.

Abstract: The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.

Abstract: Disclosed are hydrochloride salts of telavancin having a chloride ion content of from about 2.4 wt. % to about 4.8 wt. %. The disclosed salts have improved stability during storage at ambient temperatures compared to other hydrochloride salts. Also disclosed are processes for preparing such salts.

Abstract: Disclosed herein are isolated, purified peptides, biologically active fragments and analogs of the peptides having anti-tumor activity in mammals, pharmaceutical formulations comprising the peptides, fragments and analogs and methods of treating mammals suffering from tumors using such materials.

Abstract: A new process for the preparation of bicyclic peptide compounds Formula (I) in high yields of high purity, useful as intermediates for preparing compounds with pharmacological activity, is described.

Abstract: Isolated cyclic polypeptides useful as vaccinations for the treatment/prevention of HIV are disclosed. An exemplary peptide comprises at least 18 consecutive amino acids of a V3 domain of gp120, starting at position 303 and ending at position 322, the positioning being according to a numbering of the V3 domain of gp120 in a HXB2 strain, wherein amino acids at position 303 and 322 are bonded. Vaccines comprising same and methods of treating AIDS using same are also disclosed.

Abstract: The invention provides peptide epitopes for use in the prevention and/or treatment of influenza or for the development of such treatment or vaccine against influenza. The invention also relates to a method for evaluating the potential of a chemical entity, such as an antibody, to bind to a peptide epitope derived from the divalent sialoside binding site of hemagglutinin protein of influenza virus, and to conjugates containing one or more such peptide epitopes. The peptide epitopes of the invention are cyclic peptides comprising a 7-mer peptide derived from H1, H3 or H5 hemagglutinin of influenza virus. The 7-mer peptide has a sequence corresponding to the loop sequence at positions 220-226 of X31-hemagglutinin.

Abstract: Provided are methods and compositions for selectively targeting CRKL through the use of targeting peptides. Selective targeting of secreted CRKL through the use of a targeting peptide may be used, for example, in the treatment of cancer to deliver a chemotherapeutic compound, fusion protein, or fusion construct to a cancer cell or tissue.

Abstract: Described herein are peptide compositions of a prominin-1, which have regenerative activity. As such the peptides are useful when regeneration is needed, for example, to enhance angiogenesis, increase VEGF binding to endothelial cells, promote vasodilation, enhance cell migration, enhance cell proliferation, stimulate neuronal growth, prevent neurodegeneration, and/or promote neuroregeneration.

Abstract: An isolated polypeptide, Z domain, derived from B domain of Staphylococcal protein A, comprising a pair of anti-parallel alpha helices that are capable of binding a target, is provided herein. Introduction of different natural amino acid mutations in the polypeptide are provided here. Also provided are methods of using the two-helix binders.

Abstract: Characterization of the biosynthetic gene cluster for the lantibiotic actagardine, identification of a novel variant of actagardine and its biosynthetic cluster, and methods of production and use of actagardine are described.

Abstract: The present invention describes a previously unknown interaction between secreted aspartic proteases (SAPs), including SAPs 4-6 of Candida albicans, and integrins on host cells. The SAPs secure entry into the host cell through RGD-like binding motifs and subsequently induce apoptosis, thereby clearing the way for systemic infection. The invention thus provide a new target for therapeutic intervention and describes peptides and antibodies that inhibit the action of SAPs in this context, including their interaction with integrins.

Abstract: The invention relates to an improved vaccine to treat Alzheimer's disease.

Abstract: The present invention discloses the structure, preparation methods and uses of a series of novel polyheterocyclic based compounds (Ia-Ib and IIa-IIb) that are highly effective for inhibiting hepatitis C virus (HCV): where the structural variables are defined herein. The present invention is also provides a method of treating HCV infection by the polyheterocyclic based HCV inhibitory compounds, compositions and therapeutic methods.

Abstract: Functionalized peptide monomers, peptides that have been functionalized to contain a polymerization moiety, are disclosed. The use of these functionalized peptide monomers to form peptide polymers which are useful as synthetic surfaces capable of supporting culture of cells in culture, particularly cells that will be used therapeutically, is also disclosed. Methods of making the surfaces and methods of using the surfaces are also disclosed.

Abstract: The present invention relates to peptides derived from the proinflammatory cytokines, interleukin-1? (IL1?) and tumor necrosis factor ? (TNF?), and their use in human or veterinary therapy, such as to generally treat diseases linked to the overproduction of IL1? or TNF? as well as acute or chronic inflammatory diseases, rheumatoid arthritis, septic shock, autoimmune diabetes, graft rejection in the host, etc.

Abstract: Devices, compositions, and methods are described which provide a tubular nanostructure or a composite tubular nanostructure targeted to a lipid bilayer membrane. The tubular nanostructure includes a hydrophobic surface region flanked by two hydrophilic surface regions. The tubular nanostructure is configured to interact with a lipid bilayer membrane and form a pore in the lipid bilayer membrane. The tubular nanostructure may be targeted by including at least one ligand configured to bind to one or more cognates on the lipid bilayer membrane of a target cell.

Abstract: The present invention relates to liquid nisin compositions having a high anti-microbial activity. The invention further relates to a method for preparing the liquid nisin compositions as well as their use as a preservative in food products.

Abstract: The present invention relates to novel octapeptide compounds of general formula (I): H-2-Nal1-cyclo(Cys2-Tyr3-AA4-Lys5-Val6-Cys7)-Thr8-NH2. Since these products have a good affinity for certain somatostatin receptor subtypes, they are particularly advantageous for treating pathological states or diseases in which one (or more) somatostatin receptor(s) is (are) involved. These compounds furthermore have physiochemical properties that make it possible to envisage them in diverse solutions for the formulation of medicaments, for example as a pharmaceutically acceptable carrier. The invention also relates to pharmaceutical compositions containing said products and to the use thereof for the preparation of a medicament.

Abstract: The current invention relates to the use of a peptide comprising an amino acid sequence in the preparation of a medicament for the regeneration of tissue, preferably for the treatment of a wound. Further the invention relates to compositions comprising such peptides, and use of said peptides in both medical and nonmedical (cosmetic) applications.

Abstract: Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production, are provided.

Abstract: An isolated polypeptide, Z domain, derived from B domain of Staphylococcal protein A, comprising a pair of anti-parallel alpha helices that are capable of binding a target, is provided herein. Introduction of a covalent bridge between two modified amino acids in the polypeptide is provided here. Also provided are methods of using the two-helix binders.

Abstract: The invention provides methods of producing functional split inteins having small N-intein and/or small C-intein. Using these split inteins with their protein trans-splicing and cleavage activities, we provide new and more effective methods of manipulating proteins. They include site-specific addition of synthetic peptides at protein's terminal and internal locations, ligation of synthetic and/or expressed polypeptides, controllable cyclization of synthetic and/or expressed polypeptides, and controllable cleavages of recombinant proteins. These methods have numerous utilities including but not limited to protein fluorescence labeling, fixation on microchips, site-specific PEGylation, and linkage with pharmaceutical molecules.

Abstract: The invention relates to KLK protease inhibitors. In particular, the invention is directed to KLK4 protease inhibitors and their uses in the treatment of a cancer, such as prostate cancer.

Abstract: Compounds which are FK228 analogues of the general formula (I) or (I?), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.

Abstract: The present invention provides a conjugate containing a moiety linked to a homing molecule that selectively homes to tumor lymphatic vasculature. The invention also provides a method of directing a moiety to tumor lymphatic vasculature in a subject by administering to the subject a conjugate containing a moiety linked to a homing molecule that selectively homes to tumor lymphatic vasculature.

Abstract: The invention provides nesiritide that is chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of nesiritide not attached to the water-soluble oligomer.

Abstract: Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporin and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.

Abstract: Provided is a cyclic peptide which comprises: (i) a CDK4 peptide region; and (ii) a cell-penetrating region; wherein the CDK4 peptide region comprises the amino acid sequence P1R1x1y1R2P2V (SEQ ID NO: 1), in which P1 and P2 are each proline, R1 and R2 are each arginine and each of x1 and y1 are either a linker or proline, wherein if x1 is a linker then y1 is proline or if x1 is proline then y1 is a linker, or wherein x1 and y1 when taken together form a linker, and wherein V may be present or absent; and wherein the cell-penetrating region is capable of enhancing the uptake of the cyclic peptide or a part thereof into cancer cells and comprises an amphiphilic amino acid sequence; and wherein the cyclic peptide or a part thereof is cytotoxic to and/or inhibiting to the growth of a cancer cell.

Abstract: Multifunctional probes are synthesized in a single step using peptide scaffold-based multifunctional single-attachment-point reagents. To obtain multifunctional probes using the methods of the invention, a substrate (e.g., a nanoparticle, polymer, antibody, protein, low molecular weight compound, drug, etc.) is reacted with a multifunctional single-attachment-point (MSAP) reagent. The MSAP reagents can include three components: (i) a peptide scaffold, (ii) a single chemically reactive group on the peptide scaffold for reaction of the MSAP with a substrate having a complementary reactive group, and (iii) multiple functional groups on the peptide scaffold. The peptide scaffold can include any number of residues; however, for ease of synthesis and reproducibility in clinical trials, it is preferred to limit the residues in the peptide to 20 or less.

Abstract: Disclosed are non-immunosuppressive cyclophilin-binding cyclosporins, e.g., of formula (I, Ia or II) as defined herein, having useful properties in the prevention of Hepatitis C infections.

Abstract: Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

Abstract: The invention provides an immunoglobulin G Fc region binding polypeptide, which polypeptide comprises an immunoglobulin G Fc region binding motif, BM, consisting of an amino acid sequence selected from: i) EQQX4AFYEIL HLPNL-TEX18QX20X21AFIX25X26LRX29, and ii) an amino acid sequence which has at least 85% identity to the sequence defined in i). Also provided are methods of isolation or production of IgG Fc-containing molecules.

Abstract: The invention refers to a synthetic peptide comprising an amino acid sequence of seven residues in length, preferably flanked by 2 cysteine residues at both ends, which is capable of specifically recognizing human CD154 and blocking CD40:CD154 interaction, thereby inhibiting the biological effects depending on such interaction. The peptide of the invention, which is preferably in a cyclic form, is suitable for use for diagnostic and therapeutic applications, especially for the diagnosis and therapy of tumor, inflammatory diseases and transplant rejection.

Abstract: The present invention discloses novel complex molecules useful as anti-allergic agents. These complex molecules include in particular, peptidic or peptidomimetic molecules, having a first segment which is competent for cell penetration and a second segment which is able to reduce or abolish mast cell degranulation, and in particular to reduce or abolish allergy mediators such as histamine secretion from mast cells. Specific examples of peptides with the desired activity are disclosed.

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.