Abstract: An autophagy-inducing compound comprises an autophagy-inducing peptide comprising beclin-1 residues 269-283 and a heterologous moiety that promotes therapeutic stability or delivery of the compound. The compound may be used to induce autophagy and in assays with beclin-1 binding partners.

Abstract: The present invention relates to immobilized biologically active entities that retain a significant biological activity following manipulation. The invention also comprises a medical substrate comprising a heparin entity bound onto a substrate via at least one heparin molecule, wherein said bound heparin entity is heparinase-1 sensitive.

Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis.

Abstract: TRPV1 antagonists and associated methods are provided. A TRPV1 channel antagonist can have the structure: Formula (I) wherein R1 can be —CH3, —(CH2)X(CH)YCH3 where x+y=1-20, an aromatic, a (CH2)n aromatic where n can be less than or equal to 6, a lipid, or a linker, and wherein R2 can be either Formula (II) or Formula (III) Additionally, R3 can be —O—R4 or —NH—R4 and R4 can be —H, —CH3, an ester, a cyclic ester, or an amide.

Abstract: The present application provides biligand and triligand protein-catalyzed capture (PCC) agents that specifically bind VEGF, as well as the use of these capture agents as detection, diagnosis, and treatment agents.

Abstract: The method of the preparation of micafungin sodium comprises the step of mixing the weak base and the aqueous solution containing micafungin acid (the structure is illustrated by formula I) or the mixed aqueous solution containing the compound of formula I and organic solvent in order to obtain the sodium salt of micafungin (the structure is illustrated by formula II).

Abstract: Antibodies and meditopes that bind to the antibodies are provided, as well as complexes, compositions and combinations containing the meditopes and antibodies, and methods of producing, using, testing, and screening the same, including therapeutic and diagnostic methods and uses.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 4 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.

Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.

Abstract: The present application describes a method of treating a bacterial infection comprising administering to a subject in need thereof a pharmaceutically acceptable amount of a defined macrocycle compound.

Abstract: The invention relates to novel pharmaceutically-useful peptides, in particular cyclic peptides that are agonists of the AngII type 2 receptor (AT2 receptor). The invention further relates to the use of such peptides as medicaments, to pharmaceutical compositions containing them, and to their production.

Abstract: The present invention concerns novel lantibiotic compounds, processes for the isolation and preparation thereof, pharmaceutical compositions containing the same, pharmaceutical acceptable salts thereof, and methods of use of the lantibiotics as antibacterial agents.

Abstract: A method of treating a bacterial infection in a subject is disclosed. The method comprises administering to the subject a therapeutically effective amount of a peptide being between 3 and 5 amino acids, wherein at least one amino acid of said 3 and 5 amino acids is selected from the group consisting of tryptophan, cysteine, proline and methionine.

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 present invention generally provides a separation matrix comprising at least two stationary phases and a stationary phase comprising at least one chiral modality and at least one achiral modality. Also provided are methods of using the separation matrix or the stationary phase to separate enantiomers of one or more chiral molecules.

Abstract: An autophagy-inducing compound comprises an autophagy-inducing peptide comprising beclin-1 residues 269-283 and a heterologous moiety that promotes therapeutic stability or delivery of the compound. The compound may be used to induce autophagy and in assays with beclin-1 binding partners.

Abstract: A prodrug comprising at least two different pharmaceutically and/or diagnostically active compounds independently bound by cleavable linkers and a protein-binding moiety which is capable of binding to carrier a molecule is described.

Abstract: Cross-linked proteins and peptides, and methods of making and uses of such cross-linked proteins and peptides. The cross-linked proteins and peptides have rigid, distance-matching bismethylene aryl cross-linking moieties. Compositions comprising the cross-linked proteins and peptides can be used as pharmaceutical delivery formulations. The cross-linked proteins and peptides can have improved properties, such as cell permeability, as compared to the parent protein or peptide.

Abstract: The present invention is related to peptides, which are suitable for use as cell-penetrating peptides (CPPs), variants thereof and/or complexes, fusion molecules and/or conjugates comprising same, use thereof for manufacture of compositions for diagnosing, treating and/or preventing of medical conditions.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Abstract: Methods and compositions for modulating cyclophilin D, e.g., at least one cyclophilin D biological activity, are provided. Modulation of cyclophilin D is useful in preventing or treating obesity, an overweight condition, or in accommodating a desire to lose weight as well as being useful in treating a variety of kidney diseases.

Abstract: The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.

Abstract: Provided are a cyclic peptide compound or a pharmacologically acceptable salt thereof capable of inhibiting parakeratosis of skin, and a method for producing the same.

Abstract: The molecular structures of metal-salen complexes which exerts pharmacological effects are clarified and the metal-salen complexes having such molecular structures and their derivatives are provided. A metal-salen complex compound is characterized in that a metal atom part in each of multiple molecules of the metal-salen complex or its derivative is multimerized via water.

Abstract: The present invention relates generally to tissue differentiation factor (TDF) analogs. More specifically, the invention relates to structure-based methods and compositions useful in designing, identifying, and producing molecules which act as functional modulators of TDF-like receptors. The invention further relates to methods of detecting, preventing, and treating TDF-associated disorders.

Abstract: The present invention relates to methods of treating or preventing retinal ganglion cell (RGC) death and/or glaucoma using modulators of neurotrophic receptors that comprise ?-turn peptidomimetic cyclic compounds or derivatives thereof. The neurotrophic receptor modulators can be used alone, in combination and/or in conjunction with one or more other compounds, molecules or drugs that treat or prevent ocular hypertension, RGC death and/or glaucoma.

Abstract: The present invention relates to hydrophobic modified peptides for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the compound(s) to be specifically delivered to the liver. The present invention furthermore relates to the use of the inventive hydrophobic modified peptides as well as to a method for the prevention and/or treatment of liver diseases or disorders.

Abstract: Methods, systems and compositions comprising novel peptidomimetics are disclosed that can be used to inhibit calpain and, more specifically, to treat tissue damage caused by pathologic activation of calpains.

Abstract: The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis.

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 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: 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: Specific template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are ?-amino acid residues connected from the carbonyl (C?O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these ?-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.

Abstract: Provided herein are polypeptides comprising or consisting essentially of a QSYDNTLSGSYVF (SEQ ID NO:1) or LSADSSGSYLYVF (SEQ ID NO:2) amino acid sequence. Also provided herein are methods of treating or preventing cast nephropathy in a subject. The methods comprise identifying a subject with or at risk of developing cast nephropathy and administering to the subject any of the polypeptides disclosed herein.

Abstract: Disclosed are short chain peptides that are constrained to adopt an alpha helicial conformation and their use as alpha helical scaffolds for directing amino acid side chains into positions analogous to those found in longer chain alpha helical peptides. Also disclosed is the use of these peptides for attaching peptidic or non-peptidic appendages in order to mimic side chains of longer alpha helical peptides. The peptides find use in mimicking naturally occurring peptides or proteins or in preparing new materials.

Abstract: A naive WW domain peptide library derived from a WW domain peptide sequence which has been diversified by changing the amino acid sequence at one or more positions is provided. The naive WW domain peptide library may be derived from a GroupIV WW domain peptide. Methods for making the naive WW domain peptide library and methods for selected a modified WW domain peptide that binds a target ligand using the naive WW domain peptide library are also provided. Also disclosed are modified WW domain peptides that bind desired target ligands, pharmaceutical compositions comprising such peptides, and uses for such peptides. The modified WW domain peptides have altered, improved or different, target ligand binding characteristics to those of the unmodified WW domain peptides from which they are derived.

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: The present invention relates to technetium imaging agents comprising radiolabeled c-Met binding peptides suitable for SPECT or PET imaging in vivo. The c-Met binding peptides are labelled via chelator conjugates. Also disclosed are pharmaceutical compositions, methods of preparation of the agents and compositions, plus methods of in vivo imaging using the compositions, especially for use in the diagnosis of cancer.

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: A cyclosporin derivative of general Formula (I) or a pharmaceutically compatible salt thereof, which have a pharmaceutical effectiveness, for example in the case of chronic inflammatory diseases. The cyclosporin derivatives are preferably free from a peptide section capable of passing through the membrane of a biological cell.

Abstract: Disclosed are compositions and methods useful for targeting tissue undergoing angiogenesis or to cells or tissue expressing ?v integrins. The compositions and methods are based on peptide sequences that selectively bind to and home to tissue undergoing angiogenesis or to cells or tissue expressing ?v integrins in animals. The disclosed targeting is useful for delivering therapeutic and detectable agents to tissue experiencing angiogenesis or to cells or tissue expressing ?v integrins.

Abstract: Factor H-binding peptides that binds to a region of factor H that does not impede the complement-inhibitory activity of factor H are disclosed. When immobilized onto the surface of a biomaterial, these peptides recruit factor H, resulting in a substantial inhibition of biomaterial-induced complement activation in a biological substance exposed to the biomaterial.

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.

Abstract: The subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.

Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.

Abstract: A method for measuring the proliferation status of a cell present in a biological sample, comprising the step of measuring in the said cell the loss of BACH2 by Fluorescence after In Situ Hybridization (FISH) analysis and mRNA quantification or by Comparative Genomic Hybridization (CGH) and corresponding kit and applications.