Abstract: Peptide aldehydes or ketone derivatives are particularly efficient for stabilizing subtilisin-type proteases in aqueous compositions such as liquid detergents, including peptide compounds with OH-substituted phenylalanine aldehyde as the C-terminal residue.

Abstract: Methods for improving the health of a female human or non-human animal are disclosed. The methods include the step of administering to the animal compositions including an effective amount of glycomacropeptide (GMP) for effectuating the methods. Specifically, the methods can be used to increase the rate of fat metabolism or fat oxidation, decrease percentage of body fat, increase the rate of bone mineralization, increase bone mineral content, increase bone mineral density, and/or increase bone strength in the animal. GMP-containing compositions can be used according to the disclosed methods to treat obesity and related metabolic conditions, or to treat or prevent osteoporosis, osteopenia, and other conditions related to loss of bone mineral content or bone strength.

Abstract: A polypeptide based block copolymer having biodegradability due to peptidase, a process for the preparation thereof, and polymer micelles using the same are provided. The block copolymer is a block copolymer of a polyethylene glycol-based compound having properties such that the solubility for water is different depending on the pH, but cannot form micelles due to a self-assembly phenomenon; and a polyglutamic acid-based compound formed using an aminolysis reaction of glutamic acid and tertiary amine in which the end of one alkyl group is substituted with NH2, or using an aminolysis reaction of glutamic acid and triamine.

Abstract: An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) or a salt thereof. In formula (I), Y represents a polypeptide containing an amino acid sequence set forth in SEQ ID NO.: 1 wherein 1 to 4 amino acids are substituted; X represents a methoxypolyethylene glycol; X? is absent or represents a methoxypolyethylene glycol; and a moiety represented by formula: La-Lb-[Lc]j represents a linker.

Abstract: Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs.

Abstract: Disclosed herein, in certain embodiments, is an HC•HA complex comprising hyaluronan and a heavy chain of I?I, wherein the transfer of the heavy chain of I?I is catalyzed by TSG-6. Further disclosed herein, in certain embodiments, is an HC•HA complex comprising hyaluronan and a heavy chain of I?I, wherein the transfer of the heavy chain of I?I is catalyzed by the TSG-6 like protein. Additionally, disclosed herein are methods of manufacturing said complex and methods of use thereof.

Abstract: Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.

Abstract: The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.

Abstract: Compounds comprising peptides and peptidomimetics capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds.

Abstract: Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.

Abstract: The invention provides a method of treating a subject having, or at risk of developing, a condition in which functioning of the small or large intestine is impaired, enhancing functioning or preventing damage to the small or large intestine in a subject, or ameliorating inflammation of the small or large intestine in a subject, comprising administering to the subject a GLP-1 receptor agonist. A GLP-1 receptor agonist may also be provided in a pharmaceutically acceptable form in an amount effective to treat or prevent conditions of the small or large intestine. Further, pharmaceutical compositions are provided for the treatment or prevention of conditions of the small or large intestine comprising a GLP-1 receptor agonist, together with a pharmaceutically acceptable carrier, excipient or vehicle.

Abstract: Disclosed are compositions and methods for decreasing the viscosity and/or cohesiveness of and/or increasing the liquefaction of excessively or abnormally viscous or cohesive mucus or sputum. The composition contains a protein or peptide containing a thioredoxin monocysteinic active site in a reduced state and optionally further contains a reducing system.

Abstract: Compounds of formula R1-A-NH—CH(R2)—CO—R3 are presented. The compounds can be used to treat or alleviate conditions associated with bone loss or low bone density, or to inhibit osteoclast differentiation and stimulation, bone resorption and/or loosening of a prosthetic device. The compounds can be administered as a pharmaceutical composition or in a prosthetic device.

Abstract: This invention relates to a topical gel drug product preparation containing a composition comprising an isolated polypeptide having a carboxy-terminal amino acid sequence of an alpha connexin (ACT peptide), peptide stabilizers, excipients, buffering agents, and the like. A formulation and preparation steps are disclosed for the manufacturing of a stable, elegant, and pourable topical gel. The resulting formulation possesses long term stability suitable for aesthetic as well as therapeutic applications including the prevention of scaring and accelerated healing of wounds. Methods for treatment of chronic wounds, including chronic ulcers, are also provided.

Abstract: Isolated peptides comprising sequences derived from the protein integrase of HIV-1, as well as their analogs, mixtures, conjugates with permeability enhancing moieties, and pharmaceutical compositions are disclosed. The peptides and compositions are capable of selectively killing HIV-1 infected cells and are used in treatment of HIV infection and AIDS.

Abstract: The invention relates to a method and a kit for preparing a radiopharmaceutical, the method comprising the steps: elution of a 68Ge/68Ga-Generator using hydrochloric acid as an eluent for obtaining a generator eluate comprising 68Gallium, feeding the generator eluate through a cation exchange cartridge, which collects the 68Gallium, separating the used eluent, eluting the 68Gallium from the cation exchange cartridge using a solution comprising sodium chloride and hydrochloric acid and feeding the resulting eluate into an aqueous precursor mixture comprising at least a labelling precursor thereby forming a reaction solution.

Abstract: The present invention relates to multimeric (e.g., dimeric, trimeric) forms of peptide vectors that are capable of crossing the blood-brain barrier (BBB) or efficiently entering particular cell types. These multimeric peptide vectors, when conjugated to agents (e.g., therapeutic agents) are capable of transporting the agents across the BBB or into particular cell types. These compounds are therefore particularly useful in the treatment of neurological diseases.

Abstract: The invention relates to bifunctional stapled or stitched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stitched peptides that bind to an effector biomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stitched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stitched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Uses of the inventive bifunctional stapled or stitched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.

Abstract: The present invention relates to novel tubulin binding molecules of formula (I) and their use for the treatment of cancer and other diseases.

Abstract: Methods of treatment or prophylaxis of bacterial vaginosis, prevention of recurrence of bacterial vaginosis and alleviation or prevention of symptoms or diagnostic criteria of bacterial vaginosis are provided. The methods include administration of an effective amount of a macromolecule comprising a polylysine, polyamidoamine, poly(etherhydroxyamine) or poly(propyleneimine) dendrimer and one or more sulfonic acid containing moieties attached thereto.