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: Methods and compositions to reduce immunogenicity of proteins are disclosed. Compositions comprising therapeutic proteins (such as Factor VIII or any other protein or peptide) complexed with liposomes comprising PS and PC (PS liposomes), or comprising PS, PI and PC and, optionally, cholesterol (PS/PI liposomes) may be used.

Abstract: The present invention relates to a cyclic peptide compound, and a preparation method, pharmaceutical composition and use thereof. In particular, the cyclic peptide compound of the present invention has a structure as shown by general formula (I). The compound of general formula (I), and isomers, racemates, pharmaceutically acceptable salts, crystalline hydrates, solvates or mixtures thereof have a use in the preparation of medicaments for preventing or treating mammalian diseases associated with histone deacetylase dysregulations.

Abstract: Long-acting agonistic analogs for CLR/RAMP receptors are provided that have an extended half-live in vivo.

Abstract: Depression and PTSD are treated by administration of hCG, or an hCG analog, or a prodrug or metabolite of hCG or an hCG analog, in an amount equivalent to a subcutaneous dose of 50-200 IU, preferably 120-170 IU, more preferably 140-160 IU, of hCG per day.

Abstract: The present invention relates to a peptide derivative for regulating the thymic stromal lymphoid protein-mediated signaling and a pharmaceutical composition including the peptide derivative for preventing and treating allergy and asthma diseases and, more particularly, to a peptide derivative represented by Chemical Formula 1 and a pharmaceutical composition including the peptide derivative for preventing and treating allergy and asthma diseases. According to the present invention, provided are a peptide derivative capable of effectively inhibiting the formation of an inflammatory response of allergy and asthma diseases and a pharmaceutical composition including the peptide derivative. By using the present invention, various allergy and asthma diseases can be fundamentally prevented or treated.

Abstract: A method of making a skin care product that includes a skin care composition containing a skin care active with a diamagnetic susceptibility of between about ?400 and ?600, constructing an applicator for applying the skin care composition to a target portion of skin, and packaging the composition and applicator for retail sale. The applicator includes a magnetic array tailored to enhance penetration of the skin care active into skin. The magnetic array may be unidirectional magnetic array or a bi-directional magnetic array.

Abstract: The current disclosure provides methods for detecting and quantitating the 6-O-methylguanine-DNA methyltransferase protein (MGMT) directly in biological samples that have been fixed in formalin by the method of Selected Reaction Monitoring/Multiple Reaction Monitoring (SRM/MRM) mass spectrometry. Such biological samples are chemically preserved and fixed with formaldehyde containing agents/fixatives and may include formalin-fixed tissue/cells, formalin-fixed/paraffin embedded (FFPE) tissue/cells, FFPE tissue blocks and cells from those blocks, and tissue culture cells that have been formalin fixed and/or paraffin embedded. A protein sample is prepared from the biological sample and the MGMT protein is quantitated in the sample using SRM/MRM mass spectrometry by quantitating one or more fragment peptides.

Abstract: An instrument and method for accelerating the solid phase synthesis of peptides are disclosed. The method includes the steps of deprotecting a protected first amino acid linked to a solid phase resin by admixing the protected linked acid with a deprotecting solution in a microwave transparent vessel while irradiating the admixed acid and solution with microwaves, activating a second amino acid, coupling the second amino acid to the first acid while irradiating the composition in the same vessel with microwaves, and cleaving the linked peptide from the solid phase resin by admixing the linked peptide with a cleaving composition in the same vessel while irradiating the composition with microwaves.

Abstract: Naphthalimide compounds as used in tissue bonding and protein cross-linking applications. When activated by an activating agent, such as light in the 400-500 nm absorption range, the naphthalimide compounds form chemically-reactive species that cross-link proteins, bond connective tissues together, and bone tissues and other biomaterials together. A naphthalimide-labeled biomolecule, such as a naphthalimide-labeled chitosan, is also capable of bonding tissues without subsequent direct illumination of the contacted tissue area. The naphthalimide compounds may be used in tissue or arterial repair, stabilization of an expanded arterial wall after angioplasty, tethering pharmaceutical agents to tissue surfaces to provide local drug delivery, and for chemically bonding skin care products, sunscreens, and cosmetics to the skin.

Abstract: The present invention relates to a method for identification and quantification of carboxyethylated valine modified haemoglobin to assess the extent of diabetic complications.

Abstract: Selective inhibitor of c-Fos and their antiproliferative properties The invention relates to selective inhibitor of c-Fos for use in the prevention and/or treatment of cancers and restenosis.

Abstract: The invention relates to a method for preparing a composition for treating a tooth lesion, said composition comprising peptides that are capable of undergoing self-assembly at a certain pH. The compositions of the invention are highly suitable for being used in the medical field, in particular for remineralizing a tooth lesion such as a subsurface caries lesion.

Abstract: The invention provides methods of delivering pharmacologic agents linked to an internalization peptide, in which an inflammatory response inducible by the internalization peptide is inhibited by co-administration of an anti-inflammatory or by linking the internalization peptide to biotin or similar molecule. Such methods are premised in part on the results described in the examples whereby administration of a pharmacological agent linked to tat at high dosages is closely followed by an inflammatory response, which includes mast cell degranulation, histamine release and the typical sequelae of histamine release, such as redness, heat, swelling, and hypotension.

Abstract: The invention relates to a hemostatic composition in powder form comprising collagen of the fibrillar type comprising a content of fibrous collagen and/or fibrillar collagen of at least 70% by weight relative to the total weight of the collagen, and at least one monosaccharide, and optionally, at least one compound selected from coagulation factors and glycosaminoglycans. The invention further relates to a method for preparing such composition, and to a unit comprising such composition and a spraying device.

Abstract: A therapeutic agent delivery system includes a therapeutic agent delivery platform and a therapeutic guest agent. The therapeutic agent delivery platform is capable of being implanted in a tissue being treated. The platform includes a substrate and at least one host molecule coupled to the substrate. The therapeutic guest agent is capable of reversibly coupling with the host molecule when administered to the tissue being treated. The reversible coupling is defined by the binding affinity between the host molecule and the therapeutic guest agent. The therapeutic guest agent is delivered at a rate determined by the affinity release rate between the host molecule and the therapeutic guest agent. The degradation rate of the therapeutic guest agent may be slower than the affinity release rate between the host molecule and the therapeutic guest agent.

Abstract: A method for chemically modifying a peptide, derivative or analogue thereof is described. The method comprises contacting a peptide, derivative or analogue thereof with a fluoro-heteroaromatic compound to activate the peptide, derivative or analogue thereof. The activated peptide, derivative or analogue thereof is then contacted with a nucleophile or base to create a chemically modified peptide, derivative or analogue thereof.

Abstract: Disclosed herein are formulations, substrates, and arrays for amino acid and peptide synthesis on microarrays. In certain embodiments, methods for manufacturing and using the formulations, substrates, and arrays including one-step coupling, e.g., for synthesis of peptides in a C?N orientation are disclosed. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate.

Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.

Abstract: The invention relates to a method for determining the presence of at least one distinct polypeptide in a biological sample comprising contacting the biological sample with a hydrolyzing agent, wherein the hydrolyzing agent is capable of hydrolyzing the distinct polypeptide in a sequence-specific manner such that at least one distinct peptide having a predetermined peptide measured accurate mass would result if the at least one distinct polypeptide were present in the biological sample, to obtain a hydrolyzed sample; bringing the hydrolyzed sample in contact with a substrate comprising at least one immobilized binding partner, wherein the at least one immobilized binding partner is capable of specifically binding the distinct peptide; removing the hydrolyzed sample from the substrate in a manner such that the distinct peptide would remain bound to the immobilized binding partner; contacting the substrate with an elution solution, wherein the distinct peptide would dissociate from the immobilized binding partne