Abstract: A process for the total synthesis of Distamycin, and synthetic poly-(4 aminopyrrole-2-carboxamide) congeners thereof, using 1-methyl-4-forinylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate, is provided. The process finds application for both in solution and solid support synthetic technologies.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae (I), wherein Z is a template-fixed chain of 7 to 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 of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: The invention concerns a method for binding, in solution, at least a peptide composition and at least a lipophilic vector bearing an aldehyde function, the coupling comprising a step which consists in producing a hydrazone bond between the peptide compound and the lipophilic vector. The invention also concerns lipophilic vectors for use in this method, lipopeptides obtained by this method, uses of the lipopeptides for cell screening, and the applications of the invention, in particular for preparing targeting of an active principle of the peptide kind (for example hormone or neuropeptide) through physiological barriers such as cell membranes.

Abstract: Stable insulin formulations can be prepared by mixing a monomeric insulin and a soluble acylated insulin analog.

Abstract: The purpose of this invention is: new selenohydroxy acid compounds and their derivatives; their process for the preparation; use of the new compounds as precursors of L(+)-selenomethionine and/or source of selenium in human or animal nutrition, in cosmetics and pharmaceutics; and nutritional, cosmetic and pharmaceutical compositions containing them.

Abstract: A novel peptide found as gonadotropin-releasing hormone (GnRH) in octopuses, a member of mollusks. The structure and the activities of the peptide have been unraveled. The peptide finds use as a reagent used in the studies of correlations between the structure and the activities of GnRH and the information processing mechanisms of the nervous systems in higher animals. It can also serve as a base compound in the development of pesticides and drugs. The peptide has the GnRH activity and has the following amino acid sequence (I): <Glu-Zaa-Zaa-His-Zaa-Ser-Zaa-Zaa-Zaa-Zaa-Pro-Gly-NH2 (SEQ ID NO: 7) ??(I) wherein <Glu represents pyroglutamic acid and Zaa represents any amino acid. Specifically, the peptide has the following amino acid sequence (1): <Glu-Asn-Tyr-His-Phe-Ser-Asn-Gly-Trp-His-Pro-Gly-NH2 (SEQ ID NO: 1) ??(1) wherein <Glu represents pyroglutamic acid.

Abstract: Aplidine and aplidine analogues are used in the manufacture of a medicament for treating multiple myeloma.

Abstract: The present invention provides methods and agents for treating subjects who have or are at risk of developing or having cardiovascular disease. Such agents inhibit binding of myeloperoxidase (MPO) to a molecule comprising the MPO binding site of apolipoprotein A-1 (apoA-1) and include a peptide fragment of apoA-1 comprising at least 4 contiguous amino acids in SEQ ID. NO: 2, a modified form of the apo-1 fragment comprising one or more D amino acids, a retro-inverso form of the apoA-1 peptide fragment, an organo-mimetic of the apoA-1 peptide fragment, a peptide-mimetic of the apoA1 peptide fragment, or a nucleic acid encoding the apo A-1 peptide fragment. The present invention also provides methods of identifying or screening test agents for treating subjects having or at risk of having or developing CVD.

Abstract: Disclosed is a composition of matter comprising a defined dispersion of lactoferria immobilized on a naturally occuring substrate via the N-terminus region of the lactoferrin. Compositions comprising immobilized lactoferrin (Im-LF) are used in a method for reducing the microbial contamination of a composition subject to microbial contamination, which is also disclosed, and which encompasses a method for reducing the microbial contamination of a foodstuff, such as a meat product. Foodstuffs treated by the method are disclosed, including meat products. A method of inhibiting the growth and/or adhesion of a microbial species on a food-contacting surface f a material for food packaging or food handling with Im-LF is also disclosed. Food containers and food-handling implements so treated are also disclosed, as are antimicrobial cleansers, polishes, paints, sprays, soaps, or detergents containing Im-LF for applying to an inanimate surface.

Abstract: The present invention relates to a composite for the treatment of a variety of medical conditions, the composite comprising an oxidized glutathione-based compound, which has a disulfide bond, and a metal material, in particular where the metal is either platinum or palladium. The oxidized glutathione-based compound and metal material can be present in a ratio of 3000 to 1 and preferably 1000 to 1. The oxidized glutathione-based compound can be oxidized glutathione itself or salts or derivatives. A feature of the invention is that the composite has a more stabilized disulfide bond than the oxidized glutathione-based compound itself. Methods for preparing the composite are provided, such methods being beneficial in that the composite is provided in high yields and at high purity. Methods for treating various medical conditions with the composites of the present invention are also disclosed.

Abstract: The invention relates to a compound comprising a labeled nickel complex (FIG. 1) that is used to detect and purify nucleic acid sequences by forming an adduct between a specific nucleic acid base and the labeled nickel complex.

Abstract: The present disclosure teaches analogs of human chemokines and methods of using them in the prevention, treatment, and ameliorization of diseases that can benefit from therapeutic angiogenesis. The teachings are generally directed to compositions comprising SDF-1 mimetics, as well as methods that include the use of SDF-1 mimetics to induce neo-vessel formation. The disclosure also teaches articles of manufacture that can be useful in practicing the methods taught herein.

Abstract: The subject invention provides novel peptides for use in treating mammals to control appetite and obesity. Disclosed is a peptide derivative having the formula: X1-Z-Q-arg-trp-NH2 wherein: X1 is an acyl group, Z is amino-2-naphthyl-carboxylic acid or histidine, Q is (D)phenylalanine or p-iodo-(D)phenylalanine, or a pharmacologically acceptable salt, complex or derivative thereof, the peptide derivative having melanocortin-4 receptor agonist activity.

Abstract: A pharmaceutical composition is disclosed which comprises a solid dispersion of an HIV protease inhibitor in a water soluble carrier, such as PEG, having enhanced bioavailability and improved dissolution properties. The solid dispersion may optionally be encapsulated in hard gelatin capsules, compressed into a tablet, or may be granulated with a pharmaceutically acceptable granulating agent. Also disclosed are methods of making said solid dispersion and methods of treating an HIV infection employing said solid dispersion.

Abstract: Described are methods for electrical treatment of biological cells, in particular using electrical field pulses, involving the steps: arrangement of the cells (1) on apertures (2) of a solid planar carrier element (3) which divides a measuring chamber (10) into two compartments (11, 12); and temporary formation of an electrical treatment field which permeates the cells, wherein an alternating-current impedance measurement takes place on the carrier element (3), and from the result of the alternating-current impedance measurement, a degree of coverage of the carrier element and/or healing of the cells after electrical treatment are/is acquired. Also described are devices for implementing the methods.

Abstract: Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.

Abstract: The invention relates to anti-microbial and immunostimulatory molecules of the cathelicidin family derived from fish. The invention provides a novel cathelicidin molecule, fragments, derivatives and uses thereof, and nucleic acids encoding the same.

Abstract: The invention relates to aplidine derivatives of the general formula: which are useful for the treatment of tumors.

Abstract: The present invention provides methods of treating a lymphoma (e.g.

Abstract: Peptide inhibitors of glycogen synthase kinase-3 (GSK-3) having an amino acid sequence motif of XZXXXS(p)X, wherein S(p)=phosphorylated serine or phosphorylated threonine, X=any amino acid, and Z=any amino acid except serine or threonine. These inhibitors, which are about 7 to 20 amino acids long, are specific for GSK-3 and strongly inhibit the enzyme with an IC50 of about 150 ?M. Also provided are methods of treating biological conditions mediated by GSK-3 activity, such as potentiating insulin signaling in a subject, treating or preventing type 2 diabetes in a patient, and treating Alzheimer's Disease by administering peptide inhibitors. Compositions of these peptide inhibitors and pharmaceutically acceptable carriers are also provided, as is a method for identifying inhibitors of GSK-3. The invention further relates to a computer-assisted method of structure based drug design of GSK-3 inhibitors using a three-dimensional structure of a peptide substrate of GSK-3.