Abstract: The invention concerns vaccines comprising as an active principle an immunogen which is a cytokinetic factor or a cell regulating factor particularly transcriptional or another type of factor with immunosuppressive/apoptotic/angiogenic properties abnormally released in the extracellular (stromal) environment by cancer or stromal cells of malignant tumors, and a pharmaceutically acceptable carrier for inducing a systemic or mucosal immune response with secretory formation of class IgC or IgA neutralizing antibodies directed against the native factor, or which is derived from such a factor and the use of said immunogen to obtain a medicine for use as anticancer drug.

Abstract: The invention provides cell penetrating peptide-nucleic acid conjugates having the formula P-L-N, wherein P is a cell penetrating peptide, N is a nucleic acid, preferably an oligonucleotide and more preferably a siRNA, and L is a hydrophilic polymer, preferably a polyethylene glycol (PEG)-based linker linking P and N together. Compositions, methods of use and methods for producing such conjugates are also disclosed.

Abstract: The present invention relates to surface proteins of Moraxella catarrhalis and their ability to interact with epithelial cells via cell-associated fibronectin and laminin, and also to their ability to inhibit the complement system. These surface proteins are useful in the preparation of vaccines. The present invention also provides peptides interacting with fibronectin, laminin and the complement system.

Abstract: A method for site-specific modification of protein molecules includes providing a protein molecule having at least first and second non-terminal Cys residues at respective first and second sites within the protein molecule, providing a blocking molecule that is suitable to interact with the protein molecule to selectively block the second non-terminal Cys residue to prevent modifications of the second non-terminal Cys residue while leaving the first non-terminal Cys residue unblocked, and providing a Cys-modifying molecule that is suitable to modify the first non-terminal Cys residue. The blocking molecule according to an embodiment of the invention may be a protein molecule, DNA, an aptamer or synthetic organic molecules. The Cys-modifying molecule according to an embodiment of the invention may be a fluorophore, biotin, spin label, a sugar or a non-natural amino acid analogue.

Abstract: Pharmaceutical agents, compositions containing the same and methods for their use for enhancing the bioavailability and pharmacological efficacy of therapeutic peptides. The pharmaceutical agents have the formula Carrier-Linker-Peptide Wherein Peptide is a therapeutically active peptide species having the formula aan wherein n is the number of amino acid residues in the peptide and n is 2 to 40, Carrier is benzoyl, phenylacetyl, cinnamoyl, 3-OH-cinnamoyl, 3,4-OH-cinnamoyl, 3,4-dimethoxycinnamoyl, 3,4-methylenedioxycinnamoyl, 3-methoxycinnamoyl, 3,4-diethoxy-cinnamoyl, 3,4,5-trimethoxy-cinnamoyl, t-butoxycarbonyl, benzyloxycarbonyl, pivaloyl, N-9-fluorenylmethoxycarbonyl, fumaroyl and derivatives thereof and Linker is a C6 to C16 lipidic chain or a derivative thereof, an 8-amino-3,6-dioxaoctanoic acid or polymeric derivative thereof, pseudo peptide, or peptide mimic. Methods of use of compositions having the formula Carrier-Peptide wherein Carrier and Peptide are as just defined are also disclosed.

Abstract: The present invention relates to compositions and methods for obtaining (e.g., expressing, isolating and/or purifying) polypeptides capable of binding to and/or activating the guanylate cyclase C receptor.

Abstract: Disclosed herein are novel peptide amphiphile molecules and compositions discovered to possess improved solubility in aqueous buffers which, in turn, facilitates purification required for pharmaceutical applications, particularly for in vivo administration to human patients. In addition, gels of such peptide amphiphile compositions are shown herein to possess unexpectedly superior gelation kinetics and rheological properties, including an increased mechanical stiffness, which better mimics the mechanical properties of natural central nervous system tissues.

Abstract: Some embodiments relate to analogs of peptides corresponding to class I MHC-restricted T cell epitopes and methods for their generation. These analogs can contain amino acid substitutions at residues that directly interact with MHC molecules, and can confer improved, modified or useful immunologic properties. Additionally classes of analogs, in which the various substitutions comprise the non-standard residues norleucine and/or norvaline, are disclosed.

Abstract: Provided herein are methods for introducing fluorine atom onto a biomolecule comprising: (i) providing a linker comprising a thiol-reactive terminus and an azido/alkyne-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a biomolecule comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the azido/alkyne-reactive terminus of the linker with a fluorine-substituted azide or alkyne respectively. Also provided are compositions and method of synthesis of bifunctional linkers and bioconjugates as well as radio-diagnostic agents comprising fluorine-labeled biomolecules.

Abstract: The present invention features biarsenical molecules. Target sequences that specifically react with the biarsenical molecules are also included. The present invention also features kits that include biarsenical molecules and target sequences. Tetraarsenical molecules are also featured in the invention.

Abstract: The invention provides agents and vaccines for treating and diagnosing celiac disease. In particular, the present invention provides a combination of three peptides that are useful for treating and diagnosing celiac disease in a large proportion of patients.

Abstract: Disclosed herein are compositions and methods for generating ribo-nucleic neutral (RNN) or deoxyribo-nucleic-neutral (DNN) polynucleotides with reduced anionic charge, for improved intracellular delivery. Also disclosed herein are methods of using RNN and DNN compositions.

Abstract: Methods for producing biomolecule-polymer conjugates, such as polypeptide-polymer conjugates, include attachment of an initiator agent to a biomolecule and in situ polymerization of a polymer from defined sites on the biomolecule. The conjugates may have desirable pharmacological properties and may be used therapeutically.

Abstract: The invention discloses identification and therapeutic use of matrix metalloproteinase oligopeptides and peptidomimetics. The oligopeptides are used for making antibodies. The antibodies are used for diagnostic and treatment purposes of various diseases. In particular, the diseases may involve the mechanism of degradation of extracellular matrix by MMP's during cell proliferation cycle. Suppression of MMP activity seems to arrest tumor growth during cancer progression. MMP oligopeptides were used as vaccines to treat mice having murine melanoma B16FO induced tumor. There was a significant drop in tumor weight and size for the group of mice that were immunized with MMP oligopeptide.

Abstract: The present invention provides a process for producing a peptide thioester compound. The process involves: (A) forming a peptide by a solid-phase synthesis method using a resin modified with a linker represented by the formula (1) as a solid phase: wherein R1 represents C1-4 alkyl group, R2 represents hydrogen atom or C1-4 alkoxy group, and n represents an integer of 1 to 4; (B) cleaving a bond between the solid phase and the peptide with at least one acid selected from dilute hydrochloric acid, dilute sulfuric acid, formic acid, and acetic acid to produce a peptide having a carboxyl group at the C-terminus; and (C) reacting a thiol compound with the peptide at ?100 to 0° C. in the presence of a condensing agent in a solvent.

Abstract: The invention relates to the fields of materials sciences and medicine and relates to an agent, which can be used, for example, as a contrast medium for the localization of cancer cells. The object of the present invention is to disclose an agent which sensitively and selectively recognizes the site and the type of the molecules or cells to be examined. The object is attained through an agent composed at least of bio-shuttle molecules to which endohedral fullerenes are coupled by way of peptide-based molecules, wherein the endohedral fullerenes are hydrophobic and correspond to the formula A3-xMxZ@C2n in which x=0 to 3 and n?34, A means rare earths and/or transuranic elements, M means metals, Z means non-metals and C means carbon. The object is further attained through a method in which hydrophobic endohedral fullerenes are coupled with bio-shuttle molecules by way of an irreversible Diels-Alder reaction with an inverse electron demand (DARinv).

Abstract: This invention provides novel active agents (e.g. peptides, small organic molecules, amino acid pairs, etc.) peptides that ameliorate one or more symptoms of atherosclerosis and/or other pathologies characterized by an inflammatory response. In certain embodiment, the peptides resemble a G* amphipathic helix of apolipoprotein J. The agents are highly stable and readily administered via an oral route.

Abstract: The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilizing microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Abstract: According to the present invention, it is possible to provide a novel cell penetrating peptide that transports proteins into cells and/or into nuclei at higher frequency than conventional cell penetrating peptides, and a pharmaceutical containing the peptide.

Abstract: The present invention relates to a method of preparation of a solid substrate capable of immobilizing at least one cell and/or at least one part of a cell, said method comprising a step consisting of fixing, to said solid substrate, a fusogenic compound capable of being inserted in cell membranes. The present invention also relates to a method for immobilizing at least one cell and/or at least one part of a cell using the solid substrate thus prepared, said solid substrate and its uses in the area of biomedical diagnostics or health monitoring of biological fluids or intended for human or animal use.

Abstract: The present invention provides isolated methylated Tat peptides; and compositions comprising the peptides. The present invention further provides isolated antibodies specific for a Lys-51-methylated Tat polypeptide. Also provided are methods of identifying agents that inhibit Lys-51 methylation of a Tat polypeptide. The present invention further provides methods of treating an immunodeficiency virus infection in a mammalian subject.

Abstract: Bis-diazo, triaryl and aryldiazo-N-arylphenazonium quencher moieties, substituted with electron-withdrawing and electron-donating substituents which induce polarity in the delocalized aryl/diazo ring systems, are useful as labels when attached to biomolecules such as polynucleotides, nucleosides, nucleotides and polypeptides. The quencher moieties are non-fluorescent and accept energy transfer from fluorescent reporter labels by any energy-transfer mechanism, such as FRET. Fluorescence quencher compositions are useful in preparing quencher labeled biomolecules for various molecular biology assays based on fluorescence detection.

Abstract: The invention provides a method for introducing 1,4,7,10-tetraazacyclododecane-N,N?,N?,N??-tetraacetic acid (DOTA) into a compound such as a peptide. The method comprises a first step for preparing a mixed liquid of DOTA having no protecting group and dimethylsulfoxide, and a second step for contacting the mixed liquid with the compound carried on a solid-phase carrier.

Abstract: The invention relates to marker molecules for identifying physical properties of molecular species separated by the use of electrophoretic systems. The invention further relates to methods for preparing and using marker molecules.

Abstract: Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, [Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.

Abstract: A polypeptide dimer is provided wherein both protomers have a sequence according to SEQ ID NO: 1 and at least one phosphocholine derivative is attached to the polypeptide. The polypeptide shows a specific binding for C-reactive protein (CRP). The utilization of the polypeptide in assays for determining the concentration of CRP is described. The purification of CRP, and compositions comprising the CRP also are provided.

Abstract: A novel polyoxyalkylene derivative represented by the following formula (1), wherein each symbol is as defined in the specification, which has a functional group capable of reacting with various physiologically active substances according to the object is provided.

Abstract: Methods and systems to generate 6-amino-6-deoxy-D-luciferin precursor, 2-cyano-6-aminobenzothiazole and related compounds and derivatives

Abstract: The invention relates to the preservation of an active agent, such as a polypeptide, by contacting the active agent with a preservation mixture including a sugar and polyethyleneimine.

Abstract: Nanoparticles can include a core linked to a polymerizable moiety that can be polymerized, cross-linked or cured. The polymerizable nanoparticles can be included in a composition for a polymerization, cross-linking or curing reaction in an amount and disposition sufficient for inhibiting or preventing volume shrinkage during polymerization, cross-linking or curing reaction. Also, the nanoparticles can be included with monomers, dendrimers, oligomers or polymers in the compositions that can be reacted to form a polymerized, cross-linked or cured product.

Abstract: The use of lipopeptides as inducers of NF-?B for the protection of mammals from the effects of apoptosis is described.

Abstract: A substantially hydrophilic conjugate is provided having a peptide that is capable of passing the blood-brain barrier covalently linked to a water-soluble nonpeptidic polymer such as polyethylene glycol. The conjugate exhibits improved solubility and in vivo stability and is capable of passing the blood-brain barrier of an animal.

Abstract: A method of use of a cysteine labeling system includes: providing a 2-cyano benzothial core with a covalently-linked biomolecule X in a reaction environment; and reacting the 2-cyano benzothial core to an N-terminal cystenine.

Abstract: The invention relates to methods and compositions for causing the selective targeting and killing of tumor cells. The present invention describes prophylactic or therapeutic cancer vaccines based on purified TAA proteins or TAA-derived synthetic peptides altered by chemical, enzymatic or chemo-enzymatic methods to introduce ?Gal epitopes or ?Gal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-?Gal antibodies to stimulate TAA capture and presentation, thereby inducing a humoral and cellular immune response to the TAA expressed by a tumor. The animal's immune system thus is stimulated to produce tumor specific cytotoxic cells and antibodies which will attack and kill tumor cells present in the animal.

Abstract: The present invention is directed stromal cell derived factor-1 peptides that have been mutated to make them resistant to digestion by the proteases dipeptidyl peptidase IV (DPPIV) and matrix metalloproteinase-2 (MMP-2) but which maintain the ability of native SDF-1 to attract T cells. The mutants may be attached to membranes formed by self-assembling peptides and then implanted at sites of tissue damage to help promote repair.

Abstract: The invention relates to an isolated, synthetic or recombinant ?-conotoxin peptide having the ability to inhibit a neuronal amine transporter, nucleic acid molecules encoding all or part of such peptides, antibodies to such peptides and uses and methods of treatment involving them.

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: This invention pertains to the surprising discovery that salicylanilides, e.g., niclosamide and/or niclosamide analogues can be reacted with a therapeutically active peptide to produce a modified peptide complex that shows increased resistance to proteolysis and that shows higher bioactivity when orally administered than the unmodified peptide.

Abstract: The present invention provides novel 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. In various embodiments, the peptidomimetic macrocycles are of Formula I: The linker L includes a triazole moiety. Peptidomimetic macrocycles according to the invention may exhibit increased ?-helical or beta sheet structure in aqueous solution compared to a corresponding non-macrocyclic polypeptide.

Abstract: Biomedical devices with antimicrobial coatings are provided. One or more surfaces of the device are coated with a cationic peptide, cationic proteins, or mixtures thereof to impart antimicrobial properties to the surface.

Abstract: The present invention discloses a process for making an insulin-oligomer conjugate as a one-pot reaction by conjugation of insulin-ester with an activated oligomer wherein simultaneous deblocking and conjugation is carried out.

Abstract: The present invention relates to methods and compositions for modifying, isolating, detecting, visualizing, and quantifying citrulline and/or homocitrulline-containing peptides, polypeptides, and proteins using mono- and disubstituted glyoxal derivatives. The invention also provides kits for modifying, isolating, detecting, visualizing, and quantifying the relative amounts of citrulline and/or homocitrulline-containing peptides, polypeptides, or proteins in solutions or samples.

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: The present invention is directed to truncated dockerin polypeptides, recombinant polypeptides and affinity systems comprising the truncated dockerin polypeptide, methods of generating same, and methods of use thereof to purify, isolate, and detect molecules of interest.

Abstract: The present invention relates to new amphiphilic polymers comprising hydrophobic groups and methionine groups. It also relates to compositions with a controlled release profile comprising such polymers, non-covalently combined with an active ingredient, in particular an active ingredient such as a peptide or a protein comprising in their sequence at least one amino acid which is sensitive to oxidation.

Abstract: The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.

Abstract: The present invention relates to a method of improving the resistance of a peptide or peptidomimetic to degradation by trypsin which comprises incorporating into said peptide or peptidomimetic a C-terminal capping group of formula (I): X—Y—Z (I) wherein X is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from —Ra—Rb—, —Ra—Rb—Rb,- and —Rb—Rb—Ra— wherein Ra is C, O, S or N, and Rb is C; each of Ra and Rb, may be substituted by C1-C4 alkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z. moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ra or Rb of Y and a non-hydrogen atom of one of the cyclic groups of Z.

Abstract: This disclosure provides peptides, polypeptides, fusion polypeptides, compositions, and methods for enhancing or increasing the stability of a polypeptide (e.g., Taq polymerase). Such peptides, polypeptides, fusion polypeptides, or compositions include polypeptides linked to a peptide tag that enhances the stability of the polypeptide. The peptides, polypeptides, fusion polypeptides, compositions may also enhance the activity, specificity, and/or fidelity of other polypeptides in a reaction mixture. The disclosure also provides methods of using such peptides, polypeptides, fusion polypeptides, compositions.

Abstract: The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.

Abstract: The invention describes compositions of peptide analogs exemplified by peptides derived from vasopressin, terlipressin, and GLP1 and others that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide, wherein A is a hydrophobic moiety or a metal binding moiety, and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. A may be linked to Cm by a linker group. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.