Abstract: Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

Abstract: The present invention is directed compounds for reversibly modification of biologically active molecules. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery conjugates. The use of reversible modification provides for physiologically responsive activity modulation.

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

Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Abstract: The invention describes compositions of peptide analogs 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 (SEQ ID NO: 76), wherein A is hydrophobic moiety or a metal binding moiety, e.g., a chemical group or moiety containing 1) an alkyl group having 6 to 36 carbon units, 2) a nitrilotriacetic acid group, 3) an imidodiacetic acid group, or 4) a moiety of formula (ZyHisw)p (SEQ ID NO: 50), wherein Z is any amino acid residue other than histidine, His is histidine, y is an integer from 0-6; w is an integer from 1-6; and p is an integer from 1-6; wherein if A has alkyl group with 6 to 36 carbon units x is greater than 0; 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. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.

Abstract: The present invention relates to a series of compounds useful for effecting purification, in particular for use in purification of synthetic peptides and proteins. The compounds of the invention are particularly efficient at securely anchoring peptides or proteins to a surface and allowing the peptide or protein to become uniformly orientated, thus ensuring that substantially all of the peptide or protein is available for molecular binding to a substrate.

Abstract: Described herein are CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates. Also disclosed are methods of using (e.g., to treat a disorder) the CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates.

Abstract: Conjugates comprising a N-oxime bond are disclosed. In one embodiment, a suitable conjugate is represented by the following Formula (I): wherein R? is derived from a compound comprising at least one reactive amide group, R? is derived from a compound comprising at least one reactive aminooxy group, and X is H, CnH(n+2) or other atoms. Additional methods are also provided.

Abstract: Methods for introducing fluorine atom onto a polypeptide are provided. Also provided are linkers, bioconjugates, and bifunctional compound agents made using the methods, linkers, and bioconjugates. The methods comprise: (i) providing a linker comprising a thiol-reactive terminus and an aldehyde-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a polypeptide comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the aldehyde-reactive terminus of the linker with a fluorine-substituted aldehyde.

Abstract: A liposomal composition, preferably a vaccine, comprising liposomes formed of liposome forming compounds, containing coentrapped polysaccharide antigen and T-cell dependent protein carrier, such as tetanus toxoid or diphtheria toxin modified to render it non-toxic. The invention is of use in the production of vaccines against Haemophilus influenzae, Streptococcus pneumoniae or Neisseria meningitidis.

Abstract: [Problems] To provide a polypeptide having a novel structure and showing an activity of inhibiting angiogenesis or an activity of inhibiting osteoclastogenesis, and to provide a recombinant protein by constructing a method of purifying the above protein. To provide an ingredient useful in designing remedies for tendinitis, rheumatoid arthritis, arthritis deformans, malignant tumor, etc. [Means for Solving Problems] A novel soluble polypeptide protein.

Abstract: Methods for making an immunogenic conjugate that includes a hapten or an antigen covalently linked to a carrier. The methods include reacting a first agent with a dihydrazide resulting in a hydrazine-modified first agent, wherein the first agent is a hapten, an antigen or a carrier; reacting a second agent with a benzaldehyde compound resulting in a benzaldehyde-modified second agent, wherein the second agent is a hapten, an antigen or a carrier, provided that the first agent or the second agent is a carrier; and reacting the hydrazine-modified first agent with the benzaldehyde-modified second agent resulting in an immunogenic conjugate comprising a hapten or an antigen covalently linked to a carrier via a hydrazone linkage.

Abstract: Peptides have been identified that bind to tooth enamel. Compositions and methods comprising peptide-based oral care reagents having at least one tooth enamel-binding peptide and an oral care benefit agent are provided to adhere the benefit agent to the oral surface.

Abstract: The disclosure provides methods and materials for improving the pharmacokinetic properties of drugs. For example, a construct is provided having a drug covalently joined to first and second ligands, or a drug covalently joined to a first ligand and a molecular weight increasing moiety. The ligands have affinity for binding partners, and in a physiological fluid, an equilibrium forms between bound and free forms of the construct. The constructs retain most of the drug's activity while simultaneously increasing half life.

Abstract: The present invention relates to the identification and functional characterization of human cell-penetrating peptides (CPPs) and their use; in particular as transfection vehicles.

Abstract: The present invention relates to antibodies raised against fragments of apolipoprotein B, in particular defined peptides thereof, for immunization or therapeutic treatment of mammals, including humans, against ischemic cardiovascular diseases, using one or more of the antibodies.

Abstract: There is described herein compounds comprising a mitochondrial penetrating peptide (MPP) conjugated to an antimicrobial, and their method of use.

Abstract: A method of labeling a sulfenic acid (—SOH) group of a cysteine residue in a protein; or peptide, comprises contacting said protein or peptide with a beta-ketoester to covalently couple said beta-ketoester to said cysteine residue and form a beta-ketoester-labeled cysteine residue in said protein or peptide.

Abstract: The present invention relates to methods and compositions for pretargeting delivery of therapeutic agents. In preferred embodiments, the pretargeting method comprises: a) administering a bispecific antibody with a first binding site for a disease-associated antigen and a hapten on a targetable construct; b) administering a targetable construct comprising at least one therapeutic agent. In preferred embodiments, the bispecific antibody is made by the dock-and-lock (DNL) technique. In a more preferred embodiment, the targetable construct comprises one or more SN-38 moieties.

Abstract: A cationic antimicrobial peptide (CAMP) conjugate is disclosed. The CAMP conjugate may be made by identifying a suitable carrier peptide; identifying a suitable antimicrobial agent; creating a conjugate by conjugating the peptide with the antimicrobial agent; and evaluating and refining the conjugate. The peptide may be short peptide based on the sequence of a CAMP, such as human ?-defensin-3. The peptide can be directly connected to the antimicrobial agent or through a linker segment. The antimicrobial agent may be connected to the peptide or the linker segment through stable or cleavable bonding. The peptide may carry and facilitate the delivery of the conjugated antimicrobial agent to a microbe.

Abstract: Disclosed are SPARC and albumin binding peptides for the targeting of disease sites, such as tumors, with therapeutic and diagnostic agents In particular, compositions comprising SPARC binding peptide—Antibody Fc domain fusion proteins and methods of their use are disclosed.

Abstract: The present invention relates to a novel synthesis of peptide-gold nanoparticle hybrid spheres comprising a step of forming a hybrid structure by inducing self-assembly of a gold-binding peptide, and forming a gold nanoparticle in the structure at the same time. According to the present invention, size of the structure can be controlled according to temperature, and it can be used for various biomedical and electronic applications using the structure.

Abstract: The present invention relates in general to labeling reagents useful for labeling biomolecules. In particular, the invention provides activated labeling reagents having the formula L-Ph, wherein L is an activated labeling molecule and Ph is a phenol. The invention further provides methods of preparing the labeling reagents, methods of using the labeling reagents for synthesizing a labeled biomolecule, kits that include reagents for labeling a biomolecule and kits containing labeled biomolecules.

Abstract: The present invention relates to a conjugate of chitosan and polyamine polymer that is useful for transferring a desired gene medicine into cells, and a method for preparing the same. In particular, the present invention relates to a double conjugate that is prepared by 1 in king poly-L-arginine to low molecular weight chitosan or triple conjugate that is prepared by additionally linking polyethylene glycol (PEG) to the double conjugate, and a method for preparing the same. The chitosan based cationic polymer conjugate of the present invention forms a complex with negatively charged gene medicine such as plasmid DNA and small interfering RNA to efficiently transfer the desired gene medicine into cells with low cytotoxicity. Accordingly, the conjugate can be used as an effective delivery system for in vivo administration of gene medicine.

Abstract: Derivatives of PSAs are synthesised, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems.

Abstract: A fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. Also, lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

Abstract: Methods of modulating interfacial characteristics in a self-assembled, force-transmitting peptide network at a fluid-fluid interface are disclosed. The methods involve exposing a peptide capable of participating in a self-assembled, force-transmitting peptide network, either before or after it interacts with other peptides to form the peptide network to a stimulus that alters the chemical and/or physical properties of the peptide. Use of such methods in applications such as emulsions and foams are also disclosed.

Abstract: The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptide moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.

Abstract: A method for processing animal-derived tissue and cross-linking animal-derived tissue is disclosed. Each method includes exposing or contacting the animal-derived tissue with a supercritical fluid.

Abstract: The invention relates to a method of modifying a specific lysine residue in a polypeptide comprising at least two lysine residues, said method comprising (a) providing a polypeptide comprising a target lysine residue protected by a first protecting group, and at least one further lysine residue; (b) treating the polypeptide to protect said further lysine residue(s), wherein the protecting group for said further lysine residues is different to the protecting group for the target lysine residue; (c) selectively deprotecting the target lysine residue; and (d) modifying the deprotected lysine residue of (c).

Abstract: Compositions and methods for making a composition comprising a polymer and one or more chelators covalently coupled to polymer, wherein the one or more chelators has a benzene ring with more than one hydroxyl group at any position that is free, or a derivative of the chelator, or a salt of the chelator and methods of use.

Abstract: The present invention relates to a method for producing a polypeptide.

Abstract: A method of one reaction step for synthesis of peptide template fluorescent metal nanoclusters as bioprobes. Specific targeting peptide containing a metal reactive group is synthesized and used to react with a metal salt solution under a sufficient pH condition at room temperature in forming peptide template fluorescent metal nanoclusters. The dialyzed metal nanoclusters is used directly as bio-probes.

Abstract: The present invention provides a process for attaching one or more effector molecules to one or more cysteines in a protein comprising: a) activating one or more cysteines in the protein by diafiltering the protein against a monothiol reducing agent or a multi-thiol reducing agent which is incapable of forming intramolecular disulphide bonds and b) reacting the treated protein with an effector molecule.

Abstract: The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to one of the fragments. The fragments are then coupled together in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to other fragments. The present invention is very useful for forming insulinotropic peptides such as Exenatide(1-39) and its natural and non-natural counterparts.

Abstract: Disclosed herein are novel antimicrobial peptides with useful, improved, or superior properties such as antimicrobial activity, specificity, resistance to degradation desirable levels of hemolytic activity, and therapeutic index against a broad range of microorganisms including gram-negative and gram-positive bacteria and other organisms having a cellular or structural component of a lipid bilayer membrane. Also provided are methods of making and using such peptides to control microbial growth and in pharmaceutical compositions for treatment or prevention of infections caused by such microorganisms. Certain peptides result from structure-based rational design relating to antimicrobial peptide V681, with single D-/L-amino acid substitutions or charged residue substitutions in or near the center of the peptide on the nonpolar or polar face. Some peptides contain one or more (or all) amino acids in the D configuration.

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 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 epi topes 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: Compositions comprising certain tripeptides which are capable of binding a metal in a square planar orientation, a square pyramidal orientation, or both, are disclosed in processes for modulating tagged peptides or proteins. Such compositions and processes may be used for site-specific chiral inversion of amino acids, site-specific peptide cleavage, and protein purification, among other uses.

Abstract: Scaffold comprises a polymer defining macropores and comprising hydroxypropylcellulose partially substituted by a substituent comprising a self-crosslinkable group, which is crosslinked through the self-crosslinkable group. The macropores have an average pore size larger than 50 microns and are at least partially interconnected. In one method, bicontinuous emulsion comprising a continuous aqueous phase and a continuous polymer phase is formed. The polymer phase comprises hydroxypropylcellulose partially substituted by a substituent comprising a self-crosslinkable group, and is crosslinked through the self-crosslinkable group to form a polymer defining at least partially interconnected pores. In another method, phase separation is induced in a solution comprising a polymer precursor and water to form a bicontinuous emulsion comprising a continuous polymer phase and a continuous aqueous phase.

Abstract: The invention relates to stabilized polypeptides having an IGF-1 or IGF-2 sequence and an E-peptide sequence, where the natural physiological cleavage of the E-peptide from the IGF is prevented.

Abstract: An inorganic nanoparticle array is self-assembled onto an unpatterned or patterned, peptide-functionalized substrate surface using peptide constructs comprising a substrate-binding peptide and a mineralization peptide.

Abstract: Provided are peptides imparting cell permeability to a lipid membrane structure and/or enhancing the cell permeability of a lipid membrane structure, and a lipid membrane structure which comprises, as a constituent lipid, a lipid bound to such a peptide and has cell permeability or shows enhanced cell permeability. The amino acid sequences of the peptides imparting cell permeability to a lipid membrane structure and/or enhancing the cell permeability of a lipid membrane structure are represented by: LX1X2X1X1X1L, LLX2X1X1X1L and LX1X2X1X1L (wherein L represents a leucine residue; X1 represents a polar amino acid residue; and X2 represents a polar, non-charged and branched chain amino acid residue).

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.

Abstract: Nanoparticles having a core and a corona of ligands covalently linked to the core, wherein differing species of peptides are bound to the nanoparticles and incorporated into various dosage forms.

Abstract: This application relates to peptide conjugates comprising peptides that suppress or otherwise inhibit an unwanted or undesirable immune response attached to lipid moieties, and methods for suppressing immune responses, including preventing, inhibiting, treating or decreasing unwanted or undesirable immune responses including autoimmune or allergic immune responses using these peptide conjugates.

Abstract: The present invention relates to novel compositions and methods for the generation of MHC class II compounds. Such methods are useful in identifying antigen-specific T cells, regulating an immune response and treating subjects suffering from an immune disorder.

Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.

Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

Abstract: Compounds of the formula (I) are disclosed: 18F—(CHR)n(CH2)mCHO??(I) in which n and m are independently 0 and 1 with at least one of n and m being 1, and R (if present) is a hydrogen atom or a methyl group, subject to the proviso that if n is 1 and R is methyl then m is 0. Synthesis of the compounds is described together with their use in radiolabelling reactions, e.g. for the radiolabelling of peptides to facilitate detection by Positron Emission Tomography (PET) imaging. The preferred compound is [18F]Fluoroacetaldehyde.