Abstract: A compound including a cell penetrating peptide (CPP), an elastin-like polypeptide (ELP), and a therapeutic peptide (TP) can be preferentially directed to a target site by applying hyperthermia. The compound can be useful for the treatment of tumors.

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: Novel biologically active compounds of the general formula (I) in which one of X and X? represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X? represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X? and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nuc

Abstract: This invention describes soluble, monovalent, non-natural protein molecules that can activate NK cells and certain T-cells to attack specific cellular target cells by attaching the NKG2D-binding portions of monovalent MICA or MICB protein, i.e. their ?1-?2 platform domain, to the intended target cell specifically. The ?1-?2 domain is contiguous with a heterologous ?3 domain that has been genetically modified to bind directly or indirectly to the extracellular aspect of the target cell, thereby serving as the targeting domain. The genetic modification to create a non-natural and non-terminal targeting motif within the ?3 domain can include a portion of an antibody, another protein molecule or portion thereof, a peptide, or a non-natural, modified ?3 domain of a MIC protein.

Abstract: The present invention relates to the Synthesis of Triterpenoid peptides and mechanism of action for Anti ageing and skin care. The present invention is directed towards anti-aging skin care compositions comprising peptides which are made by linking herbal actives to a pentapeptide for enhanced anti ageing activity by regenerating the dermal matrix. In detail, the present invention relates to the Synthesis of Triterpenoid peptides, providing an enhanced and synergistic activity for reducing the consequences of ageing such as appearance of fine expression lines and wrinkles on the skin by cosmetic modes of application. The Triterpenoid peptides of the present invention with its novel dual action mode can be used for skin ageing & collagen insufficiency. Its Triterpenoid group acts by preventing oxidation and excess activity of serine proteases like elastase and collagenase that result in wrinkling of skin.

Abstract: Reagents and methods for functionalizing polypeptides with moieties poly (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly (alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly (alkylene glycol) molecule and/or the glycan group.

Abstract: The invention is based on the discovery that the presence of a discordant helix in a protein or peptide is predictive of that protein or peptide's ability to form amyloid. The invention includes methods for detecting discordant helices and methods of screening for compounds that stabilize the ?-helix of a discordant helix-containing polypeptide. Compounds discovered using these methods are useful for treating or preventing disorders in which amyloid is produced. Such disorders include Alzheimer's disease and prion-associated disorders.

Abstract: Peptides useful in determining the presence of autoantibodies in patients suffering from rheumatoid arthritis are disclosed.

Abstract: The present invention provides isolated homogeneous polyfunctionalized proteins (e.g., erythropoietin), isolated glycopeptides, and a method for preparing polyfunctionalized peptides and/or proteins via cysteine-free native chemical ligation. In certain embodiments, the invention provides an isolated homogeneous polyfunctionalized protein having the structure (I). In certain other embodiments, the invention provides an isolated glycopeptide having Formula (II). In certain other embodiments, the inventive method is a method for preparing a polyfunctionalized peptide comprising a peptidic backbone made up of four or more amino acids, wherein two or more non-adjacent amino acids are independently substituted with a moiety having the structure (III) -LH. wherein A and L1 are as defined herein.

Abstract: Disclosed are surprising discoveries concerning the role of anionic phospholipids and aminophospholipids in tumor vasculature and in viral entry and spread, and compositions and methods for utilizing these findings in the treatment of cancer and viral infections. Also disclosed are advantageous antibody, immunoconjugate and duramycin-based compositions and combinations that bind and inhibit anionic phospholipids and aminophospholipids, for use in the safe and effective treatment of cancer, viral infections and related diseases.

Abstract: The present invention is directed to peptide amphiphile compounds, compositions and methods of use, wherein nanofiber bundling or epitope aggregation is inhibited. In certain embodiments, the peptide amphiphiles of the present invention have increased solubility and reduced nanofiber bundling. The molecules may be used in pharmaceutical applications, for example for in vivo administration to human patients, by increasing biological activity of the compositions toward neurite outgrowth and nerve regeneration.

Abstract: Therapeutic peptides having guanylyl cyclase C agonist activity are disclosed. The therapeutic peptides are analogues of the E. coli STa peptide with non-natural amino acid, isosteric or D-amino acid substituents. The therapeutic peptides are useful in the treatment of chronic ideopathic constipation, inflammatory bowel disease, and other diseases. Pharmaceutical compositions comprising the therapeutic peptides are also disclosed.

Abstract: The present disclosure provides polymer compounds binding with lipoamide produced by the reaction of the primary amine group of lipoamide with the carboxy group of polysaccharide compounds such as chondroitin sulfates, carboxymethyl celluloses, or hyaluronic acids; functional compounds such as peptides, proteins, growth factors; or drugs; or biocompatible polymers such as poly(ethylene oxide), poly(vinyl alcohol), or poly(vinyl pyrrolidone). The present disclosure also provides their synthesis methods, products of hydrogels and films using the same as and methods for manufacturing the products.

Abstract: A method for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.

Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.

Abstract: The invention provides compounds of the formula Poly-([SP-LI]n-PL-L2) including a collection of 152 peptides useful to create the compounds, and their uses thereof for the treatment of a variety of mammalian diseases. The compound, a novel ligand-targeted multi-stereoisomer peptide polymer conjugate, comprises two or more stereoisomer peptides and a peptide-ligand conjugated via linkers to a biocompatible hydrophilic polymer, preferably HPMA. The increased stability and solubility of the compound carrying the stereoisomer peptides and a peptide-ligand provide ideal pharmaceutical properties including the delivery by the polymer of the peptides into the target cells. The compounds of the invention are useful therapeutics for the treatment of a variety of mammalian diseases.

Abstract: This invention discloses a group of 298 peptides from which several peptides are independently selected and synthesized in their stereoisomer and chemically modified forms, and conjugated to a polymer via linkers creating novel anti-HIV-1 multi-peptide-polymer conjugate compounds for the treatment and prevention of HIV-1 infection. The peptides mimic the domains of major HIV-1 proteins, and therefore, they function as inhibitors of the targeted HIV-1 proteins. The polymer is a useful delivery system for the stereoisomer peptides, and certain peptides are peptide-ligands for targeted delivery into the HIV infected cells.

Abstract: Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.

Abstract: The invention provides a pharmaceutical composition including a peptide comprising at least a portion of a chemokine receptor or a G-protein coupled receptor and optionally a cytokine. The pharmaceutical composition of the invention may be used for altering immune system functioning, for example, to treat an immune system disorder, such as an autoimmune disease, multiple sclerosis, transplant rejection, psoriasis and asthma. The invention also provides peptides that may be used in the pharmaceutical composition and a method for preparing the pharmaceutical composition of the invention. The invention further provides a method for to treating an immune system disorder, such as an autoimmune disease, multiple sclerosis, transplant rejection, and psoriasis asthma.

Abstract: The invention relates to method for quantification of the absolute amount of allergen in an allergen sample comprising: a) providing a known amount of one or more allergen calibration standard peptide(s) having a sequence of amino acids which is identical with, and optionally unique for, a sequence to be found in the allergen to be quantified and optionally labelling said allergen calibration standard peptide(s), b) degrading the allergen sample to obtain a mixture of peptides, and optionally labelling said peptides with one or more labelling agent(s), wherein at least the peptides in the degraded allergen sample or the calibration standard peptides are labelled, and if both the peptides in the degraded allergen sample and the allergen calibration standard peptide(s) are labelled, the labelling agent(s) used for labelling the allergen calibration standard peptide(s) are different from the labelling agent(s) used for labelling the peptides of the degraded allergen sample, c) quantifying the absolute amount of

Abstract: Described herein are compositions and methods for inhibiting HIV integrase activity. Also described are methods of identifying agents that inhibit HIV integrase for use in treating or preventing HIV. Also disclosed are methods of identifying agents that inhibit HIV viral mutants that are resistant to integrase inhibitors.

Abstract: The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.

Abstract: This invention describes soluble, monovalent, non-natural protein molecules that can activate NK cells and certain T-cells to attack specific cellular target cells by attaching the NKG2D-binding portions of monovalent MICA or MICB protein, i.e. their ?1-?2 platform domain, to the intended target cell specifically. The ?1-?2 domain is contiguous with a heterologous ?3 domain that has been genetically modified to bind directly or indirectly to the extracellular aspect of the target cell, thereby serving as the targeting domain. The genetic modification to create a non-natural and non-terminal targeting motif within the ?3 domain can include a portion of an antibody, another protein molecule or portion thereof, a peptide, or a non-natural, modified ?3 domain of a MIC protein.

Abstract: Compounds of general formula I are used as labels in an electrochemical assay: (I) in which: Fc and Fc? are substituted or unsubstituted ferrocenyl moieties, X is a C1 to C6 alkylene chain which is optionally interrupted by —O— or —NH—; Y is a C1 to C6 alkylene chain which is optionally interrupted by —O— or —NH—; Z is a C1 to C12 alkylene chain which may optionally be substituted and/or may optionally be interrupted by —O—, —S—, cycloalkyl, —CO—, —CON R1—, —NR1CO— or —NR1— in which R1 represents hydrogen or C1 to C4 alkyl; and R is a linker group. Compounds I are used to make labelled substrates, as well as functionalised compounds for making the labelled substrates.

Abstract: The object of the present invention is to provide a novel thiosulfonate compound, a reversible cationization agent for protein and/or peptide, which can reversibly cationize a wider range of proteins and peptides with high stability of quality and accuracy and which are useful for a high degree of purification and recovery, as well as, a method for solubilization for protein and/or peptide using the agent. The present invention is a thiosulfonate compound having three or more cations derived from a quaternary ammonium group within one molecule.

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 said antibodies.

Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1, Chem. 2, Chem. 3 or Chem. 4; or a pharmaceutically acceptable salt, amide, or ester thereof.

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: 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: The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.

Abstract: The present invention relates to a process for producing N-alkyl-N-trialkylsilylamides from trialkylsilylhalides and N-alkylamides in the presence of a base and in the absence of a solvent.

Abstract: This invention concerns isotopically coded or non-isotopically coded affinity-tags for analysis of certain target molecules in complex samples, in particular for mass spectrometric analysis of proteomic samples. The affinity-tags have the following general formula X-SPACER-OPO3H2, wherein X is a functional group or moiety capable of reacting with a functional group of a protein, peptide, DNA, lipid, sugar and/or steroid. These phosphate affinity tags (‘PTAG’) are capable of high but reversible binding to metal-oxides like TiO2. Due to this property, tagged sample fractions can be isolated from non-tagged sample fraction by affinity chromatography. The binding of organophosphate to metal-oxides remains intact during multiple washings of preferably acidic solutions to remove non-specifically bound components. PTAG's are also envisaged wherein X is selected such that it is capable of binding proteins, peptides, nucleic acid molecules, lipids, carbohydrates, steroids and the like.

Abstract: Polypeptides labelled with a donor and acceptor pair of dyes selected from a dibenzorhodamine dye and a diamino-benzophenoxazine dye are peptide conjugates which are useful for intracellular and bead-based assays with fluorescence detection. Peptide conjugates with a caspase-recognition site undergo cleavage into peptide fragments which may be detected, located, and quantitated by the changes in fluorescence. Intracellular cleavage of peptide conjugates is correlated with apoptosis.

Abstract: The invention relates to ?-catenin targeting peptides comprising an a-helical segment that are optionally stapled or stitched, and pharmaceutical compositions thereof. Uses of the inventive ?-catenin targeting polypeptides including methods for treatment of disease, such as diseases associated with aberrant Wnt signaling, including cancer, are also provided.

Abstract: The present disclosure relates to novel vascular endothelial growth factor receptor (VEGFR)-binding polypeptides and methods for using these polypeptides to inhibit biological activities mediated by vascular endothelial growth factors (VEGFs). The present disclosure also provides various improvements relating to single domain binding polypeptides.

Abstract: The present invention relates to a conjugate of a protein or peptide with a polyethylene glycol derivative having catechol, wherein the protein or peptide is mono-PEGylated at the N-terminal with the polyethylene glycol derivative, and to a preparation method thereof. According to the invention, the catechol-PEG derivative can be site-specifically conjugated with the N-terminal amine group of a protein or peptide, so that a homogeneous polyethylene glycol-protein or -peptide conjugate can be obtained in high yield. Unlike a prior art conjugate, the conjugate obtained according to the invention allows the decrease in the activity of the protein to be minimized without chemically modifying the protein, and thus the conjugate has an excellent pharmacological effect. Also, because the conjugate is homogeneous, the process for preparing the conjugate can be simplified. Moreover, the conjugate has uniform biological efficacy in vivo and shows strong resistance to hydrolysis and thus a long in vivo duration time.

Abstract: A polymeric drug, in which a cancerostatic connected via spacers containing hydrolytically cleavable hydrazone bonds is bound to a water-soluble polymeric carrier prepared on the basis of a N-(2-hydroxypropyl)methacrylamide copolymer, wherein the structure of the polymeric drug consists of the main chain of N-(2-hydroxypropyl)methacrylamide carrying the cancerostatic and another chain of N-(2-hydroxypropyl)methacrylamide—a graft, which may also carry a cancerostatic, said grafts being bound to the main chain by a bond that is stable in the body and/or by a bond cleavable in the body, especially by an oligopeptide spacer selected from the series of GlyLeuGly (SEQ ID. NO. 1), GlyPheGly (SEQ ID. NO. 2), GlyPheLeuGly (SEQ ID. NO. 3) and GlyLeuPheGly (SEQ ID. NO. 4), and a method of its preparation.

Abstract: Neuropeptide analogs and compositions including neuropeptide analogs are described herein. Also provided are methods of producing and using the neuropeptide analogs and compositions including one or more neuropeptide analogs.

Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are functionalised BTMs useful in the method, as well as methods of preparing such functionalised BTMs under mild conditions.

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: Conjugates of a Factor IX moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided (among other things) are compositions comprising the conjugates, methods of making the conjugates, and methods of administering to a patient compositions comprising the conjugates.

Abstract: Conjugates of a GLP-1 moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-1 polymer conjugate may include a GLP-1 moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-1 polymer conjugate may include a GLP-1 moiety covalently attached to a water-soluble polymer, wherein the GLP-1 moiety possesses an N-methyl substituent.

Abstract: Provided are MUC18 targeting peptides which may be used, e.g., to therapeutically target B-1 lymphocytes to reduce the influence of these cells on the metastatic potential of melanoma cells and/or to target cancerous cells, including certain melanoma and leukemia cells. MUC18 targeting peptides may be comprised in fusion constructs, imaging constructs, and/or therapeutic constructs such as fusion constructs which may be used for diagnosing or treating a cancer.

Abstract: In general, the invention relates to novel bioactive pentapeptides from heat stabilized defatted rice bran having anti-cancer, anti-obesity, anti-Alzheimer and other health-promoting activities proteins. The bioactive pentapeptides can be incorporated into pharmaceutical, nutraceuticals and food compositions having at least the bioactive pentapeptide as an active ingredient.

Abstract: The present invention relates to short polypeptides (e.g., fewer than 19 amino acids in length) and longer polypeptides (e.g., 19 or more amino acids in length) having one or more D-amino acids as targeting moieties. These polypeptides, when conjugated to agents (e.g., therapeutic agents or transport vectors) are capable of transporting the agents across the BBB or into particular cell types. In particular, the short polypeptides can include one or more D-amino acids. These compounds are therefore particularly useful in the treatment of neurological diseases or diseases associated with particular cell types, organs, or tissues.

Abstract: Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.

Abstract: The invention provides pharmaceutical compositions and method for inhibiting growth of prostatic adenocarcinoma, stomach cancer, breast cancer, endometrial, ovarian or other cancers of epithelial secretion, or benign prostate hyperplasia (BPH). In one embodiment the pharmaceutical composition includes human rHuPSP94, antigenic portions thereof, and functionally equivalent polypeptides thereof. In another embodiment, the pharmaceutical composition includes a mixture of human rHuPSP94, antigenic portions thereof, and functionally equivalent polypeptides thereof and an anticancer drug which may be administered in an appropriate dosage form, dosage quantity and dosage regimen to a patient suffering from, for example of prostatic adenocarcinoma, stomach cancer, breast cancer, endometrial, ovarian or other cancers of epithelial secretion, benign prostate hyperplasia, or (BPH) gastrointestinal cancer.

Abstract: Dyes and photoluminescent compounds based on polymethine dyes that contain at least one alkyl-phosphonate or substituted alkyl-phosphonate group, including the synthetic precursors, methods of synthesis, and applications thereof. Certain embodiments include heterocyclic ring systems and polymethine linkage are selected such that the resulting polymethine dye is a cyanine dye, a merocyanine dye, or a styryl dye.

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.