Abstract: Provided herein are a novel class of oligopeptides and prodrugs that include amino acid sequences containing cleavage sites for fibroblast activation protein (FAP). Also provided herein are methods of treating FAP related disorders, including cancer.

Abstract: The present invention identifies biomarkers that are diagnostic of nerve cell injury, organ injury, and/or neuronal disorders. Detection of different biomarkers of the invention are also diagnostic of the degree of severity of nerve injury, the cell(s) involved in the injury, and the subcellular localization of the injury.

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

Abstract: The invention relates to a new method of preparation of a hyaluronan derivative with an aldehydic group in the position (6) of the polysaccharide glucosamine part. The hyaluronic acid oxidation can be performed by means of TEMPO/NaCIO or TEMPO/TCC systems in a protic environment with or without the presence of anorganic salts. Thus prepared aldehyde can be used for binding amines, diamines, amino acids, peptides and other compounds containing an amino group, e.g. by means of the reductive amination with NaBH3CN in water or in a water-organic solvent system. When a diamine or compounds containing three or more amino groups are used, cross-linked hyaluronan derivatives can be prepared. Cross-linked derivatives can be also prepared by a reaction of the aldehyde with a hyaluronan substituted by an amino-alkyl group HA-alkyl-NH2.

Abstract: The present invention relates to novel methods of making soluble proteins having free cysteines in which a host cell is exposed to a cysteine blocking agent. The soluble proteins produced by the methods can then be modified to increase their effectiveness. Such modifications include attaching a PEG moiety to form pegylated proteins.

Abstract: A palladate palladium-promoted hydrolytic polypeptide cleavage process which selectively cleaves the polypeptide at a Cys-His cleavage site comprising solubilizing the polypeptide in a reaction mixture comprised of a palladate palladium promoter dissolved in a high-concentration acidic organic acid solvent.

Abstract: The present invention relates to the therapeutic application of the Kazal-type serine protease inhibitor Infestin or domains thereof or modified Kazal-type serine protease inhibitors based on Infestin homologs, which prevent the formation and/or stabilization of three-dimensional arterial or venous thrombi by interfering with proteins involved in activation of the so-called intrinsic coagulation pathway. The present invention also relates to the use of Kazal-type serine protease inhibitors or fragments thereof or modified Kazal-type serine protease inhibitors in the treatment or prophylaxis of a condition or disorder related to arterial thrombus formation, i.e. stroke or myocardial infarction, inflammation, complement activation, fibrinolysis, angiogenesis and/or diseases linked to pathological kinin formation such as hypotonic shock, edema including hereditary angioedema, bacterial infections, arthritis, pancreatitis, or articular gout, Disseminated Intravasal Coagulation (DIC) and sepsis.

Abstract: Dermatological and cosmetic compositions and methods are provided to reduce the appearance of biological and/or environmentally-caused aging.

Abstract: The present invention provides monodisperse primary carbon nanoparticles, and methods of preparation and use thereof. In particular, the present invention provides surface-modified monodisperse primary carbon nanoparticles, and methods of preparation and use thereof.

Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of ?-amino boronic acid derivatives.

Abstract: A method for producing a radioactively marked peptide, uses a precursor molecule that is prepared in an organic solvent. A radioactively marked compound having a carboxyl function is added. The carboxyl function is activated, and the activated radioactively marked compound is bonded to the precursor molecule in order to form the radioactively marked peptide. The radioactively marked compound is an isocyanocarboxylic acid. A radioactively marked isocyanocarboxylic acid is used for producing a radioactively marked peptide.

Abstract: The invention comprises peptidyl analogs according to formulae (I) or (II) as depicted below: (R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13- A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25- A-26-A27-A28-R1 wherein the definitions of A1 to A28 and R1 to R3 are provided for in the specification for each of formulae (I) and (II), pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of a compound of formula (I), that possess agonist or antagonist ghrelin activity, along with therapeutic and non-therapeutic uses thereof.

Abstract: The present invention is directed to an inventive polymeric carrier molecule according to generic formula (I) and variations thereof, which allows for efficient transfection of nucleic acids into cells in vivo and in vitro, a polymeric carrier cargo complex formed by a nucleic acid and the inventive polymeric carrier molecule, but also to methods of preparation of this inventive polymeric carrier molecule and of the inventive polymeric carrier cargo complex. The present invention also provides methods of application and use of this inventive polymeric carrier molecule and the inventive polymeric carrier cargo complex as a medicament, for the treatment of various diseases, and in the preparation of a pharmaceutical composition for the treatment of such diseases.

Abstract: Methods for generating an Ac-225 radioconjugate comprising a monoclonal antibody (mAb) (IgG) is disclosed. The Ac-225 radioimmunoconjugate is an [Ac-225]-p-SCN-Bn-DOT AIHuM195 radioimmunoconjugate.

Abstract: Elastin-like polypeptide (ELP) serves as a vector for thermally-targeted delivery of therapeutics, including cytotoxic chemotherapeutic drugs such as doxorubicin. Examples of an ELP-based delivery vehicle can comprise: (1) a cell penetrating peptide, such as a Tat peptide, (2) ELP, and (3) the lysosomally degradable glycylphenylalanylleucylglycine (GFLG) (SEQ ID NO: 3) spacer and a cysteine residue (SEQ ID NO: 4) conjugated to therapeutic such as doxorubicin, or an analog thereof.

Abstract: Disclosed herein are methods and compositions relating to the detection and measuring of kinetic binding interactions.

Abstract: Methods and reagents for site-selective functionalization of peptides and proteins. The methods most generally involve the reaction of a thioester with hydrazine. Reagents include bifunctional reagents of formula: H2N—NH—CH2-M-L-FG and salts thereof where M is a single bond or a chemical group carrying a non-bonding electron pair, such as —C(O)NR?—, where R? is H, or an alkyl or aryl group; L is an optional linker group as described above; and FG is a functional group having reactivity that is orthongonal to that of the hydrazine group. FG can, among others, be an azide, alkenyl, alkynyl, nitrile (—CN) or triazole group and is preferably an azide group (—N3). Methods and reagents can, for example, be combined with intein-mediated protein splicing to link proteins or fragments thereof to various chemical species or to a surface.

Abstract: The invention concerns a method for producing an aqueous albumin solution from a starting albumin solution which contains stabilizer molecules which are capable of occupying binding sites of the albumin, wherein in a method for increasing the albumin binding capacity (ABiC) for other molecules, at least a portion of the stabilizer molecules is removed from the albumin of the starting albumin solution and separated from the starting albumin solution.

Abstract: The present invention generally relates to methods and compositions for generating vancomycin analogs. Specifically the invention relates to generating a vancomycin library through chemoselective ligation of a sugar moiety with a vancomycin aglycon. In particular, the present invention provides a library of vancomycin analogs, where the member of the library comprises at least one vancomycin analog selected from 2?-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 3?-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 4?-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 6?-N-acyldecanoyl-glucosyl vancomycin neoglycoside, 2?-N-acylbiphenyl-glucosyl vancomycin neoglycoside, 3?-N-acylbiphenoyl-glucosyl vancomycin neoglycoside, 4?-N-acylbiphenoyl-glucosyl vancomycin neoglycoside and 6?-N-acylbiphenoyl-glucosyl vancomycin neoglycoside.

Abstract: A method is disclosed for the syntheses of thiol-containing radiopharmaceuticals without the need for purification starting from chelators containing disulfide bonds. This is done by providing a method that reduces disulfide bonds on a precursor molecule or a precursor compound in the presence of phosphine compounds, thus freeing thiols for metal complexation.

Abstract: A process for chemically converting a peptide chain into a peptide thioester includes, when a —C(?X)—R1 group is introduced to the thiol group of the cysteine residue and then the resulting peptide is reacted with a compound having a leaving group represented by the formula: —NH—C(?Y)NHR3 in an organic solvent, the —NH—C(?Y)NHR3 group binds via addition reaction to the carboxyl group of the N-terminal-side peptide bond of the cysteine residue, whereby the peptide bond is cleaved and the C-terminal-side peptide fragment is cut off. Further, when the resulting peptide chain having the —NH—C(?Y)NHR3 group is reacted with a thiol in a buffer solution, a thiol exchange reaction occurs, namely, the thiol group of the thiol binds to the carbonyl carbon to which the —NH—C(?Y)NHR3 group has bound, whereby the —NH—C(?Y)NHR3 group is eliminated.

Abstract: Substituted tricyclic diproline analogues of the formula (I): wherein the variables are as defined herein. Also disclosed are methods for the production thereof, the use thereof for the induction of an alpha-helix conformation in peptides and/or proteins, pharmaceuticals containing said compounds, methods for the production of a peptide library containing said compounds, and peptide libraries containing said compounds.

Abstract: The invention relates to novel citrulline peptides derived from fibrin ? and ? chains which are recognizable by specific citrulline antiprotein autoantibodies (AAPC) of a rheumatoid arthritis (PR) and to the use thereof for detecting the presence of said specific PR AAPC in a biological sample.

Abstract: The present invention includes compositions and methods for the isolation, separation and chelation of Carbon Nanotubes (CNTs) using a cyclizable peptide.

Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.

Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.

Abstract: The present invention relates to a peptide aptamer which mimics particularly the human platelet antigene HPA-Ia epitope present on the platelet GPIIb/IIIa molecules and which is capable of neutralizing the binding of HPA-I a specific antibodies (anti-HPA-1 a). This peptide aptamer is advantageously used in a method for detecting and identifying HPA-I a specific antibodies in human serum, in a diagnostic kit for screening and identifying antibodies, in an immunoassay and a pharmaceutical composition.

Abstract: The present invention relates generally to structural studies of the insulin binding site of the insulin receptor (IR) and the insulin-like growth factor 1 receptor (IGF-1R). More particularly, the present invention relates to the crystal structure of the low affinity insulin binding site of the IR ectodomain comprising the C-terminal region of the IR ?-chain, as well as the corresponding region of IGF-1R, and to methods of using the crystal and related structural information to screen for and design compounds that interact with or modulate the function of IR and/or IGF-1R.

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: Contrast agents comprising a scaffold protein having at least one operative integrated metal ion binding site.

Abstract: Reagents and methods for functionalising polypeptides with moieties poly (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalising 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 functionalising 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: A sensor for detecting of an analyte in a solution phase comprises a plurality of functionalised silver nanoplates wherein a functionalising agent is directly bonded to the surfaces of the nanoplates. The nanoplates provide a detectable wavelength shift change in their local surface plasmon resonance spectrum in response to the binding of an analyte. Two or more of the nanoplates may be electromagnetically coupled.

Abstract: Disclosed are a novel cyanine compound, represented by the following Formula 1, for labeling biomolecules, and a method for preparing the same. wherein R1, R2, R3, R4, B, m and n are defined as above.

Abstract: Compounds that are capable of inhibiting the activity of one or more protein kinases are provided. The compounds are short, predominantly basic peptidic compounds comprising between about 5 and about 20 amino acids, and can optionally comprise an ATP mimetic moiety. The protein kinase inhibiting compounds can be used to inhibit the activity of one or more protein kinases in vitro or in vivo. Also provided are methods of inhibiting a protein kinase in a subject by administration of an effective amount of a protein kinase inhibiting compound and the use of the protein kinase inhibiting compounds, alone or in combination with other chemotherapeutic agents, in the treatment of protein kinase mediated diseases and disorders.

Abstract: The invention provides a process for amidating a desired peptide comprising cleaving a substrate polypeptide at a X1-cysteine sequence, wherein X1 is the amino acid at the peptide carboxyl-terminus and cysteine is the first amino acid of a palladium cleavage site comprising the sequence cysteine-X2-X3, wherein X2 is any amino acid, X3 is an amino acid selected from the group consisting of cysteine, histidine, or methionine, and wherein the carboxyl-terminus of the peptide is amidated upon cleavage at the X1-cysteine sequence.

Abstract: Absorbent hydrogels are formed by reacting a protein meal base, a radical initiator and a polymerizable monomer. Optionally, a cross-linking agent and/or a radical accelerant, such as tetramethylethylenediamine (TMEDA) or sodium bisulfite (NaHSO3), is also added to the mixture. Preferably, the radical initiator is ammonium persulfate (APS) or potassium persulfate (KPS), and the cross-linking agent is preferably trifunctional trimethylolpropane trimethacrylate (TMPTMA) or methylene bis acrylamide (MBA). The polymerizable monomer is preferably acrylic acid, or a combination of acrylic acid and acrylamide. The as-formed hydrogel is washed in order to extract non-reactant components from the gel and then dried. The resultant absorbent and superabsorbent hydrogels have high water uptake ratios, and can be utilized for a variety of applications.

Abstract: The present invention relates to unprotected amino aldehydes and applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also relates to aziridine-conjugated amino derivatives, and processes for preparing the same. Pentacyclic compounds may be prepared using the aziridine aldehydes of the present invention, and the invention relates to these compounds and the processes by which they are made. The invention also relates to aziridine-conjugated bioactive molecules, such as amino acids and peptides, and processes for preparing such compounds.

Abstract: Pharmaceutical compounds, pharmaceutical compositions and methods of treatment are disclosed, wherein a compound comprises a targeting moiety which, in free form, binds a cell receptor with a dissociation constant Kd of less than about 10?7 M, and a pharmaceutically active moiety, wherein the targeting moiety is other than an oligopeptide, a polypeptide, a peptidomimetic, a protein or a protein domain, and wherein the targeting moiety and the pharmaceutically active moiety are covalently attached. In some aspects, the targeting moiety binds a sigma-2 receptor with high affinity and high specificity, and the pharmaceutically active moiety is a pro-apoptotic peptide moiety. Methods of cancer treatment are disclosed comprising administering a disclosed pharmaceutical compound to a subject in need of thereof. The treatments selectively induce apoptosis in cancer cells. These methods can further comprise co-administration of radiation therapy and/or an additional chemotherapeutic agent.

Abstract: A Ianthanide complex, method of forming and method of using the lanthanide complex as a near-infrared luminescent material are described. The complex includes at least one lanthanide ion and at least one polydentate ligand derived from a molecule having the general formula of Structure: Structure 2, where: E represents a heteroatom or heteroatom-containing group and R1R8 are independently selected from H, —OH, —NH2, —SO3H, —CO2H, halides, optionally substituted organic groups; and conjugated linking groups which link two of the polydentate ligands of Structure 2 together.

Abstract: The present invention is directed to compounds, compositions, and methods useful for delivering polynucleotides or other cell-impermeable molecules to mammalian cells. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery vehicles. The use of multiple reversible linkages connecting component parts provides for physiologically responsive activity modulation.

Abstract: The present invention provides universal tags, probes and detection methods for multiple targets detection of biomolecules. The universal tag in the present invention is a fragment of DNA, RNA, peptide nucleic acid, or LNA, and is 3-20 mer in length. The probe in the present invention contains in order from 3? terminus to 5? terminus, a nucleotide sequence which is reverse complementary to a target molecule or a portion of the target molecule, and a nucleotide sequence which is reverse complementary to the universal tag; or said probe contains in order from 3? terminus to 5? terminus, a nucleotide sequence which is reverse complementary to the universal tag, and a nucleotide sequence which is reverse complementary to a target molecule or a portion of the target molecule.

Abstract: This invention relates to compositions and methods that can be used immunize a subject against influenza. Generally, the compositions and methods include peptides obtained or derived from human influenza A virus M2 protein.

Abstract: Provided are methods and compositions which are useful for separating, isolating, detecting, and quantifying compounds of interest which have been modified chemically, enzymatically or catalytically from other compounds which have not been so modified. The modifications may take the form of functional groups which are gained, lost or retained by the compounds of interest.

Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.

Abstract: The present invention relates to peptides, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated cytotoxic T cell (CTL) peptide epitopes, alone or in combination with other tumor-associated peptides that serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses. The present invention relates to 30 peptide sequences and their variants derived from HLA class I and class II molecules of human tumor cells that can be used in vaccine compositions for eliciting anti-tumor immune responses.

Abstract: The present invention provides a method for analyzing the C-terminal amino acid sequence of a peptide by using a reaction for successively releasing the C-terminal amino acids of the peptide, which method can suppress, when successively releasing the C-terminal amino acids of a peptide of long amino acid length, such a undesirable side reaction as cleavage of peptide bond in the intermediate position of the peptide and can carry out the chemical treatment thereof under widely applicable conditions; In the method, a dry sample of a peptide with long amino acid length is beforehand subjected to an N-acylation treatment; by using a reaction reagent where an alkanoic acid anhydride is combined with a small amount of a perfluoroalkanoic acid, successive release of C-terminal amino acids is conducted under mild conditions; a hydrolysis treatment is applied; then, selective fragmentization at site of arginine residue is performed by digestion by trypsin; thereafter, decreases in molecular weight are measured for the

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: This disclosure provides modified antimicrobial agents, for example modified defensin polypeptides. Compositions including a modified arginine residue, such as an ADP-ribosylated and/or ribosylated alpha defensin polypeptide, are provided. Also provided are methods of modulating an immune response using the modified defensin polypeptides. Methods are provided for modulating an antimicrobial activity and for inhibiting a cytotoxic activity. Also disclosed are methods for treating diseases in a subject that are associated with an immune response, such as inflammatory and pulmonary diseases, using the disclosed modified defensin polypeptides.

Abstract: A method for manufacturing cubic diamond nanocrystals (10) comprising the following successive steps: (a) providing crystalline diamond powder where the maximum particle size of the powder is equal or more than 2 um and equal or less than 1 mm; (b) milling said crystalline micron diamond powder using nitrogen jet milling micronization so as to manufacture a fine powder; (c) nanomilling the fine powder of step b) using a planetary tungsten carbide ball mill; (d) acid treating the nanomilled powder of step c); (e) extracting the cubic diamond nanocrystals (10) by centrifugation. Advantageously round-shaped cubic diamond nanocrystals are manufactured.

Abstract: Relative quantification of metabolites by Electrospray Ionization Mass Spectrometry (ESI-MS) requiring a mechanism for simultaneous analysis of multiple analytes in two or more samples. Labeling reagents that are reactive to particular compound classes and differ only in their isotopic compositions facilitate relative quantification. Heavy and light isotopic forms of methylacetimidate were synthesized and used as labeling reagents for quantification of amine-containing molecules. Heavy and light isotopic forms of formaldehyde and cholamine were also synthesized and used independently as labeling reagents for quantification of amine-containing and carboxylic acid-containing molecules, such as found in biological samples. The labeled end-products are positively charged under normal acidic conditions involving conventional Liquid Chromatography Mass Spectrometry (LC/MS) applications.