Abstract: Disclosed herein are methods for immobilizing membrane proteins or membrane protein complexes on analytical surfaces, which in some aspects comprise: obtaining a membrane protein or membrane protein complex comprising a capture moiety; immobilizing the membrane protein or membrane protein complex on the analytical surface by means of the capture moiety; and stabilizing at least one of the secondary, tertiary, or quaternary structures of the immobilized membrane protein or membrane protein complex by crosslinking with a crosslinking reagent. Also disclosed are analytical surfaces, which in some aspects comprise: a membrane protein or membrane protein complex comprising a capture moiety, wherein the membrane protein or membrane protein complex is immobilized on the analytical surface by means of the capture moiety, and wherein at least one of the secondary, tertiary, or quaternary structures of the membrane protein or membrane protein complex is stabilized by crosslinking.

Abstract: The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.

Abstract: Disclosed herein are compounds useful in the preparation non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are compound useful in the preparation of non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: Methods, compositions and kits are disclosed directed at voriconazole derivatives, immunogens, signal generating moieties, antibodies that bind voriconazole and immunoassays for detection of voriconazole.

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: Compounds of the following Formula (I): in which A represents either a nitrogen atom, or a ring having 3 to 6 carbon atoms, or an aromatic ring having 5 to 10 members, the ring and the aromatic ring optionally include one or more heteroatoms selected from N, O and S, and W represents a grafting function and X and Y represent chelating functions.

Abstract: A bifunctional chelating agent of the formula (I): wherein the variables R1, R1?, Q1, Q2 and M are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a stable or radioactive metal; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate.

Abstract: A new and versatile class of cyclic diazodicarboxamides that reacts efficiently and selectively with phenols and the phenolic side chain of tyrosine through an Ene-like reaction is reported. This mild aqueous tyrosine ligation reaction works over a broad pH range and expands the repertoire of aqueous chemistries available for small molecule, peptide, and protein modification. The tyrosine ligation reactions are shown to be compatible with the labeling of native enzymes and antibodies in buffered aqueous solution. This reaction provides a novel synthetic approach to bispecific antibodies. This reaction will find broad utility in peptide and protein chemistry and in the chemistry of phenol-containing compounds.

Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).

Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.

Abstract: Compound of Formula I: are described, along with compositions containing the same and methods of use thereof.

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 magnetic nanoparticle is provided in the disclosure. The magnetic nanoparticle includes a magnetic nanoparticle; a biocompatible polymer of the following formula (II) covalently coupled to the magnetic nanoparticle, wherein R1 is alkyl, aryl, carboxyl, or amino; n is an integer from 5 to 1000; and m is an integer from 1 to 10.

Abstract: Provided is an organic nanotube having a hydrophobized inner surface, formed by molecules including an asymmetric bipolar lipid molecule represented by the following General Formula (1) and a derivative thereof represented by the following General Formula (2), wherein the organic nanotube has a hydrophilized outer surface and a hydrophobized inner surface of a hollow cylinder and is formed by binary self-assembly, the organic nanotube encapsulates a hydrophobic guest in the hollow cylinder, has a function of refolding a denatured protein, and has a function of sustainably-releasing a hydrophobic drug according to the change in hydrophobicity of the inner surface of the tube or external stimulus, In Formulas (1) and (2), wherein the same symbols have the same meanings, G is a 1-glucopyranosyl group or 2-glucopyranosyl group, and n is an integer of 12 to 22.

Abstract: The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.

Abstract: Novel polypeptide combinations, polynucleotides encoding the polypeptides, and related compositions and methods are disclosed for zcytor17-containing multimeric or heterodimer cytokine receptors that may be used as novel cytokine antagonists, and within methods for detecting ligands that stimulate the proliferation and/or development of hematopoietic, lymphoid and myeloid cells in vitro and in vivo. The present invention also includes methods for producing the multimeric or heterodimeric cytokine receptor, uses therefor and antibodies thereto.

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: Immunogenic capsule polysaccharide polymer composition, and its method of producing, with improved structural integrity and immunogenic properties. The invention also relates to a method of using the compositions to elicit an immune response to Campylobacter jejuni.

Abstract: The present invention relates to a novel method for preparing compounds having the formula (I), where X is biotin or Y being biotin or Z being biotin or V being biotin or It also relates to compounds having the formula (I) and their use in clinical and industrial diagnosis.

Abstract: Enzyme-activatable photosensitizing polymer conjugates are disclosed for photochemotherapeutic treatment of human diseases and disorders, bacteriologic or virologic indications, cosmetic applications and other pathologic situations. These polymer conjugates may comprise a polymer carrier, a photosensitizer, a quencher, a targeting molecule and/or a biocompatibilizing unit. These macromolecular conjugates may be designed to guide to the target tissue a photosensitizing agent in an inactive, non-phototoxic form. However, upon entering the target environment, in which certain enzymes are presently active, the conjugate may release its photosensitizers in its fully active form, resulting in a highly localized activation of the photoactive agent. Also described here are methods, compositions and kits for the preparation and testing of such photochemotherapeutic conjugates.

Abstract: Provided are crystalline ?, ?-disubstituted amino acids and their crystalline salts containing a terminal alkene on one of their side chains, as well as optionally crystalline halogenated and deuterated analogs of the ?, ?-disubstituted amino acids and their salts; methods of making these, and methods of using these.

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: A fluorescent protein (bFP) having chemiluminescence activity is a complex composed of the apoprotein of a calcium-binding photoprotein, coelenteramid or an analog thereof, and calcium ions or divalent or trivalent ions that can be substituted for the calcium ions. In the complex, the ratio of the number of molecules of the apoprotein to that of the coelenteramid is 1:1 and the ratio of the number of molecules of the apoprotein to that of the divalent or trivalent ions is 1:1 to 1:4. The fluorescent protein is used as a marker because it catalyzes luminescence of coelenterazine and has fluorescence capability. Removal of calcium ions etc. from this fluorescent protein (bFP) having luminescence activity provides a novel fluorescent protein (gFP). Mixing this gFP with the coelenterazine provides a calcium-binding photoprotein, which emit light instantaneously, enabling use as a marker.

Abstract: The present disclosure includes an electrochemical proximity assay (ECPA) which leverages two aptamer or antibody-oligonucleotide probes and proximity-dependent DNA hybridization to move a redox active molecule near an electrically conductive base. The ECPA of the present disclosure produces rapid, quantitative results, enabling point-of-care use in the detection of biomarkers of disease.

Abstract: A peptide nanotube (PNT) device and method of manufacturing thereof are disclosed herein. The PNT device comprises PNTs composed of cyclo-(D-Trp-Tyr) peptide and a matrix, including biomolecules, complexed with the PNTs. The PNT device is biodegradable and biocompatible, as well as capable of being uptake by mammalian cells. Wherein, the biomolecules comprise peptides, proteins, nucleic acids including DNA, shRNA and siRNA, and drugs. The method for manufacturing PNT device comprises: dissolving a cyclo-(D-Trp-Tyr) peptide powder in a solvent to be a solution in a container; incubating the solution at a predetermined temperature for a predetermined time for the solvent to evaporate to obtain PNTs formed of cyclo-(D-Trp-Tyr) peptide; and mixing the PNTs with a matrix including biomolecules to obtain the PNT device.

Abstract: The present invention relates to bifunctional compounds, the bifunctional compounds for use in molecular imaging and therapy, methods of molecular imaging using the bifunctional compounds and kits including the bifunctional compounds for use molecular imaging. The bifunctional compounds have a tripodal hydroxypyridinone chelating portion and may be conjugated to a targeting group so that the compounds target specific cells or tissues in a subject.

Abstract: The present invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a therapeutic moiety, and further relates to processes for making and using the conjugates.

Abstract: A composition comprising a main species HER2 antibody that binds to domain II of HER2 and acidic variants thereof is described. Pharmaceutical formulations comprising the composition, and therapeutic uses for the composition are also disclosed.

Abstract: Methods and compositions for the selective derivatization of a oligohistidine-tagged recombinant protein. A modifying compound comprised of an imidazole reactive group, a linker, and a ligating group is contacted with the recombinant protein, and a cooperative bond forms between the ligating group and the oligohistidine tag in the presence of a metal cation, and a covalent bond forms between the imidazole reactive group and an imidazole ring of the oligohistidine tag followed by the concomitant separation of the imidazole reactive group from the linker. Addition of a metal chelator results in the dissociation of the ligating group and the oligohistidine tag.

Abstract: Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin ?v?3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin ?v?3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.

Abstract: Methods for preparing complex multivalent immunogenic conjugates that include simultaneously reacting a plurality or immunogenic-distinct polysaccharides with at least one protein to make the complex multivalent immunogenic conjugates. The simultaneous reaction involves reaction of a hydrazide group on one reactant with an aldehyde or cyanate ester group on the other reactant.

Abstract: The present invention relates to hydrophobic modified peptides for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the compound(s) to be specifically delivered to the liver. The present invention furthermore relates to the use of the inventive hydrophobic modified peptides as well as to a method for the prevention and/or treatment of liver diseases or disorders.

Abstract: The invention conjugates that can be prepared by contacting a polymer comprising an acetal or ketal branching point with a pharmacologically active agent under conditions suitable to form a covalent attachment between the polymer and the pharmacologically active agent.

Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).

Abstract: The low-molecular-weight compound represented by the general formula (1): ArX-(Linker)-ArYHB (1), wherein ArX is a structure containing an optionally substituted aromatic six-membered ring, ArYHB is a structure containing an optionally substituted aromatic six-membered ring having a proton donor, the atom group “Linker” has not less than 4 and not more than 30 atoms and binds ArX with ArYHB, is used for binding a proteinaceous substance.

Abstract: The invention provides interfering RNA molecule-ligand conjugates useful as a delivery system for delivering interfering RNA molecules to a cell in vitro or in vivo. The conjugates comprise a ligand that can bind to a low density lipoprotein receptor (LDLR) or LDLR family member. Therapeutic uses for the conjugates are also provided.

Abstract: The present invention relates to IL-1 receptor antagonist compounds, compositions and use thereof as well as methods for preparation thereof.

Abstract: The present invention describes the modification of polypeptides, more particularly channel proteins with a thiol reactive agent so as to introduce an azide group. The present invention further describes vesicles comprising channel proteins modified according to the invention, which upon reaction with a phosphine open up thereby releasing the content of the vesicles. The reagents, polypeptides and vesicles described in the present invention have in vivo and in vitro applications in both drug delivery and imaging.

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 invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance.

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: The present invention relates to methods and kits for the detection of 5-hydroxymethylcytosme (5hmC). In some embodiments, the present invention relates to methods and kits for detection of 5hmC in nucleic acid (e.g., DNA, RNA). In some embodiments, the present invention relates to detection of 5hmC in genomic DNA, e.g., mammalian genomic DNA.

Abstract: A method for manufacturing a carrier having temperature responsive protein A, which is protein A mutated such that a binding property to an antibody changes depending upon temperature, immobilized thereto, wherein the temperature responsive protein A has the binding property to the antibody in a first temperature region and no binding property to the antibody in a second temperature region; and the method comprises a step of immobilizing the temperature responsive protein A to a carrier surface at a temperature within the first temperature region in which the temperature responsive protein A has the binding property to the antibody.

Abstract: The present invention provides targeted Schiff base complexes. In particular the present invention provides biopolymer targeted transition metal complexes configured to inhibit the activity of targeted proteins, methods of synthesis thereof, and pharmaceutical compositions and uses thereof.

Abstract: Provided is a composition for detecting a protein, containing a tyrosine oxide-coupled biomaterial. Various diseases may be easily and rapidly diagnosed by easily detecting the composition containing a tyrosine oxide-coupled biomaterial according to the present invention, by identifying a color of the protein bound with a tyrosine oxide-coupled biomaterial prepared by binding tyrosine oxide, which is a natural pigment present in a living body, with the biomaterial. Accordingly, the composition of the present invention may be used to easily and rapidly diagnose various diseases in real time in an operating room, and may usefully replace conventional histological analysis without a secondary antibody reaction and a final operation of color expression.

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: The invention features a method of attaching a ligand that has a free carboxyl group to a solid support by adding an amino group to the ligand to form a ligand-amino derivative, converting the ligand amino derivative to a ligand sulfhydryl derivative, attaching the ligand sulfhydryl derivative to a protein to form a ligand-linker-protein conjugate, and applying the ligand-linker-protein conjugate to the solid support. The method is particularly useful for immobilizing small molecule ligands having a free carboxyl group, such as cloxicillin, to a lateral-flow test strip, in order to make a detection zone on the test strip that exhibits a clear signal and enhanced sensitivity.

Abstract: The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.

Abstract: The present invention relates to a method for cross-linking peptides using an activated furan-moiety. In particular, the present invention provides a method for cross-linking peptides comprising the steps of: a) providing a composition comprising furan-peptides, said furan-peptides comprising at least one amino acid comprising a furan-moiety; b) contacting said composition comprising furan-peptides with second peptides, thereby obtaining a mixture comprising furan-peptides and second peptides; c) adding an activation signal to said mixture of step b), thereby activating said furan-peptides to activated furan-peptides, and d) reacting said activated furan-peptides with said second peptides, thereby cross-linking said activated furan-peptides with said second peptides.

Abstract: The present invention relates to a method for labeling proteins in a sample prior to separation thereof using a protein reactive dye, comprising the following steps a) dissolving the proteins in, or diluting the proteins with, or exchanging an existing protein buffer with, a labeling buffer comprising a dye-reactant (reacting with the protein reactive dye) to form a mixture, b) adding protein reactive dye to said mixture, c) incubating said mixture wherein the labeling of said proteins with said dye can be completed within 5 minutes, and wherein both the proteins and the dye-reactant form measurable reaction products with said dye, and d) separating said reaction products. The invention also relates to a kit for pre-labeling of proteins, comprising a labeling buffer, a dye, a molecular weight marker, and a sample gel loading buffer.