Abstract: Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): —OX—Y (Ia) or —O—R1 (Ib) wherein X is C(O), S(O) or SO2; Y is NR1R2 or R3; R1 is C1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R2 is H or C1-6 alkyl; and R3 is C1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.

Abstract: Disclosed are dithio compounds that include a quenched fluorophore and a non-fluorophore peptide linked via a dithio bond to the fluorophore. The dithio compounds may be used in methods for detecting thiol-containing compounds or dithio-containing compounds. The dithio compounds also may be used as cellular probes where the peptide portion of the compounds targets the compounds to a specific cellular location.

Abstract: The present application describes a process for conjugating a PNAG which is less than 40% N-acetylated to a carrier protein.

Abstract: A protein containing one or more activatable groups, e.g., an antibody, is subjected to partial or complete reduction of one or more such bonds to form reactive groups; the resulting protein is reacted with a drug which is reactive with some of the reactive groups, such as certain radiometals, chelating agents, and toxins, so as to form a conjugate useful in, e.g., in vitro diagnosis, in vivo imaging, and therapy.

Abstract: The present disclosure is directed to fluorogenic schiff base-forming dyes capable of detecting analytes containing aldehyde and ketone groups. The dyes contain nucleophilic hydrazinyl appendages and are capable of binding and detecting analytes in situ.

Abstract: The invention provides reagents and methods for conjugating a polymer specifically to the ?-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ?-amine of a polypeptide having a cysteine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.

Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.

Abstract: The invention provides methods of chemically synthesizing chimeric proteins comprising at least a portion of an immunoglobulin constant region and a biologically active molecule.

Abstract: Engineered proteins for the assembly of two-dimensional and three-dimensional nanostructure assemblies. Methods for the systematic design and production of protein node structures that can be interconnected with streptavidin or streptavidin-incorporating struts to produce structures with defined dimensions and geometry. Nanostructure assemblies having utility as functional devices or as resists for the patterning of substrates. Nanostructure architectures including polygons, polyhedra, two-dimensional lattices, and three-dimensional lattices.

Abstract: The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal N-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a ?-(methylamino)-thioester intermediate that spontaneously rearranges to form an amide bond. Furthermore, the invention relates to methods of converting N-methyl-thiazolidine to N-methyl-cysteine (SEQ ID NO: 1) of polypeptides and proteins. The invention also relates to methods of synthesizing peptide-thioester from peptide-acid fluoride.

Abstract: The invention relates to compositions and methods useful in the labeling and identification of proteins. The invention provides for highly soluble zwitterionic dye molecules where the dyes and associated side groups are non-titratable and maintain their net zwitterionic character over a broad pH range, for example, between pH 3 and 12. These dye molecules find utility in a variety of applications, including use in the field of proteomics.

Abstract: A system for producing multi-component colloidal structures has a supply system; an assembly system that is in fluid connection with the supply system to receive a supply of colloidal structural components from the supply system; and an output system in fluid connection with the assembly system. The assembly system has an assembly chamber adapted to contain colloidal structural components during assembly of a multi-component colloidal structure and is structured and arranged to control positions and orientations of first and second c structural components in the assembly chamber to bring the first and second colloidal structural components together in predetermined relative positions and orientations for assembly into at least a portion of the multi-component colloidal structure.

Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.

Abstract: The present invention relates to methods for the formation of inter-molecular disulphide bonds, including (poly)peptides/proteins, nucleic acids, vectors, host cells and bacteriophages used in these methods. Furthermore the invention relates to the use of this method for the improved display of (poly)peptides/proteins on the surface of bacteriophage particles.

Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

Abstract: An affinity matrix comprising a base matrix containing biotin; and a fusion protein attached to the base matrix, wherein the fusion protein contains a matrix binding element capable of binding to the base matrix via biotin and a target binding element capable of binding, or being bound by, at least one target component.

Abstract: The present invention concerns a process by which a misfold in an Fc fusion molecule can be prevented or corrected. In one embodiment, the process comprises (a) preparing a pharmacologically active compound comprising an Fc domain; (b) treating the fusion molecule with a copper (II) halide; and (c) isolating the treated fusion molecule. The pharmacologically active compound can be an antibody or a fusion molecule comprising a pharmacologically active domain and an Fc domain. The preferred copper (II) halide is CuCl2. The preferred concentration thereof is at least about 10 mM for fusion molecules prepared in E. coli; at least about 30 mM for fusion molecules prepared in CHO cells. The process can be employed with any number of pharmacologically active domains. Preferred pharmacologically active domains include OPG proteins, leptin proteins, soluble portions of TNF receptors (e.g., wherein the fusion molecule is etanercept), IL-1ra proteins, and TPO-mimetic peptides.

Abstract: The invention relates to a process for modifying allergens to enhance their suitability in immunotherapy. The invention further relates to the modified allergens and pharmaceutical compositions thereof, as well as to their use in immunotherapy.

Abstract: The present invention relates to the tagging of Histidine in polypeptides with arylboronic acid tagging reagents. The present invention further describes methods and devices to identify proteins in a sample by isolating and identifying Histidine-comprising peptides from one protein sample or a pool of protein samples. The present invention further describes databases of Histidine-comprising peptides from in silico cleaved proteins and their use in the identification of proteins.

Abstract: Topiramate analogs have substituents at the sulfamate group, 9-position, or 10-position. Topiramate analogs may include immunogenic moieties to prepare anti-topiramate antibodies, or antigenic moieties for immunodiagnostic assays. Also, the topiramate analog can include tracer moieties for detecting the presence or amount of the analog during an immunodiagnostic assay. Additionally, the topiramate analogs can be used in immunodiagnostic assays to compete with topiramate for binding with anti-topiramate antibodies. Such an immunodiagnostic assay can be used for detecting the presence of topiramate in a sample obtained from a subject previously administered topiramate by the following: combining an anti-topiramate antibody and a topiramate analog with a sample to form a first composition; allowing any free topiramate from the sample and the topiramate analog to compete for binding with the antibody; detecting binding between the topiramate analog and the antibody.

Abstract: The present invention relates to novel methods for making and refolding insoluble or aggregated proteins having free cysteines in which a host cell expressing the protein is exposed to a cysteine blocking agent. The soluble, refolded proteins produced by the novel methods can then be modified to increase their effectiveness. Such modifications include attaching a PEG moiety to form PEGylated proteins.

Abstract: The invention relates to the field of drug delivery, in particular, to compounds and methods for the chemical modification of a proteinaceous channel to be used in pharmaceutical delivery vehicles for controlled and/or localized release of therapeutic molecules (e.g., small molecules, peptides, proteins or other macromolecules). Provided are drug delivery vehicles comprising a pH- and/or light-responsive channel protein.

Abstract: Protein-based photovoltaic cells and the manufacture and use of protein-based photovoltaic cells are described. In one embodiment, bacteriorhodopsin from Halobacterium salinarum, which undergoes structural transitions when irradiated with a given wavelength of light, is used as the protein in the protein-based photovoltaic cells. In another embodiment, mutant bacteriorhodopsin from H. salinarum is used. Exposure of the protein to sunlight causes proton transfer across a membrane resulting in the generation of an electrical charge. The protein can be oriented and/or layered on a substrate and modified by mutation to enhance transmembrane proton transfer, covalent binding to a substrate and layering. The protein-based photovoltaic cells sequentially or simultaneously generate hydrogen gas from water or salt, which also can be harnessed to produce electricity.

Abstract: First, an ammonium acetate solution and an acetate solution of a metal such as Cd or Zn are mixed, so as to form an ammonium complex of the metal. Next, an apoferritin solution and thioacetic acid are added to the thus obtained reaction solution. By allowing the reaction solution to stand for 12 hours or more, a complex of a nanoparticle including CdS or ZnS and apoferritin is produced.

Abstract: This invention relates to a method of producing a modified (poly)peptide, said method comprising the step of modifying in an organic solvent a crown ether-bound (poly)peptide at one or more carboxylic groups by esterification or thioesterification and/or at the amino group of the N-terminal amino acid by amidation or alkylation. Furthermore provided are (poly)peptides and antibodies obtainable with the method of the invention as well as medical uses thereof.

Abstract: The invention is directed to methods and compositions for chemical ligation of a first component that includes a carboxythioester and a second component that includes an amino-functionalized compound bearing a branched side chain that includes a removable thiol auxiliary, to give a ligation product having an amide bond at the ligation site. The reactants of the invention are chemoselective and the thiol moiety is removable from the ligation product. Removal of the thiol can be exploited to generate a native side chain at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers.

Abstract: The present invention relates to a conjugate of a biocompatible polymer and a G-CSF bonded through a thiol group of a dysteine residue in G-CSF at a 1:1 molar ratio, and methods of preparation thereof.

Abstract: Conformational isomers of modified versions of ?-Synuclein (?Syn), a protein that is associated with Parkinson's disease, have been designed and produced. These conformational isomers are produced by introducing cysteines into the ?-Synuclein and scrambling the disulfide bonds to form stable and immunogenic isomers. These isomers are generically referred to as X-isomers. X-?Syn is an X-isomer of ?Syn. X-?Syn is generally more immunogenic than wt-?Syn. Two groups of X-?Syn have been produced. One group is 3-disulfide X-?Syn(3SS) produced by introducing 6 Cys mutations into the ?Syn. The second group is 2-disulfide X-?Syn(2SS), produced by introducing 4 Cys mutations into the ?-Syn. In each of these two groups of X-?Syn, Cys was introduced not only wt-?Syn, but also in two Parkinson Disease associated ?Syn mutants, A30P-?Syn and A53T-?Syn. All six sets of X-?Syn exhibit enhanced aggregation as compared to wt-?Syn, and should therefore more much more immunogenic.

Abstract: The invention provides compositions and methods of use thereof for labeling peptide and proteins in vitro or in vivo. The methods described herein employ lipoic acid ligase or mutants thereof, and lipoic acid analogs recognized by lipoic acid ligase and lipoic acid ligase mutants.

Abstract: Improved methods for the production, selection and inhibition of catalytic antibodies are disclosed.

Abstract: N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-methyl-4,5-(methylenedioxy)phenyl-acetyl]thiophene-3-sulfonamide, sodium salt, is provided herein in the form of three polymorphs (Forms A, B and C). Forms A, B and C are specified by the peaks in their X-ray powder diffraction patterns, their absorption peaks in their infrared absorption spectra, their peaks in their Raman spectra and their melting points.

Abstract: A method for producing a S-nitrosylated species is provided. The method comprises: (a) providing a deoxygenated, alkaline aqueous solution comprising a thiol and a nitrite-bearing species; (b) acidifying the solution by adding acid to the solution while concurrently mixing the solution (e.g., by vigorously stirring the solution) to produce the S-nitrosylated species; and (c) isolating the S-nitrosylated species. The nitrite-bearing species can be, for example, an inorganic nitrite, such as an alkali metal nitrite, or an organic nitrite, such as an alkyl nitrite (e.g., ethyl nitrite, amyl nitrite, isobutyl nitrite or t-butyl nitrite). The thiol is preferably a thiol-containing polysaccharide, a thiol-containing lipoprotein, a thiol-containing amino acid or a thiol-containing protein, and more preferably a thiol-containing polysaccharide such as thiolated cyclodextrin. In many preferred embodiments, the S-nitrosylated species is insoluble in the acidified solution, precipitating upon formation.

Abstract: A protein containing one or more activatable groups, e.g., an antibody, is subjected to partial or complete reduction of one or more such bonds to form reactive groups; the resulting protein is reacted with a drug which is reactive with some of the reactive groups, such as certain radiometals, chelating agents, and toxins, so as to form a conjugate useful in, e.g., in vitro diagnosis, in vivo imaging, and therapy.

Abstract: The present invention relates to magnetic fine particles having a lower critical solution temperature to which at least one substance selected from biotin and avidin is immobilized, and a method of converting a substance, a method of separating or concentrating a microorganism, a method of modifying a denatured protein, a method of detecting a nucleic acid, a separating agent, and a method of separating a biological substance using the same.

Abstract: The invention relates to a carrier-drug conjugate comprising a carrier containing a polypeptide sequence having one or several cysteine radicals and a pharmacon containing a pharmaceutical and/or diagnostic active substance, a spacer molecule and a thiol binding group, whereby over 0.7 mol pharmacon per mol of cysteine radical is bound to the carrier by the thiol binding group. The invention also relates to a method for the production of said conjugate and to medicaments and diagnostic kits containing said conjugate.

Abstract: Compositions and methods for folding proteins belonging to the transforming growth factor beta superfamily are disclosed. The compositions and methods allow for the folding of such proteins when produced in an expression system that does not yield a properly folded, biologically active product.

Abstract: The invention provides methods of chemically synthesizing chimeric proteins comprising at least a portion of an immunoglobulin constant region and a biologically active molecule.

Abstract: Novel conjugates of busulfan and novel busulfan immunogens derived from ?-substituted derivatives of busulfan and antibodies generated by these busulfan linked immunogens are useful in immunoassays for the quantification and monitoring of busulfan in biological fluids.

Abstract: This invention relates to a process for purifying a polypeptide, a capture tag useful for purifying a polypeptide and a periodate-cleavable amino acid derivative useful for purifying a polypeptide. The polypeptide to be purified comprises a vicinal-amino-thiol, vicinal-amino-hydoxyl, vicinal-diol or vicinal-diamino group. The purification process comprises attaching the polypeptide to a purification matrix by contacting the polypeptide with a purification matrix comprising aldehyde or ketone groups under conditions which favor formation of a heterocyclic ring system, washing the purification matrix, and releasing the polypeptide from the purification matrix.

Abstract: A biologically active conjugate is disclosed comprising a biopolymer and a therapeutic agent joined by a disulfide bond. The conjugate, when formulated in a pharmaceutical composition with a suitable carrier, has improved in vivo stability and activity, and can be targeted to a variety of cells, tissues and organs.

Abstract: The present invention relates to method for selective reduction and derivatization of recombinantly prepared engineered proteins comprising at least one non-native cysteine, wherein the reduction reaction is conducted in the presence of a redox buffer or in the presence of a triarylphosphine reducing agent.

Abstract: The invention relates to the field of drug delivery, in particular, to compounds and methods for the chemical modification of a proteinaceous channel to be used in pharmaceutical delivery vehicles for controlled and/or localized release of therapeutic molecules (e.g., small molecules, peptides, proteins or other macromolecules). Provided are pH- and/or light-responsive compounds capable of controlling the channel activity of a mechanosensitive channel, such as the MscL channel protein of E. coli, or a functional equivalent thereof, and use of these compounds to convert a mechanosensitive channel protein into a pH- and/or light-responsive channel. Also provided are drug delivery vehicles comprising a pH- and/or light-responsive channel protein.

Abstract: Disclosed are methods of inactivating a protein, such as cleaving a disulfide bond of a protein, that involve contacting the protein with a reducing agent, a denaturant, and a hydroxide ion, wherein the pH of the composition is about 10.0 to about 14.0. Also disclosed are methods of treating or preventing a disease in a subject, such as a toxin-related disease or a prion-related disease, that involve contacting a subject with a pharmaceutically effective amount of a reducing agent, a denaturant, and a hydroxide ion, wherein the pH of the composition is about 9.0 to about 14.0. Also disclosed are compositions that include a reducing agent, a denaturant, and a hydroxide ion, wherein the pH of the composition is about 9.0 to about 14.0.

Abstract: A detectable complex and methods for use thereof are provided herein. The detectable complex includes: at least one target material; a first peptide tag bound to the at least one target material; and a second peptide tag bound to the at least one target material. The complex further includes a first conjugate having a detectable group and two pendant phenylarsine moieties comprising a first tag binding group; wherein the first conjugate preferentially associates with the first peptide tag; and a second conjugate having a detectable group and two pendant phenylarsine moieties comprising a second tag binding group; wherein the second conjugate preferentially associates with the second peptide tag. The mean distance and/or mean angle between the pendant phenylarsine moieties in the first conjugate is different from the mean distance and/or mean angle between the pendant phenylarsine moieties in the second conjugate.

Abstract: Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions.

Abstract: The invention relates to a method which is used to efficiently mark proteins with the help of a micromixer, in addition to a device which enables said inventive method to be carried out in an economical manner and with additional auxiliary agents.

Abstract: The present invention relates to novel methods for making and refolding insoluble or aggregated proteins having free cysteines in which a host cell expressing the protein is exposed to a cysteine blocking agent. The soluble, refolded proteins produced by the novel methods can then be modified to increase their effectiveness. Such modifications include attaching a PEG moiety to form PEGylated proteins.

Abstract: A self-assembled relay probe for detecting a target material is provided including: a first peptide tag bound to the target material; and a first fluorescent conjugate including a first fluorochrome and a first tag binding group; wherein the first fluorescent conjugate selectively associates with the first tag. The probe further includes a second peptide tag bound to the target material; and a second fluorescent conjugate including a second fluorochrome having a longer wavelength and distinct excitation and emission maxima from the first fluorochrome and a second tag binding group. Upon exposure to the target material, the first and second fluorescent conjugates independently associate with the first and second peptide tags, respectively, so as to be a distance apart represented by about 0.

Abstract: A heparin-binding protein functionalized by covalently bonding thereto a sugar chain, a method for producing the protein and a pharmaceutical composition containing the protein as an active ingredient, as well as a method of functionalizing a natural protein having no sugar chain by covalently bonding thereto a sugar chain.