Abstract: The invention relates to novel crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-(?-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy.

Abstract: The invention provides gemcitabine derivatives shown in the following formula (I) and preparation methods thereof. The invention further relates to a pharmaceutical composition which comprising the said gemcitabine derivatives in an effective amount and a pharmaceutically acceptable excipient or additive. The invention further provides use of the said derivatives for preparing anti-tumor drugs. The compound designed by the invention is novel in structure and has a remarkable anti-tumor activity. According to the compound designed by the invention, the preparation starting materials have extensive sources and are easily obtained, the preparation method is simple and easy to operate, and the yield of the product is high, so that industrial production on a large scale is facilitated.

Abstract: The present invention provides novel processes for the preparation of regadenoson having the formula (I). In some embodiments, the intermediates for the synthesis of regadenoson are also provided.

Abstract: The present disclosure provides modified nucleosides, nucleotides, and nucleic acids, and methods of using them.

Abstract: Provided are salts of arachidyl amido cholanoic acid (Aramchol), pharmaceutical compositions including Aramchol salts, methods for their preparation, and methods of use thereof in medical treatment.

Abstract: The present invention relates to processes and intermediates useful for the manufacture of cyclic undecapeptides, such as Alisporivir.

Abstract: Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

Abstract: This present invention discloses an isolated peptide which amino acid sequence is SEQ ID NO.:1. The isolated peptide can inhibit the expressions of signal transduction proteins related to the heart hypertrophy pathway, apoptosis of myocardial cells related proteins, and cardiac fibrosis related proteins to have effects of preventing such as apoptosis of myocardial cells, cardiac fibrosis, heart hypertrophy, cardiac inflammation or other heart diseases. Therefore, the peptide disclosed in this present invention can be an active ingredient of pharmaceutical composition to have effects for preventing or treating cardiovascular disease.

Abstract: The present invention discloses an integrin receptor targeting novel cationic CGKRK-lipopeptide. The present invention further discloses a liposomal formulation comprising the cationic CGKRK-lipopeptide, at least two co-lipids, at least one chemotherapeutic agent and a pharmaceutically acceptable carrier. The present invention also provides a method for regressing established tumors comprising administering therapeutically effective amount of the liposomal formulation comprising the chemotherapeutic agent.

Abstract: Peptides derived from cancer specific isoform of proliferating cell nuclear antigen (caPCNA, also known as csPCNA) or from nmPCNA-interacting proteins interfere with intracellular protein-protein interaction, thereby causing a reduction in the proliferative potential of cancer. These peptides serve as therapeutic compositions to reduce the proliferation of cancer cells and also augment existing chemotherapeutic methods.

Abstract: The present invention provides PAR4 agonist peptides. These peptides are useful for developing robust PAR4 receptor assays.

Abstract: The present disclosure provides glycosylated oligopeptides having the sequence Palmitoyl-X1-Lys-X2-X3-Lys-X4-OH, where: X1 is: absent, Ser having a glycosylated side chain, or Asn having a glycosylated side chain; X2 is: Thr, Thr having a glycosylated side chain, Asn having a glycosylated side chain, or Ser having a glycosylated side chain; X3 is: Thr, or Thr having a glycosylated side chain; X4 is: Ser, or Ser having a glycosylated side chain. At least one of X1, X2, X3 and X4 is an amino acid having a glycosylated side chain. Each glycosylated side chain is, independently, glycosylated with a carbohydrate selected from the group consisting of: glucose, N-acetyl-glucosamine, galactose, N-acetyl-galactosamine, mannose, maltose, lactose, rhamnose, cellobiose, xylose, and fucose. Each hydroxyl group on the carbohydrate is, independently, OH or acetylated.

Abstract: Cell penetrating peptides (CPPs) are established as a strategy to move cargoes into the interior of eukaryotic cells by engaging import machinery on the cell surface. In most cases the CPP is covalently linked to the cargo; it is common to express cargo proteins with a CPP extension. In some experiments a non-specific interactions (e.g., hydrophobic interactions) have been used to form CPP-cargo complexes, but this has numerous drawbacks. Transport is less efficient and the lack of specificity means that other macromolecules in the medium will also be internalized. This application describes the use of specific CPP labeled adaptor proteins that can be used to move a wide variety of cargoes into the cell interior. The prototype adaptor protein is calmodulin; it is small, stable and easily produced, and binds short (17 amino acid) targets with high affinity in the presence of calcium. A cargo produced with a calmodulin binding tag can be internalized efficiently by CPP tagged calmodulin.

Abstract: The invention provides peptide inhibitors of BACE1 that bind to the active site in a noncanonical fashion, and methods of use thereof.

Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.

Abstract: Compositions and methods useful for producing an immune response in a subject specific for the RSV G protein are described herein. The new methods and compositions described herein are made possible by the development of a new recombinant RSV G protein fragment, which has been engineered) for in vitro production and is antigenically similar to the native RSV G protein. The recombinant RSV G protein fragment is capable of inducing the production of RSV G-specific antibodies when injected into a subject. These antibodies can recognize both RSV A and RSV B strains and inhibit infection of both viruses. Accordingly, the compositions and methods described herein may be useful in protecting subjects from RSV infection via immunization, raising antibodies specific for RSV, which can in turn be used to treat RSV infection.

Abstract: Provided is staphylococcus protein A expressed by a mutational Staphylococcus aureus and its coding sequence, as well as a vector, host bacteria, composition or kit which contains the coding sequence of the mutational protein. Also provided is the use of the mutational protein and the composition thereof in the preparation of vaccines, therapeutic antibodies, diagnostic kits and the like, and for the prevention, treatment and detection of infections by Staphylococcus aureus. Also provided are methods for producing, fermenting and purifying the mutational protein.

Abstract: Provided herein are methods and compositions for the display of polypeptides of interest on the tip of pili of Gram-positive bacteria. According to the present invention, the polypeptide of interest is amino terminal to a Gram-positive bacterial pilus tip protein or an active variant or fragment thereof, wherein the active variant or fragment comprises a cleaved cell wall sorting signal (CWSS) motif. The Gram-positive bacterium displaying a polypeptide of interest on the tip of pili that are disclosed herein are useful, for example, in methods for immunizing a subject with an antigen and methods for removing contaminants from a composition.

Abstract: Compositions and methods for controlling plant pests are disclosed. In particular, novel engineered hybrid insecticidal proteins (eHIPs) having toxicity to at least corn rootworm are provided. By fusing unique combinations of complete or partial variable regions and conserved blocks of at least two different Bacillus thuringiensis (Bt) Cry proteins or a modified Cry proteins an eHIP having activity against corn rootworm is designed. Nucleic acid molecules encoding the novel eHIPs are also provided. Methods of making the eHIPs and methods of using the eHIPs and nucleic acids encoding the eHIPs of the invention, for example in transgenic plants to confer protection from insect damage are also disclosed.

Abstract: Compositions and methods for controlling plant pests are disclosed. In particular, novel engineered hybrid insecticidal proteins (eHIPs) having toxicity to at least corn rootworm are provided. By fusing unique combinations of complete or partial variable regions and conserved blocks of at least two different Bacillus thuringiensis (Bt) Cry proteins or a modified Cry proteins an eHIP having activity against corn rootworm is designed. Nucleic acid molecules encoding the novel eHIPs are also provided. Methods of making the eHIPs and methods of using the eHIPs and nucleic acids encoding the eHIPs of the invention, for example in transgenic plants to confer protection from insect damage are also disclosed.

Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7 and/or NaV1.3. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

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

Abstract: Disclosed are new recombinant isoforms of human-like lubricin or PRG4 glycoprotein having outstanding lubrication properties and a novel glycosylation pattern, and methods for their manufacture at high levels enabling commercial production.

Abstract: Disclosed herein is a method of making a fibromodulin peptide (FMOD-P), compositions thereof, and methods of using the FMOD-P and the compositions thereof for treating or ameliorating a condition.

Abstract: The present application discloses a novel fusion peptide of IL-2 and IL-33 and its use. It comprises a biologically active domain of Interleukin-2 (IL-2) or a biologically active fragment or homolog thereof, and a biologically active domain of Interleukin-33 (IL-33) or a biologically active fragment or homolog thereof. The two portions can be linked by a linker sequence. The application discloses that combination therapies using IL-2 and IL-33 or a therapy using the IL233 fusion protein are effective in preventing or treating diseases and disorders such as autoimmune diseases and disorders, inflammation, etc. Depending on the subject's disease or disorder, the compositions of the invention are useful for preventing certain symptoms, treating the disease, and alleviating at least some of the symptoms.

Abstract: The present invention relates to a method for purifying a recombinant follicle stimulating hormone (FSH) or recombinant FSH variant. The method comprises the steps of subjecting a liquid containing a recombinant FSH or recombinant FSH variant to an anion exchange chromatography, to a hydrophobic interaction chromatography, and to a dye affinity chromatography, wherein these chromatographies may be performed in any order, and wherein the method neither comprises a weak anion exchange chromatography nor a reverse phase chromatography. The method of purification results in a high yield of recombinant FSH having a desired degree of purity. The obtained FSH is especially useful for the prophylaxis and treatment of disorders and medical indications where FSH preparations are considered as useful remedies.

Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain without affecting glycemic control. In particular, the invention provides novel glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.

Abstract: The present invention pertains to glycosylated peptides of the glycophorin protein and their use in medicine. In particular, the peptides carry a carbohydrate structure of interest and are capable of binding to and being presented by MHC proteins. Using the glycosylated glycophorin peptides, a specific immune response against the carbohydrate structure of interest can be induced.

Abstract: This application relates generally to the production of polypeptides having specific antigen-binding properties of Fv domains, for example, insertable variable fragments of antibodies, and modified ?1-?2 domains of NKG2D ligands. This application further relates to modified ?1-?2 domains of NKG2D ligands attached to polypeptides, in some embodiments antibodies or fragments of antibodies. This application further relates to antigen-binding peptides derived from light and heavy chain antibody variable domains, which contain two linker regions and a split variable domain.

Abstract: This invention relates to C1ORF32 protein and its variants and fragments and fusion proteins thereof, pharmaceutical composition comprising same and methods of use thereof for treatment of immune related disorders and infections.

Abstract: The invention provides a polypeptide that specifically binds to CTLA-4, particularly human CTLA-4.

Abstract: Methods are disclosed for preventing and/or treating cardiovascular diseases comprising administering B7x or a derivative of B7x to a patient in need thereof.

Abstract: The invention relates to the use of a molecular adjuvant to generate an improved immune response in a host. Over recent years extensive research and development has been undertaken in the development of “vectored vaccines” which can be used as vaccine delivery systems. Vectored vaccines include DNA vectors and recombinant viral and bacterial vectors, which are engineered to express an antigen of interest. The invention provides a nucleic acid construct encoding a protein fusion between an antigen and an invariant chain molecule.

Abstract: Described herein are methods for purifying recombinant, cell culture derived alpha1-protease inhibitor and removing a colored species that co-purifies with the recA1PI protein. Also described are methods for reducing the iron in cell culture derived alpha1-protease inhibitor.

Abstract: The present invention relates to MafB mutants and uses thereof for research, screening and therapeutic purposes. In particular, the present invention relates to a MafB mutant polypeptide comprising the sequence as set forth in SEQ ID NO: 1 or 2 or a function conservative variant thereof wherein the glutaminic acid residue at position 269 has been deleted or substituted with a basic amino acid. The present invention also relates to a MafB mutant polypeptide comprising the sequence as set forth in SEQ ID NO: 1 or 2 or a function conservative variant thereof wherein the valine residue at position 277 has been deleted or substituted with a polar amino acid.

Abstract: A transgenic animal is provided. In certain embodiments, the transgenic animal comprises a genome comprising: an immunoglobulin light chain locus comprising: a) a functional immunoglobulin light chain gene comprising a transcribed variable region encoding: i. light chain CDR1, CDR2 and CDR3 regions that are composed of 2 to 5 different amino acids; and ii. a light chain framework; and, operably linked to the functional immunoglobulin light chain gene: b) a plurality of pseudogene light chain variable regions each encoding: i. light chain CDR1, CDR2 and CDR3 regions that are composed of the same 2 to 5 different amino acids as the CDRs of the functional gene; and ii. a light chain framework that is identical in amino acid sequence to the light chain framework of the transcribed variable region.

Abstract: This disclosure provides a novel process for testing an influenza virus preparation for the presence of extraneous agents. The disclosure further provides a process for preparing an influenza vaccine.

Abstract: A vaccine and method of vaccination for conferring immunity to Q fever is described. The vaccine comprises a polypeptide with a sequence of SLTWHKHELHRK (m1E41920) or SPPWHKHELHRK (m1E44), or at least 90% identity to m1E41920 or m1E44. Constructs are also provided for use in vaccination and treatment of Q fever. A method to identify and generate new vaccines to prevent diseases caused by intracellular Gram-negative bacteria is also described.

Abstract: Compositions and methods are provided that are useful to treat respiratory diseases such as whooping cough. Further, compositions and methods of immunizing are provided.

Abstract: The present invention relates to Fc variants having decreased affinity for Fc?RIIb, methods for their generation, Fc polypeptides comprising optimized Fc variants, and methods for using optimized Fc variants.

Abstract: The present invention relates to methods and compositions for the therapeutic and diagnostic use in the treatment of diseases and disorders which are caused by or associated with neurofibrillary tangles. In particular, the invention relates to antibodies, which specifically recognize and bind to phosphorylated pathological protein tau-conformers and to methods and compositions involving said antibodies for the therapeutic and diagnostic use in the treatment of tauopathies including Alzheimer's Disease (AD).

Abstract: The invention provides anti-polyubiquitin antibodies and methods of using the same.

Abstract: The invention provides compositions comprising SPARC binding ScFc and its use.

Abstract: The present invention relates to anti- PHF-tau antibodies and methods of making and using them.

Abstract: This invention concerns in general treatment of diseases and pathological conditions with anti-VEGF antibodies. More specifically, the invention concerns the treatment of human patients susceptible to or diagnosed with cancer using an anti-VEGF antibody, preferably in combination with one or more additional anti-tumor therapeutic agents.

Abstract: The disclosure provides compositions, kits, and methods of using a GDF-8 inhibitor to increase lean muscle mass. In embodiments, a GDF-8 inhibitor is an antibody or antigen binding fragment thereof that specifically binds GDF-8. In embodiments, a method comprises providing an exercise regimen for the subject, and administering a composition comprising an effective amount of a GDF-8 inhibitor.

Abstract: This invention provides antibodies that interact with or bind to human nerve growth factor (NGF) and neutralize the function of NGF thereby. The invention also provides pharmaceutical compositions of said antibodies and methods for neutralizing NGF function, and particularly for treating NGF-related disorders (e.g., chronic pain) by administering a pharmaceutically effective amount of anti-NGF antibodies. Methods of detecting the amount of NGF in a sample using anti-NGF antibodies are also provided.

Abstract: This document relates to methods and materials involved in treating cancer (e.g., melanoma). For example, methods and materials involved in using an anti-chronic inflammation treatment (e.g., chemotherapy) in combination with a cancer treatment agent (e.g., a cancer vaccine) to treat cancer are provided.

Abstract: The present invention relates to discovery of the ectopic expression of EDEM2 in a production cell to improve the yield of a useful multi-subunit protein. Thus, the present invention provides for production cell lines, such as the canonical mammalian biopharmaceutical production cell—the CHO cell, containing recombinant polynucleotides encoding EDEM2. Also disclosed is a production cell containing both an EDEM2-encoding polynucleotide as well an XBP1-encoding polynucleotide. Improved titers of antibodies produced by these cell lines are disclosed, as well as the improved cell densities attained by these cells in culture.