Abstract: The invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom or a hydroxyl group; two R2 are the same or different and each is a hydrogen atom or a hydroxyl group; R3 is a hydrocarbon group having 8-14 carbon atoms, which optionally has substituent(s); and R4 is a hydrocarbon group having 18-24 carbon atoms, which optionally has substituent(s), or a salt thereof. The invention also provides a method of treating an autoimmune disease or suppressing immunity by administering the aforementioned compound or a salt thereof to a patient in need thereof.

Abstract: The present invention relates to processes for preparing a glucopyranosyl-substituted benzyl-benzene derivative of general formula III, wherein R1 is defined according to claim 1.

Abstract: The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.

Abstract: Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2?- and 3?-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.

Abstract: In summary, the present invention concerns a method for multiple orthogonal labelling of oligonucleotides, preferably RNA or DNA, by simultaneously performing the inverse Diels-Alder reaction (DAinv) and the copper-catalyzed click reaction (CuAAC), wherein the method is employed in a single step by just adding the different reaction components together and incubating the aqueous reaction mixture preferably for one hour at room temperature. In detail, the reaction components are one or more N3-modified labels, a copper compound, a stabilizing ligand, a reducing agent and one or more electron-deficient label-modified dienes that are added together with an at least double-modified oligonucleotide having one more nucleotides containing one or more N3-reactive groups and one or more electron-rich dienophiles, wherein a terminal alkyne moiety is preferably used as N3-reactive group(s) and a frans-cyclooctene moiety or norbornene is preferably used as electron-rich dienophile(s), more preferably frans-cyclooctene.

Abstract: The invention involves the synthesis of nucleic acid structures of controlled size and shape and comprised of a plurality of oligonucleotides. The structures are formed, at least in part, by the self-assembly of single-stranded oligonucleotides. The location of each oligonucleotide in the resultant structure is known. Accordingly, the structures may be modified with specificity.

Abstract: Provided herein are methods for the solid phase synthesis of oligomeric compounds wherein at least one of the capping steps has been modified. More particularly, methods are provided wherein one or more of the capping steps is omitted or performed using reduced equivalents of acetic anhydride. In certain embodiments, the methods provide an enhanced purity profile. In certain embodiments, the methods provide an increased yield. The methods provided herein also provide at least an economic advantage over currently used methods in that reduced amounts of the mixture of capping reagents are required.

Abstract: The present invention relates to a novel ursolic acid derivative as an ursolic acid prodrug form, and to a method for preparing same, wherein the novel ursolic acid derivative as an ursolic acid prodrug can have excellent pharmacokinetic characteristics such as stability and oral absorptivity and exhibit excellent pharmaceutical activities by being converted into an ursolic acid in vivo, and. The ursolic acid derivative can be in an ester form in which C28 carboxylic acid in the ursolic acid is combined with a prodrug of a certain pharmaceutical compound.

Abstract: N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

Abstract: There is provided a method for purifying an antibody using temperature-responsive Protein A, wherein different buffer solutions are used in a washing step of washing a stationary phase having the temperature-responsive Protein A and in an elution step of eluting the antibody captured by the stationary phase, the method including the washing step of washing the stationary phase using a buffer solution at a temperature at which the temperature-responsive Protein A and the antibody are bound and having a first salt concentration, and the elution step of eluting the antibody captured by the stationary phase using a buffer solution at a temperature at which the antibody is released from the temperature-responsive Protein A and having a second salt concentration lower than the first salt concentration.

Abstract: Methods, systems and/or kits for the preparation, purification and isolation of oligonucleotide conjugates, comprising conjugation of modified antibodies or proteins with at least one modified oligonucleotide at greater than 80% efficiency to form oligonucleotide conjugates and isolating the oligonucleotide conjugates from the conjugation solution by binding the conjugates to an immobilized binder, wherein the binder may be a metal ion or an antibody.

Abstract: A molecular separation device includes a chamber having an inlet and an outlet through which flows an aqueous suspension and a porous separation membrane positioned in the chamber substantially orthogonally to the flow of the aqueous suspension. An electrical charging device connects to the separation membrane to apply a periodic electric charge so as to collect components blocked by the porous separation membrane. Related methods are also disclosed.

Abstract: Potent compounds having combined antioxidant, anti-inflammatory, anti-radiation and metal chelating properties are described. Short peptides having these properties, and methods and uses of such short peptides in clinical and cosmetic applications are described.

Abstract: The present application relates to novel fluorinated epoxyketone-based tetrapeptide compounds, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions mediated by proteasome inhibition.

Abstract: In one aspect, the invention relates to an inhibitor of the ?6 integrin/E-cadherin molecular complex for use as a medicament, in particular for the prevention or/and treatment of metastases of a primary cancer disease and a pharmaceutical composition or kit comprising as an active agent at least one of the inhibitors. In a further embodiment, the present invention relates to a method for determining the prognosis of metastatic homing of a primary cancer disease, in particular the aggressiveness of the metastatic potential of a primary cancer disease.

Abstract: Provided are a peptide comprising the amino acid sequence of DEAQETAVSSHEQD, the polynucleotide encoding it, the uses of said peptide for the treatment of the symptoms associated with pain and for the inhibition of the activity of influenza virus, and a pharmaceutical composition containing said peptide.

Abstract: Polypeptides which may be used for preventing or treating allergy to moulds of the Cladosporium and/or Alternaria genus, have up to 30 amino acids in length and comprise: (I) the amino acid sequence: (a) GGYKAAVRPTMLE (SEQ ID NO: 35; Cla35), (b) AE V YQKLK SLTKK (SEQ ID NO: 31; Cla16), (c) VAITYASRAQGAE (SEQ ID NO: 32; Cla25), (d) GHHFKERGT-GSLVIT (SEQ ID NO: 33; Cla26), or (e) ANYTQTKTVSIRL (SEQ ID NO: 34; Cla29); or (II) a T cell epitope-containing variant sequence which is a said amino acid sequence (I) having up to six amino acid modifications, each of which is independently a deletion, substitution or insertion.

Abstract: The purpose of the present invention is to provide a PSF1-derived peptide useful for a specific immunotherapy for cancer patients. The present invention provides: a PSF1-derived peptide which can induce a CTL; and a pharmaceutical composition for treating or preventing cancer, which contains the peptide according to the present invention.

Abstract: The invention relates generally to polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator (uPA), to activatable antibodies and other larger molecules that include the cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator, and to methods of making and using these polypeptides that include a cleavable moiety that is a substrate for at least one protease selected from matriptase and u-plasminogen activator in a variety of therapeutic, diagnostic and prophylactic indications.

Abstract: A polypeptide or multimeric polypeptide construct having the ability to bind to cMet or a complex comprising cMet and HGF, and methods for use are disclosed.

Abstract: ?-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.

Abstract: The present invention relates to analogs of alpha-amanitin, methods of inhibiting RNA polymerase with such compounds, conjugates comprising such compounds, compositions comprising such compounds and conjugates, and methods of treatment using such conjugates.

Abstract: The present invention relates to a method for producing a cyclic peptide compound or a salt thereof which comprises contacting a cyclic lipopeptide compound or a salt thereof with an acylase derived from a microorganism belonging to the genus Pseudomonas to deacylate the lipid acyl moiety of said cyclic lipopeptide.

Abstract: The present invention relates to the use of a peptide, or derivative thereof of general formula X1—X2—X3-Thr-X4-Lys-X5-Arg-X6 for promoting accelerated wound healing with reduced scarring. X1 is Ala or Gly; X2 is Tyr or Phe; X3, X4 and X5 are independently selected from the group comprising Met, Ile, Leu and Val; and X6 is selected from the group comprising Asp, Gln and Glu.

Abstract: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Abstract: The invention relates to a method or process for solution phase chemical manufacture of depsipeptides of the formula I, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.

Abstract: The present disclosure provides solid forms of a compound of formula I. In some embodiments, the present disclosure provides crystalline forms of Compound I. In some embodiments, the present disclosure provides solvate forms of Compound I. In some embodiments, the present disclosure provides amorphous Compound I.

Abstract: The present invention provides methods of preparing extracts of material fermented with Paenibacillus sp., preferably Paenibacillus elgii ourofinensis. The extracts exhibit antimicrobial activity and may be used in the treatment or prophylaxis of infections in animals or plants or as a growth promoter in animals intended for slaughter for human consumption. The invention provides new peptides derived from the fractions of the fermentation of Paenibacillus elgii ourofinensis extract, prepared for example, by n-butanol extraction of the Paenibacillus fermentation broth. The extract may optionally be dried and/or mixed with other components such as appropriate nutritional components to form an animal feed, additional therapeutic adjuvants, or pharmaceutically or agriculturally acceptable carriers. The invention is also related to the isolation of this strain of Paenibacillus, including fermentation in a medium such as corn steep liquor and selection of catalase negative bacteria.

Abstract: A method of regulating expression of a gene in a cell is described, comprising the step of introducing into the cell a recombinant polypeptide comprising a PPR RNA-binding domain which itself comprises at least a pair of PPR RNA base-binding motifs. The PPR RNA base-binding motifs of the PPR RNA-binding domain are operably capable of binding the target RNA molecule with a target RNA sequence. Recombinant polypeptides comprising at least one PPR RNA-binding domain capable of binding to target RNA sequence are also described, together with fusion proteins comprising the recombinant PPR RNA-binding domains as well as isolated nucleic acids useful in preparing the recombinant polypeptides described. Recombinant vectors; compositions comprising the recombinant polypeptides; isolated nucleic acids; recombinant vectors; host cells comprising same; use of same in the manufacture of a medicament for regulating gene expression; as well as systems and kits for regulating gene expression are also described.

Abstract: Compositions, methods, and kits are provided for treating CCR8 mediated diseases with applicability to atopic dermatitis and potential applicability to asthma, prurigo nodularis, nummular dermatitis, neurodeimatitis, and lichen simplex chronicus and some lymphomas, multiple sclerosis, acquired immunodeficiency disease, peritoneal adhesions, Kaposi's sarcoma and atherogenesis—the expression of all of which, at least in part, is mediated by cells expressing the chemokine receptor CCR8. The compositions include proteins and fusion proteins from Molluscum contagiosum Virus (MCV) or variants, analogs and derivatives thereof which exhibit inhibitory activity. Examples of such MCV proteins are MC 148 fusion protein (MC148fp) identified as MC148P-TAT-6xHis (“6xHis” disclosed as SEQ ID NO: 11), and its variants, fragments, analogs and derivatives which possess inhibitory activity.

Abstract: The invention provides a combination of an isolated peptide or peptidomimetic that includes the sequence of SEQ ID NO: 1 or a homolog thereof, and an isolated peptide or peptidomimetic that includes the sequence of SEQ ID NO: 2. The invention also provides a method of treating a BCR-ABL associated disease or a c-ABL associated disease in a subject. The method is based on the use of the aforementioned combination of one or more isolated peptides or peptidomimetics.

Abstract: Methods for improving or modulating targeting specificity of TALE proteins by introducing alternative RVDs into their modular nucleic acid binding domains. Polynucleotides encoding TALE proteins having alternative targeting specificity towards a nucleic acid target sequence. TALE proteins having alternative targeting specificity towards a nucleic acid target sequence and methods of making and using them.

Abstract: The invention relates to the polynucleotide sequence of a nontypeable strain of Haemophilus influenza (NTHi) and polypeptides encoded by the polynucleotides and uses thereof. The invention also relates to NTHi genes which are upregulated during or in response to NTHi infection of the middle ear and/or the nasopharynx.

Abstract: The invention relates to artificial forisome bodies comprising a fusion protein of at least one SEO-F protein or an at least 50-amino acid portion thereof, and at least one additional protein or peptide, with the exception of GFP and the Venus protein, wherein (a) the additional protein or peptide has a mass of at most 30 kDa, or (b) the forisome body further comprises an unfused SEO-F protein or a form of said protein having C-terminal deletions of up to 45 amino acids and/or N-terminal deletions of up to 13 amino acids, wherein the unfused SEO-F protein is selected from proteins having the property of being capable of forming homomeric forisome bodies in the absence of additional SEO-F proteins, or (c) the further protein or peptide is a portion of a second SEO-F protein, with the proviso that one of the two SEO-F proteins in its unfused form is capable of forming homomeric forisome bodies, and the fusion protein is comprised of an N-terminal SEO-F protein portion and a C-terminal SEO-F protein portion,

Abstract: The present invention relates to a synthetic peptide of 19 amino acids, called PnTx(19), constituted from the sequence of the native toxin PnTx2-6 of the Phoneutria nigriventer spider. It also relates to pharmaceutical compositions containing such a peptide and to the use thereof in the treatment of erectile dysfunction and/or in potentiating the erectile function.

Abstract: Described herein relates to methods and compositions for extracting hirudin from a plurality of leeches in vivo. The method may include contacting leeches with inducing membranes containing an inducing agent for a first predetermined time period. The inducing membranes may be removed from the leeches, and the leeches may be contacted with a regurgitation agent for a second predetermined time period in a container such that the leeches are induced to regurgitate regurgitation contents. The regurgitation contents may be collected and purified to obtain the hirudin.

Abstract: Compositions and methods for the treatment of antibiotic resistant Staphylococcus aureus infections are provided comprising ?-lactam antibiotics, as well as a hyaluronic acid binding peptide. The antibiotics include cephalosporins as well as the ?o?-? lactam antibiotic vancomycin. The methods provide administering the composition to the subject in an amount effective to reduce or eliminate the infection.

Abstract: A method for treatment of a mammalian subject for an autoimmune or inflammatory disease, the method comprising: administering to the mammalian subject an effective amount of a polymeric protein comprising five, six or seven polypeptide monomer units; wherein each polypeptide monomer unit comprises an Fc receptor binding portion comprising two immunoglobulin G heavy chain constant regions; wherein each immunoglobulin G heavy chain constant region comprises a cysteine residue which is linked via a disulfide bond to a cysteine residue of an immunoglobulin G heavy chain constant region of an adjacent polypeptide monomer unit; wherein the polymeric protein does not comprise a further immunomodulatory portion; or an antigen portion that causes antigen-specific immunosuppression when administered to the mammalian subject.

Abstract: The invention provides for peptides from syndecan 4 and methods of use therefor. These peptides can inhibit ?6?4 integrin interaction with EGFR, thereby preventing tumor cell growth and tissue invasion.

Abstract: The present invention relates to a method for treating a disease in a subject by modulating an isoform of MKL-1 by administering to said subject a therapeutically effective amount of a modulator of said isoform of MKL1, wherein said isoform of MKL1 comprises the amino acid sequence of SEQ ID NO:1.

Abstract: Provided are novel FcRn antagonist compositions comprising a variant Fc region that binds specifically to FcRn with increased affinity and reduced pH dependence relative to the native Fc region. Also provided are FcRn antagonists with enhanced CD16 binding affinity. Also provided are methods of treating antibody-mediated disorders (e.g. autoimmune diseases) using the these FcRn antagonist compositions, nucleic acids encoding the FcRn antagonist compositions, recombinant expression vectors and host cells for making the FcRn antagonist compositions, and pharmaceutical compositions comprising the FcRn antagonist compositions.

Abstract: A p16 protein variant; a polynucleotide encoding the p16 protein variant; a method for preparing the p16 protein variant; a pharmaceutical composition comprising the p16 protein variant; a method for preventing and/or treating cancer comprising administering the p16 protein variant to a subject; and use of the p16 protein variant in the prophylaxis and/or therapy of cancer.

Abstract: The invention provides for peptides from syndecan 1 and methods of use therefor. These peptides can inhibit ?4?6 interaction with HER2, thereby preventing tumor cell growth and tissue invasion.

Abstract: The present invention relates to the prevention or treatment of inflammatory diseases. The present invention also relates to a method for screening a compound capable of promoting or restoring the resolution of inflammation and which may be useful for preventing or treating inflammatory disorders.

Abstract: A p15 protein variant; a polynucleotide encoding the p15 protein variant; a method for preparing the p15 protein variant; a pharmaceutical composition comprising the p15 protein variant; and a method for preventing and/or treating cancer comprising administering the p15 protein variant to a subject.

Abstract: The present invention generally relates to fusion proteins of antibodies and interleukin-10 (IL-10). More particularly, the invention concerns fusion proteins of antibodies and mutant IL-10 that exhibit improved properties for use as therapeutic agents, e.g. in the treatment of inflammatory diseases. In addition, the present invention relates to polynucleotides encoding such fusion proteins, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the fusion proteins of the invention, and to methods of using them in the treatment of disease.

Abstract: The present invention relates to a method of treating a transient impairment of the motility of the gastrointestinal system resulting from postoperative ileus in a patient wherein said method includes the step of administering a therapeutically effective amount of a peptidyl analog of ghrelin to said patient.

Abstract: The present invention is based on a novel, alternatively spliced human isoform of MD-2 (MD-2s). In addition, the present invention relates to modified MD-2 proteins, wherein one or more tyrosine residues have been mutated to phenylalanine. In various embodiments, the invention relates to methods and kits for preventing, reducing the likelihood of developing and/or treating various conditions using MD-2s. The invention also describes methods of determining the risk of a subject to various conditions.

Abstract: A method of treating a mammal for a condition associated with undesired cell proliferation comprising administering to said mammal an effective amount of a TACI reagent, wherein said reagent extends mean survival time of said mammal by about 10% or more as compared to the absence of administering the TACI reagent.

Abstract: The present application relates to an antigen peptide derived from the sequence of epidermal growth factor receptor having T790M point mutation and a pharmaceutical composition for the treatment of cancer comprising the peptide.