Abstract: The present invention concerns novel and improved antibody-conjugates for targeting HER2. The inventors found N that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index.

Abstract: A pharmaceutical composition containing isomyosmine or a pharmaceutically acceptable salt thereof is administered to an individual in need thereof for treating a substance addiction, inclusive of addiction to heroin (diacetylmorphine), cocaine, opioids, methadone, d-methamphetamine, barbiturates, alcohol, benzodiazepines, amphetamines, or buprenorphine. The isomyosmine, along with optional additional therapeutic agent(s), may be administered in a capsule, tablet, or lozenge.

Abstract: A method for producing a compound represented by formula (C) wherein R1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C).

Abstract: The disclosure relates to methods of treating or preventing a disease in a subject by conjointly administering to the subject an arginase inhibitor disclosed herein and a composition comprising immune cells disclosed herein.

Abstract: The present invention relates to protein drug conjugates, methods of manufacturing the same and their use in therapy. In particular, the present invention relates to protein drug conjugates comprising a globular protein, an improved linker and a drug for use in targeted drug delivery applications.

Abstract: Disclosed herein are photodegradable hydrogels and associated kits for selectively capturing and releasing cells. The hydrogels result from cross linking in the presence of a photoinitiator (1) a macromer having a polymeric backbone structure, a photo labile moiety, and a first linking moiety, and (2) a cell-binding moiety having a second linking moiety. These two components are cross-linked by a polymerization reaction of the linking moieties to form a photodegradable hydrogel incorporating the cell-binding moiety within the hydrogel. Also disclosed are methods of making the hydrogels, and methods of using the hydrogels for selectively capturing and releasing cells and for detecting cells in a fluid. Such methods can be used to detect the presence and quantity of certain rare cell types in a biological fluid.

Abstract: Conjugates of an active agent attached to a targeting moiety, such as an HSP90 binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.

Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Abstract: Provided herein are antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers.

Abstract: Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.

Abstract: Drug conjugates of formula [D-(X)b-(AA)w-(L)-]n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein: A is selected from (II) and (III) R1, R2 and R3 is H, ORa, OCORa, OCO—ORa, alkyl, alkenyl, alkynyl, etc.; R3? is, CORa, COORa, CONRaRb, etc; each of R4 to R10 and R12 is alkyl, alkenyl or alkynyl; R11 is H, CORa, COORa, alkyl, alkenyl or alkynyl, or R11 and R12+N+C atoms to which they are attached may form a heterocyclic group; each of R13 and R14 is H, CORa, COORa, alkyl, alkenyl or alkynyl; each Ra and Rb is H, alkyl, alkenyl, alkynyl, etc.

Abstract: The present invention provides an in vitro method for selecting a patient affected with a tumor for a treatment with an antitumor compound, wherein the method comprises a step of measuring the expression level of CDA (Cytidine Deaminase) in a cancer sample from said patient. When the CDA expression level of a cancer sample is lower than the reference expression level, it is indicative that the patient is suitable for a treatment with an antitumor compound selected from the group consisting of the compounds of table 4, in particular aminoflavone. Alternatively, when the CDA expression level of a cancer sample is higher than the reference expression level, it is indicative that the patient is suitable for a treatment with an antitumor compound selected from the group consisting of the compounds of table 3, in particular dasatinib.

Abstract: Antibodies that include a sulfatase motif-containing tag in a constant region of an immunoglobulin (Ig) light chain polypeptide are disclosed. The sulfatase motif can be converted by a formylglycine-generating enzyme (FGE) to produce a formylglycine (fGly)-modified Ig light chain polypeptide. An fGly-modified Ig light chain polypeptide of the antibody can be covalently and site-specifically bound to a moiety of interest to provide an antibody conjugate. The disclosure also encompasses methods of production of such tagged Ig light chain polypeptides, fGly-modified Ig light chain polypeptides, and antibody conjugates, as well as methods of use of same.

Abstract: A method for identifying a tumor that is susceptible to treatment with a TTK inhibitor, including: a) providing a sample of a tumor; b) determining the presence of a mutated CTNNB1 gene in the sample, wherein the mutation is located in exon 3 of CTNNB1 and the presence of a mutated CTNNB1 gene indicates the tumor is susceptible to treatment with a TTK inhibitor. Alternatively, step b) is replaced by the step of determining the presence of a mutated CTNNB1 protein in the sample, wherein the mutation is located in exon 3 of CTNNB1 and the presence of a mutated CTNNB1 protein indicates the tumor is susceptible to treatment with a TTK inhibitor. In a further alternative, step b) includes determining an altered expression of a CTNNB1 regulated gene, whereby an altered expression of a CTNNB1 regulated gene indicates the tumor is susceptible to treatment with a TTK inhibitor.

Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

Abstract: Embodiments of a novel platform for delivering a peptide antigen to a subject to induce an immune response to the peptide antigen are provided. For example, nanoparticle polyplexes are provided that comprise a polymer linked to a peptide conjugate by an electrostatic interaction. The conjugate comprises a peptide antigen linked to a peptide tag through an optional linker. An adjuvant may be included in the nanoparticle polyplex, linked to either the polymer or the conjugate, or admixed with the nanoparticles. The nanoparticle polyplex can be administered to a subject to induce an immune response to the peptide antigen.

Abstract: Disclosed is a method for separating, with a multi-stage distillation column, a mixture containing an active hydrogen-containing compound (A) and a compound (B) that reversibly reacts with the active hydrogen containing compound (A), the method comprising distillation-separating the active hydrogen-containing compound (A) and the compound (B) with the multi-stage distillation column in the presence of an intermediate-boiling-point inactive compound (C) that has a normal boiling point between a normal boiling point of the active hydrogen-containing compound (A) and a normal boiling point of the compound (B) and is chemically inactive for both of the (A) and the compound (B).

Abstract: The present invention relates generally to stable percarboxylic acid compositions comprising, inter alia, at least two stabilizing agents, and various uses for water treatments, including water treatments in connection with oil- and gas-field operations. The present invention also relates to slick water compositions and gel based compositions that comprise stable percarboxylic acid compositions and the use thereof in oil- and gas-field operations.

Abstract: The present invention relates to antibody-drug conjugates (ADCs) wherein a plurality of active agents are conjugated to an antibody through at least one branched linker. The branched linker may comprise a branching unit, and two active agents are coupled to the branching unit through a secondary linker and the branching unit is coupled to the antibody by a primary linker. The active agents may be the same or different. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody. The branched linker may comprise one active agent coupled to the branching unit by a first branch and a second branch that comprises a polyethylene glycol moiety coupled to the branching unit. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g.

Abstract: Provided herein are materials and methods for treating a cancer and/or an infection in a mammal. One or more mitochondrial protein uncoupling protein 2 (UCP2) inhibitors can be administered to a mammal to enhance an immune response produced against an antigen (e.g., a tumor associated antigen or a pathogen associated antigen) present within the mammal.