Abstract: An immunoconjugate having the Formula Ab-[L1-(A-L2-B)m]n, wherein: (a) Ab is an antibody or a binding fragment thereof; (b) L1 and L2 are each independently a linker, wherein L1 and L2 are the same or different and wherein L1 links to L2; (c) A is a target-protein ligand/binder; (d) B is a ubiquitin ligase ligand/binder, and (e) n and m are independently integers from 1 to 8. The target protein includes kinase, G protein-coupled receptors, transcription factor, phosphatases, and RAS superfamily members.

Abstract: Disclosed are compounds of formula (I) below and tautomers, stereoisomers, isotopologues, or pharmaceutically acceptable salts thereof: in which each of variables R1, ring A, L, W, V, and G is defined herein. Also disclosed are a method for treating disease or disorder mediated by Tyro3, Axl, and/or Mer kinase with a compound of formula (I) or a tautomer, stereoisomer, isotopologue, or salt thereof and a pharmaceutical composition containing same.

Abstract: The present invention provides a compound of formula (1): wherein X, Y, Z1, Z2, R1, R2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention rurthe r provides a process for preparing the compound.

Abstract: An antibody, or an antigen-binding fragment there, binding human ENO1 (GenBank: AAH506421.1) is provided. Methods for treating an ENO1 protein-related disease or disorder, inhibiting cancer invasion and diagnosis of cancer are also provided.

Abstract: A humanized anti-Globo H antibody, or an scFv or Fab fragment thereof, comprising a heavy-chain variable domain having three complementary regions consisting of HCDR1, HCDR2, and HCDR3 and a light-chain variable domain having three complementary regions consisting of LCDR1, LCDR2, and LCDR3, wherein the sequence of HCDR1 is GYISSDQILN (SEQ ID NO:4), the sequence of HCDR2 is RIYPVTGVTQYXHKFVG (SEQ ID NO:5, wherein X is any amino acid), and the sequence of HCDR3 is GETFDS (SEQ ID NO:6), wherein the sequence of LCDR1 is KSNQNLLX?SGNRRYZLV (SEQ ID NO:7, wherein X? is F, Y, or W, and Z is C, G, S or T), the sequence of LCDR2 is WASDRSF (SEQ ID NO:8), and the sequence of LCDR3 is QQHLDIPYT (SEQ ID NO:9).

Abstract: An anti-human T-cell immunoglobulin domain and mucin domain 3 (TIM-3) antibody, can bind the peptides, comprising the amino-acid sequence RKGDVSL (SEQ ID NO: 9) and/or EKFNLKL (SEQ ID NO: 10) of human TIM-3 protein. The antibody can regulate immune cell activity. The antibody or binding fragment thereof is useful in diagnosis, prognosis, and treatment of cancers that have been reported to express cell-surface TIM-3 such as lung, liver, esophageal cancer and solid tumors.

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein L is NR8 or O; R1, R2, R3, R4, R5, R6 and R7 are defined herein. Compounds of formula (I) are useful for inhibition of protein kinases. Methods of using compounds of formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: A compound, capable of inhibiting kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof. The compound can be used in the treatments of diseases or conditions mediated by CSF-1R, c-KIT, FLT3, or PDGFR kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

Abstract: A detoxified recombinant E. coli heat-labile enterotoxin mutant, LTS61K, is employed as a carrier protein to conjugate polysaccharide. The LTS61K contains a mutated mature sub-unit A (LTA) that includes lysine at amino acid position 61 and a wild-type mature sub-unit B (LTB). Various types of bacterial capsular polysaccharide antigens were chemically conjugated with the LTS61K protein by a reductive amination reaction. The conjugated polysaccharide-LTS61K products were physically, chemically and biochemically identified as soluble form. Rabbits were immunized intramuscularly to determine the immunogenicity of conjugated vaccines by ELISA to detect anti-polysaccharide antigen IgG titers and serum bactericidal assay thereby determining the functional activity of the antibodies. Study results show that conjugated polysaccharide-LTS61K vaccines induce higher polysaccharide-specific IgG titers and greater bactericidal activity in sera than that of polysaccharide alone or polysaccharide mixed with LTS61K.

Abstract: A process for modifying glycoproteins is provided. The invention also provides a process for producing glycoprotein payload conjugates, as well as the conjugates produced thereby.

Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.

Abstract: The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, R1, R2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention further provides a process for preparing the compound.

Abstract: A compound for inhibiting BMI-1/MCL-1 having a structure of Formula (I), wherein the various groups are as described. A pharmaceutical composition for treating cancer includes an effective amount of a compound of Formula (I).

Abstract: The present invention is related to the use of an overground part of Hedychium coronarium Koenig in lowering blood glucose, increasing insulin levels and treating and/or preventing diabetes without overly reducing blood glucose in a subject; i.e., not reducing blood glucose in a fasting subject. The present invention also relates to an extract and composition of the overground part of Hedychium coronarium Koenig and its use in lowering blood glucose, increasing insulin levels and treating and/or preventing diabetes.

Abstract: A humanized anti-Globo H antibody, or an scFv or Fab fragment thereof, comprising a heavy-chain variable domain having three complementary regions consisting of HCDR1, HCDR2, and HCDR3 and a light-chain variable domain having three complementary regions consisting of LCDR1, LCDR2, and LCDR3, wherein the sequence of HCDR1 is GYISSDQILN (SEQ ID NO:4), the sequence of HCDR2 is RIYPVTGVTQYXHKFVG (SEQ ID NO:5, wherein X is any amino acid), and the sequence of HCDR3 is GETFDS (SEQ ID NO:6), wherein the sequence of LCDR1 is KSNQNLLX?SGNRRYZLV (SEQ ID NO:7, wherein X? is F, Y, or W, and Z is C, G, S or T), the sequence of LCDR2 is WASDRSF (SEQ ID NO:8), and the sequence of LCDR3 is QQHLDIPYT (SEQ ID NO:9).

Abstract: A regioselective one-step process for the synthesis of 2-hydroxyquinoxaline of Formula (1) or tautomers thereof: comprising reacting 1,2-phenylenediamine of Formula (2): with an excess amount of glyoxylic acid, glyoxylic acid monohydrate, or a 2,2-dialkoxyacetic acid of Formula (3): at a low temperature; wherein R1 and R2 are as defined in the specification.

Abstract: A recombinant protein drug includes a parent protein drug coupled with a modified kininogen-1 peptide. The modified kininogen-1 peptide has the sequence of SEQ ID NO:2 or a homolog having a sequence identity of 80% or higher. The parent protein drug is a bispecific antibody having a first targeting domain linked by a bridging domain with a second targeting domain. The modified kininogen-1 peptide is fused between the first targeting domain and the bridging domain, or between the bridging domain and the second targeting domain. A method for increasing the serum half-life of a protein drug includes constructing a fusion protein comprising the protein drug coupled with a modified kininogen-1 peptide.

Abstract: An antibody, or an antigen-binding fragment there, binding human ENO1 (GenBank: AAH506421.1) is provided. Methods for treating an ENO1 protein-related disease or disorder, inhibiting cancer invasion and diagnosis of cancer are also provided.

Abstract: The present invention provides a modified antigen-binding Fab fragment. An antigen-binding molecule comprising the antigen-binding Fab fragment and a composition comprising the molecule are also provided.

Abstract: A compound, capable of inhibiting kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof. The compound can be used in the treatments of diseases or conditions mediated by CSF-1R, c-KIT, FLT3, or PDGFR kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.