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: 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: 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: An antibody prodrug capable of being selectively activated in a central nervous system (CNS) by protease KLK6 includes an antibody for treating a disease or disorder in the CNS; a KLK6 cleavable peptide fused to an N-terminus of a heavy chain and/or a light chain of the antibody; and a blocker fused to an N-terminus of the KLK6 cleavable peptide. The disease or disorder is a cancer, inflammatory disease, autoimmune disease, infectious disease, or neuron degeneration disease.

Abstract: A host cell for protein expression having a lower expression level of a gene, as compared to a wild-type cell, wherein the gene is selected from HDAC8, Dab2, Caspase3, Sys1, Ergic3, Grasp, Trim 23, or a combination thereof. The host cells are CHO cells. The lower expression level of the gene results from RNA interference, which may be achieved by transfecting a vector that contains an shRNA targeting the gene.

Abstract: An immunoconjugate includes an anti-Globo H antibody, or a binding fragment thereof, and a therapeutic agent or a label, having the formula: Ab?(L?D)m, wherein Ab is the anti-Globo H antibody or the binding fragment thereof, L is a linker or a direct bond, D is the therapeutic agent or the label, and m is an integer from 1 to 8. The antibody may be a monoclonal antibody, which may be a humanized antibody. A method for treating a cancer includes administering to a subject in need of such treatment a pharmaceutically effective amount of an immunoconjugate containing an antibody against Globo H, or a binding fragment thereof, and a therapeutic agent covalently conjugated with the antibody.

Abstract: The present invention provides a process for the preparation of a Crassocephalum crepidioides extract, and the extract prepared thereby. The present invention further relates to a pharmaceutical composition/combination comprising the Crassocephalum crepidioides extract. The use of the extract and the composition/combination comprising the extract in the prevention or treatment of cancer is also provided.

Abstract: A bispecific anti-Globo H antibody includes an anti-Globo H antibody that binds specifically to Globo H; and a T-cell targeting domain fused to a CH3 domain of a heavy chain of the anti-Globo H antibody, wherein the T-cell targeting domain binds specifically to an antigen on T-cells; and wherein the anti-Globo H antibody comprises mutations at an effector binding site such that the bispecific anti-Globo H antibody has a diminished effector function. The T-cell targeting domain is a ScFv or Fab from an anti-CD3 antibody.

Abstract: An asymmetric heterodimeric antibody includes a knob structure formed in a CH3 domain of a first heavy chain; a hole structure formed in a CH3 domain of a second heavy chain, wherein the hole structure is configured to accommodate the knob structure so that a heterodimeric antibody is formed; and a T-cell targeting domain fused to the CH3 domain of the first heavy chain or the second heavy chain, wherein the T-cell targeting domain binds specifically to an antigen on the T-cell. The T-cell targeting domain is a ScFv or Fab derived from an anti-CD3 antibody. The asymmetric heterodimeric antibody may have L234A and L235A mutations or L235A and G237A such that its effector binding is compromised.

Abstract: The present invention relates to an antibody or antigen-binding fragment thereof that bind human vascular endothelial growth factor receptor 2 (VEGFR-2). The present invention also relates to a method for inhibiting VEGFR-2-mediated signaling in a subject in need, a method for treating diseases and/or disorders caused by or related to VEGFR-2 activity and/or signaling in a subject afflicted with the diseases and disorders, a method for treating tumor in a subject afflicted with the tumor, a method for inhibiting cell proliferation of endothelial cells in a subject in need, and a method for detecting human vascular endothelial growth factor receptor in a sample.

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.