Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

Abstract: Disclosed are methods and compositions for treating traumatic brain injury (TBI). A brain injury-specific 4-amino acid peptide (sequence CAQK), identified by in vivo phage display screening in mice with acute brain injury, shows selective binding to mouse and human brain injury lesions, and when systemically injected, specifically homes to sites of injury in penetrating and non-penetrating (controlled cortical impact) brain injury models. Significantly, the peptide alone produces therapeutic effect and so can be used in the absence of any other therapeutic compound.

Abstract: Ligand-specific HVEM variants, compositions comprising such variants, and methods of treating inflammatory diseases comprising administering such variants, are provided.

Abstract: The present invention relates to the seminal discovery that BTLA agonist antibodies modulate the immune system. Specifically, the present invention provides antibodies which bind BTLA in the activated state enhancing BTLA signaling. The present invention further provides methods of treating immune and inflammatory diseases and disorders with a BTLA agonist antibody.

Abstract: Provided herein are agonists of the apelin receptor of Formula (I): for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

Abstract: Provided herein are biomolecule conjugates, and methods of use thereof, wherein the conjugate comprises a cytokine, typically an immunopotentiating cytokine, and a peptide comprising or consisting of the sequence CSGRRSSKC (SEQ ID NO:1). Biomolecule conjugates of the invention find application, inter alia, in the treatment of tumours, atherosclerosis and fibrosis, and the degradation of ECM associated therewith. Also provided herein are uses of a peptide comprising or consisting of the sequence of SEQ ID NO:1, optionally linked to a detectable agent and/or a carrier, in the detection and/or localisation of tumour, atherosclerotic and fibrotic tissue.

Abstract: Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Abstract: Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the following formula (I): wherein X1 represents a nitrogen atom or CR9, R1 represents a hydrogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a halogen atom, R3 represents a hydrogen atom or a halogen atom, R4 represents a hydrogen atom or a halogen atom, and R5 represents a C1-C3 alkylsulfonyl group, a substituted C1-C6 alkyl group, a substituted C1-C6 haloalkyl group, a substituted C1-C6 alkoxy group, or a substituted C1-C6 alkylamino group, or a pharmacologically acceptable salt thereof.

Abstract: The present invention relates to a novel azole derivative as an apelin receptor agonist and a method for treating cardiovascular disease, diabetic disease, renal disease, hypertension, and arteriosclerosis, etc., using the same. The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof wherein X1 represents —N? or —CH?, X2 represents —CH? or —N?, R1 and R2 each represent a C1 to C6 alkoxy group or the like, R3 represents a heteroaryl group (the heteroaryl group is optionally substituted by a methyl group or the like) or the like, and R4 represents a C1 to C6 alkylthio group or a C2 to C6 alkenyl group (the C1 to C6 alkylthio group and the C2 to C6 alkenyl group are each optionally substituted by one carboxy group or the like) or the like.

Abstract: Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject.

Abstract: Provided herein are compounds that modulate the activity of inhibitor of apoptosis proteins (IAPs), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Abstract: Disclosed are compositions and methods for identifying a solid tumor cell target. Compositions and methods for treating prostate cancer are also disclosed. Further, cancer therapeutic compositions comprising CT20p are disclosed. Nanoparticles that are conjugated with a targeting ligand that is a substrate for a solid tumor-specific cell protein are disclosed.

Abstract: Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.

Abstract: Disclosed are peptides and peptidomimetics that in some embodiments include the amino acid sequence KRGARST or (SEQ ID NO: 1), AKRGARSTA or (SEQ ID NO: 2), or CKRGARSTC (SEQ ID NO: 3).

Abstract: Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.

Abstract: An implant is provided comprising a substrate having one or more nanoceria coatings coated at least partially thereon, wherein the one or more nanoceria coatings comprise surface cerium having a 3+/4+ oxidation state ratio such that the one or more nanoceria coatings exhibit catalase mimetic activity, superoxide dismutase mimetic activity, or both. Methods are provided for forming a nanoceria coaling. The coating has nanoceria having a surface cerium 3+/4+ oxidation state ratio such that such that the coating exhibits catalase mimetic activity, superoxide dismutase mimetic activity, or both. Also disclosed is a method of reducing degradation of an implant by placing nanoceria in proximity to a bone-implant interface.

Abstract: Provided herein are, inter alia, compositions that bind to a PDZ1 domain of MDA-9/Syntenin (syndecan binding protein: SDCBP), thereby inhibiting MDA-9/Syntenin activity, and methods of use of same. The compositions and methods provided herein are useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.