The present invention provides kinase inhibitor analogs with improved properties, such as improved efficacy, pharmacokinetics, safety, and specificity. In some embodiments, the present invention provides lapatinib analogs that provide therapeutic benefits.

The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition: ##STR00001##

Provided are imidazopyrazine compounds, particularly including 6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions: ##STR00001##

The present invention relates to FLT3 receptor antagonists or inhibitors of FLT3 receptor gene expression for the treatment or the prevention of pain disorders.

For efficient analysis of a protein-protein interaction, the present disclosure provides a kit for analyzing a protein-protein interaction, the kit including: a 1.sup.st expression vector including a 1.sup.st polynucleotide and a multi-cloning site, wherein, the 1.sup.st polynucleotide is operably linked to a promoter and encodes a 1.sup.st fusion protein having a 1.sup.st fluorescence protein and a 1.sup.st self-assembly protein, and the multi-cloning site is a site where a polynucleotide encoding a bait protein may be operably linked to the polynucleotide encoding the 1.sup.st fusion protein; and a 2.sup.nd expression vector including a 2.sup.nd polynucleotide and a multi-cloning site, wherein, the 2.sup.nd polynucleotide is operably linked to a promoter and encodes a 2.sup.nd fusion protein having a 2.sup.nd fluorescence protein and a 2.sup.nd self-assembly protein, and the multi-cloning site is a site where a polynucleotide encoding a prey protein may be operably linked to the polynucleotide encoding the 2.sup.nd fusion protein.

A method of determining a treatment for an inflammatory disorder in a subject, is disclosed. The method comprises determining an amount of SRSF6 in a sample from the subject, wherein an amount of the SRSF6 is indicative of the treatment. Methods of diagnosing inflammatory disorders and treating same are also disclosed.

The Present invention relates to antibodies that immunospecifically bind to phospho-Akt and certain p-Akt substrates. The invention encompasses human and humanized forms of the antibodies and their use in treating cancers and other proliferative disorders. The invention also relates to p-Akt derived peptides useful for preparing the antibodies. Methods and compositions for detecting, diagnosing, treating or ameliorating a disease or disorder, especially cancer and other proliferative disorders using the present antibodies also are disclosed.

Provided are improved methods for identifying the substrate recognition specificity or activity of a protease, convertase (sortase), or kinase. In some embodiments, methods are provided for identifying the endogenous protease or convertase cleaving patterns (e.g., “cleaveOme”) inside the secretory pathway of a living cell. Select embodiments involve aspects of yeast endoplasmic reticulum sequestration screening and next generation sequencing. Methods of producing polypeptides in Kex2 knockout yeast are also provided.

The present invention provides compositions and methods for detecting the expression and/or activation levels of components of signal transduction pathways in tumor cells such as triple-negative metastatic breast tumor cells. Information on the expression and/or activation levels of components of signal transduction pathways derived from use of the present invention can be used for cancer diagnosis, prognosis, and in the design of cancer treatments.

Provided are compounds capable of enhancing the ability of receptor-type tyrosine-protein phosphatase delta (PTPRD) to dephosphorylate a kinase. Also disclosed is a method of treating a tauopathy or restless leg syndrome in a subject comprising administering to the subject an effective amount of a disclosed compound. Also disclosed are kits comprising the compounds together with instructions for treating a condition and/or a compound known for treating the condition. Finally, disclosed herein is a screening method suitable for identifying positive allosteric modulators of the ability of a receptor-type tyrosine-protein phosphatase delta (PTPRD) to dephosphorylate a kinase.