30 results about "Ephrin" patented technology

The present invention is directed to compounds of generic formula (I)

which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.

The present invention is directed to compounds of generic formula (I)

which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.

The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

The present invention provides modified cupredoxin derived peptides with pharmacologic activity that have improved pharmacokinetic properties, and methods to use them to treat mammals suffering from various conditions related to the pharmacologic activities. Modifications of the cupredoxin derived peptides include amino acid sequence variants and structural derivations that increase the plasma half-life of the peptide, increase the specific activity of the pharmacologic activity, decrease immunogenicity, and decrease the biotransformation of the peptides. The modified cupredoxin derived peptides can be used in methods to treat mammals for cancer, conditions related to inappropriate angiogenesis, viral and bacterial infections, and specifically HIV and malaria, conditions related to ephrin signaling, and to deliver cargo compounds, including diagnostic compounds, to cancer cells.

It is intended to provide an agent for regulating axon extension during neuranagenesis by regulating ephrin-Eph receptor signaling mechanisms and to provide a mouse having abnormal ephrin-Eph receptor signaling mechanisms. The present invention relates to a regulator of axon extension, comprising an agent for promoting or suppressing the function of α-chimerin, and to a miffy (mfy) mouse derived from a B6 strain, which displays autosomal recessive inheritance of an abnormal walking trait exhibiting a hopping gait with left-right synchronized movement of limbs and has mutation in an α-chimerin gene.

The present invention provides methods and compositions for treatment, screening, diagnosis and prognosis of bladder cancer, breast cancer, colorectal cancer, head and neck cancer, kidney cancer, lung cancer or pancreatic cancer, for monitoring the effectiveness of bladder cancer, breast cancer, colorectal cancer, head and neck cancer, kidney cancer, lung cancer or pancreatic cancer treatment, and for drug development based on Ephrin Type-A Receptor 10 Protein.

Transmembrane B ephrins and their Eph receptors signal bi-directionally. The presently claimed invention describes a cytoplasmic protein, designated PDZ-RGS3, which binds B ephrins through a PDZ domain, and has a regulator of heterotrimeric G protein signaling (RGS) domain. PDZ-RGS3 mediates signaling from the ephrin-B cytoplasmic tail. SDF-1, a chemokine with a G protein coupled receptor, or BDNF, act as chemoattractants for cerebellar granule cells, with SDF-1 action being selectively inhibited by soluble EphB receptor. The claimed invention reveals a pathway that links reverse signaling to cellular guidance, uncovers a novel mode of control for G proteins, and demonstrates a mechanism for selective regulation of responsiveness to neuronal guidance cues. Further, compositions and methods of use are provided for modulating cell migration as a function of chemokines and GPCR interaction, to aid in the treatment of disease states and medical conditions, including cancer and immune responses such as allergy and autoimmune responses. In one embodiment, a method of altering the sensitivity of a cell to a chemokine is provided using a PDZ-RGS3 protein.

The invention provides a pharmaceutical composition for treating glioblastoma. The pharmaceutical composition comprises an expression inhibitor of hepatic ligand protein type A receptor 2 (EPHA2) and an expression inhibitor of platelet-derived growth factor receptor (PDGFRA). The invention also provides a diagnostic reagent for monitoring glioblastoma prognosis, which comprises a first composition for detecting the expression quantity of the EPHA2 gene and a second composition for detecting the expression quantity of the PDGFRA coding gene. The invention provides a scheme for treating GBM by jointly inhibiting PDGFRA and EPHA2 for the first time, and solves the problem that the anti-tumor effect cannot be achieved in clinical application by only using a single PDGFRA inhibitor.

The invention discloses a new use of pristimerin in preparation of an EphB4/Ephrin-B2 signal pathway inhibitor. The EphB4/Ephrin-B2 signal pathway inhibitor can treat diseases caused by EphB4/Ephrin-B2 signal pathway abnormal activation, particularly tumor proliferation and migration a non-small cell lung cancer, angiogenesis, and anti-apoptotic effects caused by EphB4/Ephrin-B2 signal pathway abnormal activation.

Azuvirin peptides are small peptide agents useful in delivering functional moieties, such as sensitizers, chemotherapeutic agents and the like to cancer cells expressing ephrin receptors. The peptides are also useful for administration to a patient suffering from a viral infection, or to an individual facing exposure to a viral infection, especially one caused by the HIV-1 retrovirus.