30 results about "Ephrin" patented technology

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 non-invasive methods for detecting, monitoring, staging, and diagnosing malignant melanoma in a skin sample of a subject. The methods include analyzing expression in skin sample of one or more melanoma skin markers. The melanoma skin markers include IL-1 RI, endothelin-2, ephrin-A5, IGF Binding Protein 7, HLA-A0202 heavy chain, Activin A (βA subunit), TNF RII, SPC4, and CNTF Rα. The skin sample can include nucleic acids, and can be a human skin sample from a lesion suspected of being melanoma.

The present invention relates to compositions and methods of use of cupredoxins, and variants, derivatives and structural equivalents of cupredoxins that interfere with the ephrin signaling system in mammalian cells. Specifically, the invention relates to compositions and methods that use cupredoxins, such as azurin, rusticyanin and plastocyanin, and variants, derivatives and structural equivalents thereof, to treat cancer in mammals. The invention specifically includes mutants with altered Eph binding constants and selectivities.

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.

The invention provides a pyridine compound and application. Based on the find of VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2), EphB4 (Ephrin type-B receptor 4) and TIE-2 compensatory activation, biphenyl arylurea is used as a novel leading compound to analyze conservative conformations of three receptor active sites and find out a general structure region; a molecular hybridization medicine design strategy is adopted to construct a compound library meeting the requirements of the conformations of the general structure region; multi-level activity screening finds out a multi-target inhibitor capable of simultaneously resisting three compensatory paths. A kinase screening test proves that almost pyridine compounds have relatively good kinase inhibition activity; a cell proliferation test proves that almost compounds have relatively strong cell proliferation inhibition activity; structure-activity relationship analysis used as a novel medical effect segment for designing the multi-target inhibitor, and the pyridine compound can be used for preparing an anti-angiogenesis medicine.

Transmembrane B ephrins and their Eph receptors signal hi-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 present invention discloses methods of reducing injury resulting from cardiovascular disease, such as myocardial infarction, and / or promoting myocardial repair. The methods include administering an ephrin and pharmaceutical compositions including ephrins to a subject. Kits useful for accomplishing the same are also provided.

The invention discloses an Eph receptor small molecule inhibitor compound or isomers, non-enantiomers, enantiomers, mesomers, racemes and mixtures thereof, or a pharmaceutically acceptable salt thereof. The Eph receptor small molecule inhibitor compound has the following structural formula: FORMULA. The Eph receptor small molecule inhibitor compound selectively acts on the extracellular binding region of an Eph receptor and an ephrin ligand for the treatment of nervous system diseases in mammals, treatment of vascular system diseases, and inhibition of the occurrence and development of tumor diseases. The invention also discloses a preparation method of the Eph receptor small molecule inhibitor compound at the same time, and the preparation method is simple to operate and good in reproducibility.