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 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 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 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 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 invention provides compositions and methods for increasing hair growth and decreasing hair loss. In one embodiment, the compositions comprise a plurality of hair growth agents. Optionally, the hair growth agents are selected from the group consisting of: IGF-1, FGF-2, FGF-10, PDGF-AA, Wnt-3a, noggin, ephrin-A3, sonic hedgehog (SHH), BMP-6 and hypoxanthine.

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 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 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.

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 invention discloses a method for preparing a peripheral nerve injury repair promotion stent containing ephrin-B2 protein, which comprises the steps of using the autologous skin of a patient as a material for a neural stent and utilizing nerves at the injured position of autologous peripheral nerves of the patient to obtain Schwann cells used as a material for preparing the neural stent, wherein the material selection mode can control the function damage caused by material selection operation on the patient at a minimum level. The stent has the effect of effective guide on axonal regeneration, and can repair nerve defect with longer distance compared with the prior art. Compared with the repair of ruptured nerves, through the method, the stent is connected between broken ends to promote the repair of missing parts of peripheral nerves based on missing nerves between the broken ends after the peripheral nerves rupture, and the stent is higher in difficulty and clinical application value.

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 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.

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.

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 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.

Disclosed herein are compositions and methods for tumor treatment involving administering to a subject having a tumor with an amount effective to limit tumor growth or metastasis of an ephrin B1 inhibitor, or a pharmaceutically acceptable salt thereof; and / or an inhibitor of tumor exosomal release, or a pharmaceutically acceptable salt thereof

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.

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.

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 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.

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.

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.

Ephrin type receptor tyrosine kinase inhibitors, also known as Eph tyrosine kinase receptor inhibitors, for treating cancer, an inflammatory disease, an autoimmune disease, or a degenerative disease characterized at least in part by the abnormal activity or expression of the Eph receptor tyrosine kinase. The inhibitors are particularly useful for treating certain cancers.

The invention relates to a tumor exosome detection reagent. The tumor exosome detection reagent is composed of magnetic nanoparticles and gold nanoparticles, wherein the surfaces of the magnetic nanoparticles are modified with phosphatidylinositol proteoglycan-1 antibodies, and the surfaces of the gold nanoparticles are modified with A-type hepatic ligand protein receptor-2 antibodies. According to the tumor exosome detection method, the detection time is greatly shortened under the condition that the detection quality is guaranteed, the detection limit is low, the sensitivity and the specificity are high, the purpose of amplifying signals to detect the tumor exosome such as pancreatic cancer is achieved, and the current early diagnosis work such as pancreatic cancer can be better assisted.