187 results about "Vascular Endothelial Growth Factor Receptor" patented technology

The present disclosure relates to novel vascular endothelial growth factor receptor (VEGFR)-binding polypeptides and methods for using these polypeptides to inhibit biological activities mediated by vascular endothelial growth factors (VEGFs). The present disclosure also provides various improvements relating to single domain binding polypeptides.

The current invention provides a method for mobilising endothelial progenitor cells (EPC) and/or mesenchymal stem cells (MSC) in a patient, wherein the method comprises the steps of (i) administering a vascular endothelial growth factor receptor (VEGFR) agonist to the patient; and (ii) administering an antagonist of CXCR4 to the patient. Also provided are uses of EPC and MSC harvested using the methods of the invention.

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.

The present invention concerns methods and reagents useful in modulating vascular endothelial growth factor (VEGF, VEGF-A, VEGF-B, VEGF-C, VEGF-D) and/or vascular endothelial growth factor receptor (e.g., VEGFR1, VEGFR2 and/or VEGFr3) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (mRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against VEGF and/or VEGFr gene expression and/or activity. The small nucleic acid molecules are useful in the diagnosis and treatment of cancer, proliferative diseases, and any other disease or condition that responds to modulation of VEGF and/or VEGFr expression or activity.

Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I)

and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).

The present invention relates to human monoclonal antibodies neutralizing vascular endothelial growth factor receptor and the use thereof. More specifically, relates to human ScFv molecules neutralizing vascular endothelial growth factor receptor, and a composition for inhibiting angiogenesis and a composition for treating cancer, which contain the human ScFv molecules. The disclosed monoclonal antibody neutralizing vascular endothelial growth factor receptor shows excellent neutralizing ability in living cells, compared to that of a commercially available antibody against vascular endothelial growth factor receptor, and shows the ability to neutralize vascular endothelial growth factor receptor not only in humans, but also in mice and rats. Thus, the monoclonal antibody will be useful in anticancer studies and will be highly effective in cancer treatment.

The invention discloses a soluble VEGFR (Vascular Endothelial Growth Factor Receptor) difunctional chimera receptor VEGFR31-Ig as well as a preparation method and application thereof in preparing antineoplastic drugs. The soluble VEGFR difunctional chimera receptor VEGFR31-Ig disclosed by the invention can not only be combined with VEGF-A and VEGF-B, but also be combined with VEGF-C or VEGF-D, and can be used for preparing the antineoplastic drugs.

The invention belongs to the technical field of genetically engineered antibody, in particular relates to a fusion protein of tumor vascular endothelial growth factor receptor 2 (VEGFR2/KDR3) antibody and MICA as well as a preparation method and use thereof. In the invention, a full-length antibody of VEGFR2 is linked with a ligand MHC I molecule associated protein A (MICA) of activated receptor of NK cell (NKG2D) through a flexible linker and expressed by CHO cells by utilizing the genetic engineering technology, and the formed fusion protein can act on VEGFR on the surface of a tumor cell to inhibit or kill tumor and inhibit or destroy tumor angiogenesis, and on the other hand, the formed fusion protein can increase the level of MICA on the surface of the tumor cell and stimulate the NK cells to kill tumor cells through identification of NKG2D on the surfaces of the NK cells, thereby reestablishing the immunological surveillance of an body activated by the NKG2D pathway, and enhancing effects of antibody-dependent cell-mediated cytotoxicity (ADCC) and the like mediated by the Fc region of the antibody to kill tumor cells.

The invention belongs to the technical field of genetic engineering antibodies and particularly relates to a whole human source single chain antibody which is designed and expressed by genetic engineering and has specific affinity towards human vascular endothelial growth factor receptor 2 (VEGFR-2). The invention also provides a nucleotide sequence of heavy chain variable region and light chain variable region immunoglobulin molecules, a nucleotide sequence which comprises the heavy chain variable region and light chain variable region immunoglobulin molecules, an amino acid sequence which comprises variable heavy chain and variable light chain immunoglobulin molecules, and a sequence which corresponds to CDR1, CDR2 and CDR3 of a complementary determining region. The invention also provides a method for generating and expressing the anti-VEGFR-2 single chain antibody, by cycling operations of gathering-elution-gathering, an antibody which has specific affinity towards the human vascular endothelial growth factor is screened, and then the single chain antibody is obtained through a prokaryotic cell secretion and expression system and an affinity purification system. The antibody can be coupled with a detectable substance and therapeutic agent.

The invention relates to the technical field of biomedicine, in particular to an improved anti-VEGFR (vascular endothelial growth factor receptor)-2 monoclonal antibody and application. On the basis of the original research, a new phage antibody library is designed by computer-aided simulation by taking two of them with the highest affinity as templates, and improved heavy chain variable region and light chain variable region amino acid sequences are obtained by multi-round screening; the affinity and biological activity of the anti-VEGFR 2 monoclonal antibody are higher than those of the original antibody. The anti-VEGFR 2 monoclonal antibody obtained by the invention has relatively high affinity, can inhibit the binding of VEGFR-2 and a ligand VEGF thereof in vitro and has good biological activity, and can be used for the treatment of tumors, macular degeneration and other diseases caused by neovascularization.

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using a one or more assays configured to detect a kidney injury marker selected from the group consisting of Thymic stromal lymphopoietin, Vascular endothelial growth factor receptor 1, C-C motif chemokine 1, C-C motif chemokine 17, C-C motif chemokine 21, C-C motif chemokine 27, FLT-3 Ligand, Immunoglobulin G subclass 3, Interleukin-1 receptor type I, Interleukin-20, Interleukin-29, Interleukin-7, Platelet-derived growth factor A/B dimer, Platelet-derived growth factor A/A dimer, and MMP9:TIMP2 complex as diagnostic and prognostic biomarkers in renal injuries.

The invention discloses a thienopyrimidine and furopyrimidine derivative, its preparation method and its application in medicines. The derivative is a compound shown as general formula I, general formula II, general formula III or general formula IV. The thienopyrimidine and furopyrimidine pyrimidine derivative provided in the invention has an obvious EGFR (epidermal growth factor receptor) inhibitory activity, and some of the compounds also have an obvious inhibitory activity on VEGFR (vascular endothelial growth factor receptor), so that the thienopyrimidine and furopyrimidine pyrimidine derivative can be expected to be developed into tyrosine kinase EGFR or/and VEGFR inhibitors, which can be used for preparation of drugs preventing or treating diseases related to EGFR and/or VEGFR. Therefore, the derivative provided in the invention provides a new development direction and approach for developing novel tyrosine kinase inhibitor drugs that have low resistance or can alleviate early inhibitor resistance, and has wide application prospect and medicinal value.

The invention relates to the fields of pharmaceutical chemistry and organic chemistry, in particular to isoquinolinone derivatives. The compounds can be used for treating various medical indications associated with postmenopausal symptoms, uterine fiber lesions and arterial smooth muscle cell proliferation, particularly ER-(+) breast cancer by inhibiting alpha-estrogen receptor subtype (ER alpha) and through vascular endothelial growth factor receptor (VEGFR-2) bi-target. Meanwhile, the compounds have an obvious inhibiting effect on tumor metastasis, and have a general formula I.

The present invention relates to the field of eye drops and particularly relates to a nanocrystalline eye drop, and a preparation method and an application thereof. The nanocrystalline eye drop comprises double-soluble macromolecules, single-soluble macromolecules and targeted drugs acting on vascular endothelial growth factor receptors and/or platelet growth factor receptors. The double-soluble macromolecules and the single-soluble macromolecules interact to encapsulate the targeted drugs to form nanocrystallines and maintain stability of the nanocrystallines. The eye drop can quickly penetrate a blood-eye barrier and enter a vitreous body through a special intercellular space penetration and/or pinocytosis method, an effective therapeutic effect is achieved through passive targeting andattachment, and at the same time, the drug is convenient to use.

The related chalketoxime shown as the formula (1) is prepared by heating and reflux reacting the 2', 4'-dihydroxy -6'-methoxyl-3', 5'-dimethylchalcone and hydroxylamine hydrochloride in pyridine, which has well solvability, fit to direct inject for drug, restrains obviously all of the activity of blood vessel endothelium growth factor receptor, HER2 receptor and Tyr kinase as PDGFR receptor, the external growth of cells for breast cancer and liver cancer, and the phosphorylation of KDR in ECV304 cell, HER2 in MDA-MB-453 cell and PDGFR receptor in C6 cell, and benefit to treat tumor.

The invention relates to a drug composition preparation for recombining human vascular endothelial growth factor receptor-antibody fusion protein and preparation thereof. The drug composition preparation specifically comprises recombination fusion protein, a buffering agent, a stabilizing agent, a surfactant and sterilize injection water. The drug composition preparation is capable of effectivelyinhibiting fusion protein accumulating and depositing, hydrolyzing, oxidizing, decarboxamidation and other side reaction, and meanwhile, the stability of the product in pressurizing (high temperature,strong light irradiating, freeze thawing, and the like), accelerating and long-term frozen storing conditions can be effectively improved; and the safety in clinical use can be improved.

The invention relates to the field of gene engineering, and particularly relates to an anti-VEGFR-1 (Vascular Endothelial Growth Factor Receptor-1) mosaic type antigen receptor and lymphocyte capable of expressing the antigen receptor, and aims at providing a new and effective choice for the technical field of antitumor. The technical scheme for solving the technical problems is as follows: a single-chain antibody ScFv is provided, the single-chain antibody can recognize VEGFR-1, the single-chain antibody is prepared into the mosaic type antigen receptor which has a structure of (ScFv-V)-(IgG1-Fc)-(CD4-TM)-(CD3-z), the encoding gene of the antigen receptor is transformed into a plasmid vector, and the plasmid vector is transfected to lymphocyte, so that the lymphocyte has antitumor action, thereby providing the new and effective choice for the field.

The present invention provides immunogenic peptides comprising the amino acid sequence of SEQ ID NO: 1, 2, 13, 32, and peptides comprising the above-mentioned amino acid sequences in which 1, 2, or several amino acids are substituted or added, and having cytotoxic T cell inducibility, and also provides drugs for treating or preventing tumors comprising these peptides. The peptides of this invention can be used as vaccines.