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30 results about "Alpha-v beta-3" patented technology

ΑVβ₃ is a type of integrin that is a receptor for vitronectin. It consists of two components, integrin alpha V and integrin beta 3 (CD61), and is expressed by platelets. Furthermore, it is a receptor for phagocytosis on macrophages or dendritic cells.

Radioactive nuclide marked RGD polypeptide medicament and preparation method thereof

The invention relates to a radionuclide-marked RGD polypeptide medicine and a preparation method thereof. The medicine comprises RGD polypeptide, a bifunctional Chelator and radioactive Nuclide, wherein the RGD polypeptide is RGD cyclic peptide dimer, namely E(L-c(RGDxK))2, which is synthesized by connecting a connecting agent L and an RGD polypeptide monomer and dimerizing two RGD polypeptide monomers connected with the connecting agent L; the radioactive Nuclide marks the RGD cyclic peptide dimer through the bifunctional Chelator; and a pharmacokinetic modified molecule PKM is also connected between the RGD cyclic peptide dimer and the bifunctional Chelator. The radionuclide-marked RGD polypeptide medicine is Nuclide-Chelator-PKM-E(L-c(RGDxK))2, and is a colorless and transparent liquid injection solution. The radionuclide-marked RGD polypeptide medicine is used for diagnosing and treating integrin alpha v beta 3 positive tumor.
Owner:PEKING UNIV

M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity

An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.
Owner:AJITO KEIICHI +7

Dual-targeting ultrasonic contrast agent and preparation method thereof

The invention discloses a dual-targeting ultrasonic contrast agent and a preparation method thereof. The contrast agent is an Integrin alpha v beta 3 / MCP-1 dual-targeting micro-vesicle, the dual-targeting micro-vesicle comprises a lipid shell and a gas inner core, and the external surface of the lipid shell is connected with an Integrin alpha v beta 3 monoclonal antibody and an MCP-1 monoclonal antibody. Through the combined application of different target spots, the targeting efficiency of the contrast agent can be effectively increased, and the degree of enrichment of the carrying genes in the target tissue can be greatly increased. In addition, the contrast agent disclosed by the invention is an ultrasonic contrast agent with double functions of development and treatment, and tumor images can be accurately observed in real time through an ultrasonic imaging system; and after gene transfection is realized through high-strength ultrasonic irradiation, the tumor gene treatment effect can be achieved.
Owner:SHENZHEN PEOPLES HOSPITAL

Fluorescence probe for targeting tumor cells and new vessels and preparation method thereof

The invention provides a fluorescence probe for targeting tumor cells and new vessels. The fluorescence probe can solve the problem of selective imaging for cancer cells of high-expression integrin alpha v beta3. According to the design of the molecular structure of the fluorescence probe provided by the invention, RGD is used as a recognition group for performing multi-site modification on triaryl fluorophore so as to construct a multivalent probe capable of combining with integrin alpha v beta 3. The probe is capable of selectively imaging the cancer cells of high-expression integrin alpha vbeta 3 at cellular level and is capable of realizing the targeting imaging of a tumor site in vivo. Meanwhile, the synthetic process of the fluorescence probe provided by the invention is simple andeasy, the raw materials are low-cost and easily acquired, the preparation cost is low and the fluorescence probe is easy for popularization.
Owner:川北医学院

Exosome carrier of target integrin alpha v beta 3 and preparation method and application of exosome carrier

The invention relates to the technical field of medicine, in particular to an exosome carrier of a target integrin alpha v beta 3 and a preparation method and application of the exosome carrier. Mononuclear suspension cells THP-1 are adopted and stimulated by PMA of the certain concentration to obtain the exosome carrier, the surface of an exosome after separating contains an RGD target molecule metalloprotease disintegrin family 15, and the target integrin receptor alpha v beta 3 can be obtained. The in-vitro releasing experiment shows that the prepared exosome can slowly release loaded chemotherapeutic medicine, and the better capacity of jointly loading genes and the chemotherapeutic medicine is achieved. In the tumor treatment process, the exosome can enhance the effects of cells of aspecificity target overexpression integrin alpha v beta 3 on tumor cells through the chemotherapeutic medicine or gene medicine, apoptosis of tumor cells is promoted, and therefore the exosome carrierforms a targeted and efficient low-toxicity bionic nanoscale delivery system of tumor treatment.
Owner:SHANGHAI NINTH PEOPLES HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE

Amino cyanine fluorescent dyes and preparation method therefor and application thereof

The invention discloses amino cyanine fluorescent dyes connected with cyclopeptide [cyclo(RGD)] and a preparation method therefor and application thereof. The structural formula of the compounds is shown in I. The compounds consist of structural units III and III; the structural unit II is a derived cyanine dye structure which is water soluble fluorescent molecules, the spectrum of which has relatively great Stokes shift, and the molecules have relatively less toxicity to normal cells; the structural unit III is a cyclopeptide structure of a specific ligand of an alpha v beta 3 integrin receptor and can be used for targeted orientation. The fluorescent dyes have the double function characteristic of tumor imaging diagnosis and targeted therapy.
Owner:DALIAN UNIV OF TECH

Cancer cell-targeting structural molecule and use thereof

The invention discloses a cancer cell-targeting structural molecule and a use thereof. A molecule shown in the formula (I) reacts with a connection molecule containing a carboxyl structure and a maleimide group so that the cancer cell-targeting structural molecule is produced by a dehydration synthesis reaction of an amino group and a carboxyl group. The cancer cell-targeting structural molecule can be bonded with a sulfydryl (-SH)-modified nucleotide molecule, can be directly applied to a human body by blood vessel administration, can be specifically bonded with cancer cells expressing integrin family alpha v beta 3 acceptors or with new vessel endothelial cells in cancer tissue, can effectively penetrate a cell membrane by receptor-mediated endocytosis, and can convey the nucleotide molecule into cytoplasm. In the formula (I), n is in a range of 1-10.
Owner:WUHAN ZEZHI BIOLOGICAL PHARMA +1

Iminodiacetic-acid-containing 99mTc-marked RGD polypeptide tumor diagnosis drug and preparation method thereof

The invention provides a 99mTc complex taking iminodiacetic acid as a difunctional chelating agent. Structure of the complex is shown as a formula (1). The complex has the advantages of simplicity in preparation, low cost, high marking rate, radiochemical purity, target to non-target ratio and tumor uptake value, long residence time and low liver-kidney background. The complex can serve as a novel photographic developer marked by technetium-99m and used for positive tumor diagnosis of intergrin alpha v beta 3 receptor to be applied in the technical field of radioactive medicinal chemistry and clinical nuclear medicine.
Owner:FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE

Nuclear medicine of structure modified RGD polypeptide

ActiveCN110227169AHigh stability in vivo and in vitroHigh tumor uptakePeptidesRadioactive preparation carriersInvolucrinDisintegrin
The invention provides a structure modified RGD polypeptide, a complex formed by the polypeptide and radionuclides and a medicinal composition containing the complex. The medicinal composition is usedfor diagnosing or treating integrin alpha v beta 3 positive tumors. The complex has the following definitions: A in the A-(L)n-RGD polypeptide has a structure as shown in the specification, L represents a linker arm molecule and has a structure as shown in the specification, and m is an integer of 1-8.
Owner:PEKING UNIV

Integrin targeted MnOL-Gd hybrid bimetallic paramagnetic nanocolloid and application in magnetic resonance imaging of angiogenesis

The invention discloses an integrin targeted MnOL-Gd hybrid bimetallic paramagnetic nanocolloid (alpha v beta 3-MnOL-Gd NC) and application in magnetic resonance imaging (MRI) of angiogenesis. The alpha v beta 3-MnOL-Gd NC provided by the invention is obtained by coupling alpha v beta 3 targeted specific biomolecules of polyethylene glycol 2000 integrated phosphatidyl ethanolamine to the surfaces of MnOL-Gd hybrid bimetallic paramagnetic nanoparticles. Research shows that, the alpha v beta 3-MnOL-Gd NC is effective in imaging of angiogenesis, and can generate specific angiogenesis imaging high signal contrast 2 hours after injection. Therefore, the alpha v beta 3-MnOL-Gd NC disclosed by the invention can be used for T1 weighted MR molecular imaging of angiogenesis, and is free of obvious allergic reaction side effect, thus providing a new technological means for magnetic resonance imaging of angiogenesis.
Owner:HARBIN MEDICAL UNIVERSITY

Chitosan covalently linked with small molecule integrin antagonist for targeted delivery

The invention relates to the chitosan polymer derivatives of formula I:and pharmaceutically acceptable salts and esters thereof, wherein Y, X1, X4, R1, R2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4β1) and alpha-V-beta-3 (αVβ3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins.
Owner:F HOFFMANN LA ROCHE & CO AG

Fructose and RGD peptide co-modified dual-targeting triple-negative breast cancer lipid material

InactiveCN110522923AImproving the ability to target triple-negative breast cancerOrganic active ingredientsPharmaceutical non-active ingredientsTherapeutic effectAlpha-v beta-3
The present invention discloses a novel lipid material for realizing transfer of triple negative breast cancer targeted drugs. The novel lipid material takes lysine as a connecting group to respectively connect a cholesteric part, a fructose part and an RGD part. Affinities between fructose in the novel lipid material and a fructose transporter GLUT5, and between RGD in the novel lipid material and an integrin receptor alpha v beta 3 are respectively utilized to realize double targeting functions of the triple negative breast cancer and exert stronger targeted treatment effects on the triple negative breast cancer. The novel liquid material can be sued for different dosages of liposomes, nanoparticles, micelle, etc. A prepared paclitaxel-loaded liposome has obvious triple negative breast cancer targeting property and a wide application prospect.
Owner:SICHUAN UNIV

Structural molecule for affinity and target cell uptake capability of enhanced integrin receptor and application thereof

The invention discloses a structural molecule for affinity and target cell uptake capability of enhanced integrin receptor. The structural molecule has a molecular structure shown in a formula (I); the structural molecule is obtained by carrying out reaction between two cRGD oligopeptides and 6-aminocaproic acid, glutamate oligopeptide or / and arginine oligopeptide, 8-amino-3,6-dioxaoctanoic acid or 3-maleimidopropionic acid and the like to perform dehydration condensation on amino and carboxyl. According to the structural molecule disclosed by the invention, tumor cells expressing an alpha v beta 3 receptor and neovascular endothelial cells can be specially combined, the carried molecules such as nucleotide enter cytoplasm through receptor-mediated endocytic uptake, so that the uptake efficiency of expression cells of the alpha v beta 3 receptor is improved and the release of the carried molecules from a target cytoplasm endosome is promoted, and therefore, the structural molecule can be applied to preparation of targeted therapy drugs or disease diagnosis tracer agents.
Owner:WUHAN ZEZHI BIOLOGICAL PHARMA

PEGylated Fe3+/ PEI genetic vector based on functional peptide R9 modification and preparation method and application of PEGylated Fe3+/ PEI genetic vector

The invention relates to a PEGylated Fe3+ / PEI genetic vector based on functional peptide R9 modification and a preparation method and application of the PEGylated Fe3+ / PEI genetic vector. The genetic vector contains polyethylene glycol modified Fe3+ / polyethyleneimine and a conjugate formed by functional peptides R9. The PEGylated Fe3+ / PEI genetic vector based on functional peptide R9 modification has the advantages that metal ions Fe3 react with PEI at first, PEG modification is carried out to form PEGylated Fe3+ / PEI, then the functional peptide R9 which has ability of improving nuclear delivery and is targeted at alpha v beta 3 is synthesized, R9 is coupled with a PEG-Fe3+ / PEI by a crosslinking technology, and therefore, a novel virogene-free vector system PEG-Fe3 + / PEI is established. On the basis of reducing PEI cytotoxicity, in-vivo targeting property and nuclear delivery ability are improved, then the transfection efficiency of the vector in vivo is improved, and an effective way is searched for final application of gene therapy on clinical treatment.
Owner:SHANGHAI OCEAN UNIV

A class of 1,3-dihydro-1-oxo-2h-isoindole compounds and their uses

The invention discloses a type of 1,3-dihydro-1-oxo-2H-isoindole compounds (I) and pharmaceutically acceptable salts thereof and also discloses application of the compounds in preparation of medicines for preventing or / and treating various symptoms or diseases such as tumor metastasis, tumor growth, solid tumor growth, angiogenesis, retinopathy, macular degeneration, osteoporosis, arthritis, smooth muscle cell migration and atherosclerosis caused by integrin alpha v beta 3 mediation. The structural formula is as shown in the specification.
Owner:SICHUAN UNIV

Tumor targeted cordycepin nanometer capsules

The invention discloses tumor targeted cordycepin nanometer capsules and a preparation method thereof. The method comprises the following steps of firstly preparing RGD modified apolipoprotein A I(ApoAI), and then constructing nanometer capsules from the RGD modified apolipoprotein A I(ApoAI), phospholipid and cordycepin. RGD peptide is a specific ligand of an integrin alpha v beta 3, and the integrin alpha v beta 3 gene is subjected to zero expression or little expression in majority of normal organ systems and normal vascular endothelial cells, and is subjected to overexpression on the surfaces of various tumor cells and tumor regenerated blood vessel endothelial cells, so that after being subjected to RGD modification, the nanometer capsules have good targeting effects on tumors, the effective concentration of cordycepin in tumor positions can be increased, and the antitumor effects of the cordycepin can be reinforced.
Owner:南京广方生物科技有限公司

Integrin-targeted manganese-gadolinium hybrid bimetallic paramagnetic nanocolloids and their application in magnetic resonance imaging of neovascularization

The invention discloses an integrin targeted MnOL-Gd hybrid bimetallic paramagnetic nanocolloid (alpha v beta 3-MnOL-Gd NC) and application in magnetic resonance imaging (MRI) of angiogenesis. The alpha v beta 3-MnOL-Gd NC provided by the invention is obtained by coupling alpha v beta 3 targeted specific biomolecules of polyethylene glycol 2000 integrated phosphatidyl ethanolamine to the surfaces of MnOL-Gd hybrid bimetallic paramagnetic nanoparticles. Research shows that, the alpha v beta 3-MnOL-Gd NC is effective in imaging of angiogenesis, and can generate specific angiogenesis imaging high signal contrast 2 hours after injection. Therefore, the alpha v beta 3-MnOL-Gd NC disclosed by the invention can be used for T1 weighted MR molecular imaging of angiogenesis, and is free of obvious allergic reaction side effect, thus providing a new technological means for magnetic resonance imaging of angiogenesis.
Owner:HARBIN MEDICAL UNIVERSITY

Targeting tumor neovasculature with modified chimeric antigen receptors

A T cell transduced with a chimeric antigen receptor can be administered to a host to kill cancer cells. The chimeric antigen receptor can include a targeting moiety with a strong binding affinity to Alpha v Beta 3 integrin, including but not limited to an echistatin polypeptide. The targeting moiety can also be modified to have a reduced binding affinity to Alpha 5 Beta 1 integrin.
Owner:UNIV HOUSTON SYST

Aptamer Specific to Integrin alpha-v-beta-3 and Use Thereof

The present invention relates to DNA aptamer specifically binding to integrin αvβ3, and a composition for diagnosis of cancer or cancer metastasis comprising the same as an active ingredient. And, the present invention relates to a composition for imaging tumor regions comprising the aptamer, and a contrast medium comprising the same.
Owner:POSTECH ACAD IND FOUND +1

RGD-type polypeptide pet imaging agent targeting integrin αvβ3 and its preparation method and application

The invention discloses an RGD (Arg-Gly-Asp)-like peptide PET (positron emission tomography) developing agent of targeting integrin alpha v beta 3 and a preparation method thereof. The preparation comprises the following steps of: performing 1, 3 dipolar cycloaddition reaction of nitrine and alkynyl in the terminal position on a compound B and a compound C under the catalysis of Cu (I) in a solvent to prepare a compound A. The compound A can be used for diagnosing tumors, cardiovascular diseases and other diseases, such as malignant glioma, melanoma, H22 liver cancer and the like. The invention finds that the RGD-like peptide PET developing agent can specifically target the tumors with high expression of alpha v beta 3 by studies. A marking method of the PET developing agent is simple and universal, a reaction system is stable, conditions are mild, and the radiochemical purity, the specific activity and the radiochemical yield are higher. RGD-like peptide monomers used in the preparation method are low in production cost and convenient to perform large-quantity synthesis and modification, and the used other chemical reagents are low in cost and easy to obtain.
Owner:SHANGHAI ATOM KEXING PHARMA

A PEGylated Fe based on functional peptide R9 modification 3+ /pei gene carrier and its preparation method and application

The invention relates to a PEGylated Fe3+ / PEI genetic vector based on functional peptide R9 modification and a preparation method and application of the PEGylated Fe3+ / PEI genetic vector. The genetic vector contains polyethylene glycol modified Fe3+ / polyethyleneimine and a conjugate formed by functional peptides R9. The PEGylated Fe3+ / PEI genetic vector based on functional peptide R9 modification has the advantages that metal ions Fe3 react with PEI at first, PEG modification is carried out to form PEGylated Fe3+ / PEI, then the functional peptide R9 which has ability of improving nuclear delivery and is targeted at alpha v beta 3 is synthesized, R9 is coupled with a PEG-Fe3+ / PEI by a crosslinking technology, and therefore, a novel virogene-free vector system PEG-Fe3 + / PEI is established. On the basis of reducing PEI cytotoxicity, in-vivo targeting property and nuclear delivery ability are improved, then the transfection efficiency of the vector in vivo is improved, and an effective way is searched for final application of gene therapy on clinical treatment.
Owner:SHANGHAI OCEAN UNIV
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