35 results about "Αvβ3 integrin" patented technology

Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin αvβ3 receptor-antagonist activity and substantially reduced integrin αllbβ3 and/or α5β1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin αllbβ3 and/or α5β1 as compared to a wild-type disintegrin. The variant is useful for treatment and/or prevention of αvβ3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.

The present invention provides αVβ3 integrin cysteine loop domain agonists and antagonists (including peptide agonists and antagonists and analogs thereof), along with methods of using the same.

The invention relates to a preparation method of RGD-modified subminiature superparamagnetic iron oxide nanoparticles. The preparation method comprises the following steps of preparing PEI-coated subminiature superparamagnetic iron oxide nanoparticles by a mild reduction method, modifying surfaces of USPIO/PEI.NH2 nanoparticles by fluorescein isothiocyanate (FI) and a RGD compound (COOH-PEG-RGD) subjected to pegylation, and carrying out acetylation treatment on the surfaces of the nanoparticles. The preparation method has simple processes and mild reaction conditions and can be operated easily. The RGD-modified subminiature superparamagnetic iron oxide nanoparticles have small sizes, a high relaxation rate, good colloid stability and biocompatibility, and high alpha<v>beta<3> integrin high-expression tumor cell targeting, and have a latent application value in the field of in-vivo tumor targeting MR imaging diagnosis.

The invention discloses a USPIO-PLA-RGD compound, a preparation method and application thereof. The USPIO-PLA-RGD compound uses USPIO as a core, is coated by PLA outside, and is labeled as PLA-USPIO; and the USPIO-PLA-GRD compound obtained through covalently coupling carboxyl of a functional group exposed on the surface of PLA and amidogen of RGD peptide has a hydrated grain diameter of between 90 and 105 nm. The USPIO-PLA-RGD compound can be applied as magnetic resonance tumor angiogenesis targeting contrast agent. The invention realizes targeting developing by the characteristics of high affinity of an alpha v beta3 integrin receptor and ligand RGD peptide thereof, and the combination has the characteristics of high specificity, selectivity, saturation and affinity, clear biological effect and the like. The concentration of a medicament in a partial focus can be increased, and toxic and side effects can be reduced by using the ligand RGD peptide as a vector of USPIO through the mediation effect of the receptor, so that the aim of development of a targeting tumor angiogenesis living body is realized.

The invention generally relates to fusion proteins comprising a rhodostomin variant having an RGD motif variant ⁴⁸ARLDDL⁵³, wherein the rhodostomin variant is conjugated with a variant of Human Serum Albumin (HSA). The invention also relates to the use of these fusion proteins for treatment and prevention of αvβ3 integrin-associated diseases.

The invention relates to a preparation method of SPECT/CT (Single Photon Emission Computed Tomography/Computed Tomography) dual-mode imaging contrast agent based on a second-generation polyamide-amine dendritic polymer. The method comprises the following steps: by taking the second-generation polyamide-amine dendritic polymer as a template material, sequentially modifying a radionuclide 99mTc chelating agent NOTA and a pegylated RGD (Arginine-Glycin-Aspartate) molecule on the surface; coating gold nanoparticles through an in-situ reduction synthesis method; and finally, labeling the radionuclide 99mTc, thereby obtaining the product. The SPECT/CT contrast agent prepared by the method disclosed by the invention has excellent colloidal stability, excellent biocompatibility, long blood circulation time and excellent in-vitro/vitro SPECT/CT imaging effect, has a specific targeting effect on C6 cells of an alphavbeta3 integrin receptor on the cell membrane surface and provides a good thought for developing a novel dual-mode nano contrast agent.

The present invention provides αVβ3 integrin cysteine loop domain agonists and antagonists (including peptide agonists and antagonists and analogs thereof), along with methods of using the same.

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.

The invention discloses the CNGRCVSGCAGRC-nrhTNF fusion protein and their preparation method, comprising the following steps: removing the 1-7 amino acid at the end of tumor necrosis factor amidogen, transforming the 8-10 amino acid into the Arg-Lys-Arg, transforming the 157 amino acid at the end of carboxy group into the phenylalanine, constructing the highly effective and low toxicity nrhTNF, selecting the CRGDC which is screened from bacteriophage exhibit library and highly effectively integrated with ª‡vª‰3 integrin specificity, fusing it into the end of amido of nrhTNF by utilizing the gene engineering method. The CRGDC-nrhTNF fusion protein can concentrate at the tumour newborn vessel, improve the therapeutic specificity of tumor necrosis factor, decrease the whole body dosage, reduce the secondary reaction and improve the quality efficiency ratio.

The present invention relates to the use of a peptide that interacts with the αvβ3 integrin of endothelial cells. More particularly, the invention relates to a method for inhibiting endothelial cell adhesion, endothelial cell migration and/or angiogenesis, using a peptide consisting of at least 18 amino acids, comprising tyrosine-histidine (TY) or asparagines-histidine (NH), and at least three hydrophobic amino acids with bulky side chains; or equivalents thereof. Furthermore, the invention provides a method for treating or preventing angiogenesis-related diseases, using the peptide.