168 results about "Integrin" patented technology

Provided is a compound for double targeting of a fibroblast activation protein and an integrin subtype, comprising: (i) a chelating ligand moiety (CL); (ii) a first targeting moiety (BT); and (iii) a second targeting moiety (CY), wherein (i), (ii), and (iii) are fixed, combined, or connected by means of any L; BT is a fibroblast activation protein (FAP)-specific binding ligand structure; CY is an integrin subunit αvβ3 or αvβ6-specific binding ligand structure; L is selected from one or a combination of L1, L2, L3, L4, L5, L6, and L7; L1, L2, L3, L4, L5, L6, and L7 are each independently a key, a monovalent joint, a divalent joint, or a trivalent joint. Also provided are a preparation method for the compound and use thereof.

The invention discloses a preparation method and application of a novel hybrid extracellular vesicle. According to the invention, vesicles derived from endothelial cells and neutrophil cells are combined with deferoxamine, and a biological mixed nano vesicle platform (DFO (HEVS)) is developed to solve the problem of diabetes wound healing. According to the dual-targeting system, DFO is accurately delivered to a wound part by utilizing CXCR4 mediated endothelial cell homing and beta2 integrin dependent inflammation tropism, DFO (at) HEVs activates and recovers vascular regeneration through HIF-1alpha / VEGF, ferroptosis is inhibited through Nrf2 / GPX4 signal transduction, macrophages are reprogrammed into a repair promoting M2 phenotype, and oxidative stress-inflammation-ferroptosis circulation is effectively broken.

The present disclosure relates, in part, to radiopharmaceuticals that target integrin, such αvβ6, their pharmaceutical compositions, and their use in imaging, diagnosing, and treatment of conditions associated with overexpression of integrins as well as to methods of making these compositions, including high purity 61Cu[Cu] radiopharmaceuticals that target integrins.

The present invention relates to use of a JWA polypeptide in the preparation of a drug for resisting androgenetic alopecia. An amino acid sequence of the polypeptide is shown as I or II: I: FPGSDRF-Z; II: X-FPGSDRF-Z, wherein an amino acid S is subjected to phosphorylation modification, and X and Z are an amino acid or an amino acid sequence, respectively. The described JWA polypeptide can directly target integrin molecules onto hair follicle cells and enter the cells to play a role in regulating and controlling hair follicle proliferation, promoting hair growth and the like; the telogen phase of the hair follicles is significantly shortened, and the anagen phase of the hair follicles is prolonged; the hair shaft and follicle volume is increased; and the expression level of the target cell integrin molecule αvβ1 can be improved, and the hair follicle stem cell signal channel MEK / ERK / E2F1 / SP1 / Wnt10a / 10b / β-catenin can be accurately activated.

Provided are an immune checkpoint inhibitor containing as an active ingredient a substance that inhibits the interaction of integrin and immunosuppressive receptor (referred to hereinafter as LILR) B3 and a therapeutic agent for immune checkpoint-related disease containing as an active ingredient a substance that inhibits the interaction of integrin and LILRB3.

An iRGD-LAMP2B-EGFP fusion protein mediated exosome surface engineering strategy is adopted, through specific recognition of iRGD peptide and integrin alpha v beta 3, corneal neovascularization core lesion cells are actively targeted, the limitation of off-target toxicity of a traditional delivery system is broken through, and a'accurate focus recognition-efficient homing 'targeted delivery normal form is established. Meanwhile, the screened circular RNA with anti-inflammatory and anti-angiogenesis dual activities is used as a core effector molecule, and in combination with an in-situ loading technology of the circular RNA molecule in an exosome parent cell, stable entrapment and targeted release of a nucleic acid drug in an exosome cavity are realized, and the problems that the nucleic acid drug is easy to degrade and poor in targeting property are solved; and dual guarantee of function specificity and delivery stability is formed. And a synergistic treatment system of a targeting exosome carrier and bifunctional circular RNA is further constructed, active molecules are accurately delivered to focus cells, and an inflammation microenvironment and an angiogenesis pathway are synchronously regulated and controlled.

The application provides a multifunctional nano particle for targeting abdominal aortic aneurysm and a preparation method and application thereof, and belongs to the field of nanobiomedicine, wherein polyphenol oxidation self-polymer nanoparticles are used as carriers, doxycycline is loaded, and a targeting ligand cRGD is modified on the surface of the nano carrier; the neovasculature in the media and adventitia of AAA sites helps accumulation of the nanoparticles in the abdominal aortic aneurysm, and the integrin αν3 beta receptor highly expressed on the surface of the diseased cell membrane can recognize the cRGD with high affinity, and then mediate the targeted endocytosis of the nanoparticles; after intravenous injection, the nanoparticles can be effectively enriched in the lesion site and achieve long-term retention, and can release DC in response to the high ROS level in the tumor microenvironment; the drug is rapidly released to take effect, and the non-specific toxic side effects are reduced; the free radical scavenging capacity of the nanoparticles can be synergized with the DC activity to treat AAA through multiple mechanisms such as anti-inflammatory, antioxidant, macrophage repolarization promotion, anti-apoptosis and calcification inhibition, and MMPs inhibition.

Disclosed in the present invention are an immunoglobulin κ-type light chain (Vκ4-1-IgLC) polypeptide having a unique Vκ4-1 and the use thereof. The amino acid sequence of the Vκ4-1-IgLC polypeptide is as shown in SEQ ID NO. 1, and the polypeptide can be used as a target or a marker for preparing a drug for diagnosing and / or treating tumors or inflammatory diseases, and can also be used for preparing an Integrin-FAK signal pathway inhibitor. An antibody prepared by using the polypeptide as an antigen can effectively inhibit the development of tumors, and provides a new thought for clinical diagnosis and treatment of tumors.

The application belongs to the field of biomedical application, and more particularly relates to a cell fluorescence probe anchoring cell integrin, and a preparation method and application thereof. The cell fluorescence probe comprises a polypeptide complex, a fluorescent molecule and a cyclodextrin unit, the polypeptide complex comprises a cysteine-containing peptide, a peptide containing a bonding group and a targeting peptide which are connected in any order, the cyclodextrin unit contains a carbon-carbon double bond functional group, and is combined with the cysteine-containing peptide through a click reaction to form the polypeptide complex, the polypeptide complex is covalently connected to the fluorescent molecule through the bonding group, and the fluorescent molecule is an aggregation-induced emission compound. The double bond functional group of the modified cyclodextrin is bonded to the sulfhydryl group of the terminal cysteine of the polypeptide through a click reaction, and the sulfhydryl group of the terminal cysteine of the polypeptide is bonded to the double bond functional group of the modified cyclodextrin through a click reaction, so that the cyclodextrin is improved to protect the fluorescent molecule and prolong the fluorescent time effectiveness of the fluorescent imaging reagent.

To provide cross-species anti-latent TGF-β 1 antibodies which inhibit a protease mediated activation of latent TGF-β 1 without inhibiting integrin mediated activation of latent TGF-β 1.SOLUTION: To obtain the anti-latent TGF-β 1 antibodies of the present invention, anti-latent TGF-β 1 antibodies which inhibit a protease mediated activation of latent TGF-β 1 without inhibiting integrin mediated activation of latent TGF-β 1 are screened, and then humanized, and further optimized. The invention also provides combination therapies comprising an anti-latent TGF-β 1 antibody and one or more immune checkpoint inhibitors, preferably PD-1 axis binding antagonists.SELECTED DRAWING: None

It is an object of the present invention to provide anti-latent TGF-beta 1 antibodies and methods of using such antibodies. The present invention provides an anti-latent TGF-[beta] 1 antibody which inhibits protease-mediated activation of latent TGF-[beta] 1 without inhibiting integrin-mediated activation of latent TGF-[beta] 1 or which partially inhibits activation of integrin-mediated latent TGF-[beta] 1, or the antibody inhibits protease-mediated latent TGF-beta 1 activation but has a small effect on inhibition of integrin-mediated latent TGF-beta 1 activation. The present invention also provides optimized anti-latent TGF-beta 1 antibodies wherein the pH dependent binding properties are improved. The anti-latent TGF-beta 1 antibody can be used to treat fibrosis or cancer. For example, the anti-latent TGF-beta1 antibodies may be used to treat renal fibrosis, hepatic fibrosis, and pulmonary fibrosis.

The present disclosure relates, in part, to radiopharmaceuticals that target integrin, such αvβ6, their pharmaceutical compositions, and their use in imaging, diagnosing, and treatment of conditions associated with overexpression of integrins as well as to methods of making these compositions, including high purity 61Cu[Cu] radiopharmaceuticals that target integrins.

This invention provides a pharmaceutical composition containing a novel compound useful for inhibiting human α4β7 integrin. [Solution] For example, a pharmaceutical composition containing a compound of the following formula is provided. JPEG2026136229000099.jpg64148

Disclosed are a specific marker combination of mesenchymal stem cell-derived small extracellular vesicles and the use thereof. The characteristic marker combination comprises aminopeptidase N (CD13), integrin β-1 (CD29), membrane glycoprotein THY-1 (CD90), and markers CD9, CD63 and CD81. By using the characteristic marker combination of mesenchymal stem cell-derived small extracellular vesicles for nano-flow cytometry analysis at the single-vesicle level, mesenchymal stem cell-derived small extracellular vesicles can be identified. On the basis of the provided characteristic marker combination, specific modification and engineering on the basis of small extracellular vesicle membrane proteins can further be realized.

Disclosed are small molecule inhibitors of αvβ8 integrin, and methods of using them to treat a number of diseases and conditions.

The invention provides a phospholipid coated silver / manganese dioxide coprecipitation particle MRI contrast agent and a preparation method and application thereof. The prepared contrast agent has efficient MRI contrast performance, and compared with a traditional gadolinium-based contrast agent, the biological safety is higher, and the risk of heavy metal ion leakage is avoided; the contrast agent has the advantages that the contrast agent is high in targeting ability and accurate in targeting ability, phospholipid layer modified cRGD targeting molecules can specifically recognize high-expression integrin alpha v beta 3 on the surfaces of tumor cells, enrichment of the contrast agent in tumor tissues is realized, and imaging resolution and focus positioning accuracy are improved. The nano-silver / manganese dioxide composite material has good biocompatibility and multifunctional diagnosis and treatment integrated potential, creatively combines a silver / manganese dioxide coprecipitation core and a phospholipid wrapping structure, has good magnetic resonance imaging (MRI) contrast performance and biocompatibility, and shows remarkable application potential in the medical imaging fields of tumor targeted imaging, disease diagnosis and the like. And a new direction is provided for the development of MRI contrast agents.

Provided herein are variant α4β7 integrin antibodies and methods of use.

The invention provides a method for improving stem cell dryness of mesenchymal stem cells and a compound and a composition thereof, the method for improving the stem cell dryness of the mesenchymal stem cells comprises the following steps: treating the mesenchymal stem cells with an active substance, activating an integrin-FAK-Src pathway, enhancing the phosphorylation level of FAK and Src proteins, and further activating a downstream PI3K / Akt pathway, so that the stem cell dryness of the mesenchymal stem cells is improved, and the stem cell dryness of the mesenchymal stem cells is improved. The cell dryness of the mesenchymal stem cells is improved. The research confirms that the COL21 has a promoting effect on MSC proliferation, and meanwhile, the COL21 is confirmed to promote expression of four stemness markers including Oct-4, Klf4, Nanog and Sox2 in MSC, so that the stemness of MSC stem cells is improved.

The application relates to a recombinant type I collagen and application thereof, which utilizes the characteristics of Pichia pastoris capable of secreting and expressing recombinant proteins, secretes the recombinant type I collagen on the culture medium supernatant, and reduces the difficulty of protein purification. In addition, the integrin site RGD is inserted into the collagen to form a recombinant type I collagen with high stability and high expression. According to the relative proliferation of cells and the relative adhesion experiment of cells, it can be seen that the recombinant type I collagen has the effects of promoting the proliferation of skin fibroblasts, improving the skin, promoting wound healing, promoting the adhesion of fibroblasts in the skin layer and the like. Therefore, the recombinant type I collagen has great potential applications in the fields of skin care and beauty, medical treatment and the like.

This disclosure relates to novel chemical compounds and methods useful for inhibiting αvβ8 integrin.

Disclosed herein are methods and compositions for disrupting the interaction between galectin-3 and insulin receptor or integrins. Also disclosed herein are methods and compositions for treating a disease or disorder in a subject, such as diabetes, inflammatory bowel syndrome, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.

The application belongs to the field of biological medicine, and relates to an anti-human integrin CD103 nanobody and application. The anti-human integrin CD103 nanobody comprises three complementarity determining regions CDR1, CDR2 and CDR3; wherein the amino acid sequence of CDR1 is a sequence or a high homology sequence shown in one of SEQ ID NO: 1 to SEQ ID NO: 6, the amino acid sequence of CDR2 is a sequence or a high homology sequence shown in one of SEQ ID NO: 7 to SEQ ID NO: 12, and the amino acid sequence of CDR3 is a sequence or a high homology sequence shown in one of SEQ ID NO: 13 to SEQ ID NO: 18. 18 The F-CYNB nanobody probe can be applied to targeted imaging of cardiac myocardial fibrosis.

Provided are a compound capable of specifically binding to integrin αvβ6, a conjugate and pharmaceutical composition containing a compound-based ligand group, and a method for preparing the compound, conjugate and pharmaceutical composition and the use thereof. The compound has a structure as shown in formula (1). The provided conjugate can specifically deliver a functional group to cells and / or tissues expressing integrin αvβ6, thereby achieving the objective of diagnosing or treating diseases.

The present invention relates to the field of nuclear medicine technology, and discloses a targeted compound bimolecular probe, comprising a component A and a component B respectively labeled with radioactive metal nuclides; component A is a molecular probe targeting fibroblast activation protein (FAP), and the molecular probe targeting fibroblast activation protein (FAP) includes a trans-cyclooctene group (TCO); component B is a molecular probe targeting integrin α v β6 molecular probe, targeting integrin α v The β6 molecular probe includes a tetrazine group (Tz); wherein the radioactivity ratio of component A to component B is (1-2): (2-1). The present invention has the following technical effects: the TCO in the FAP-targeting molecular probe and the integrin α v The Tz in the β6 molecular probe can undergo a bioorthogonal reaction, achieving a tertiary amplification effect, increasing tumor uptake, prolonging the retention time of the targeted compound bimolecular probe, improving the target / non-target ratio, and enhancing nuclear medicine diagnostic and therapeutic effects. The present invention also discloses a method for preparing and using the targeted compound bimolecular probe.

The invention discloses application of irisin in treatment of acute lung injury / acute respiratory distress syndrome. The research finds that the plasma irisin level is obviously reduced in ARDS patients, and the survival prognosis of the patients with the lower irisin level is poorer. Neutrophil as the most inflammatory cells is a cause for promoting lung tissue injury. Further analysis finds that the level of irisin is in negative correlation with the number of circulating neutrophils, and irisin incubation can significantly reduce in-vitro survival promoting (apoptosis delay) phenotypes of neutrophils in ARDS mouse alveolar lavage fluid. Iris receptor integrin alphaVbeta5 inhibitor treatment can promote neutrophil infiltration and aggravate an ARDS process. The invention provides a novel therapeutic drug and strategy for the treatment of acute lung injury / acute respiratory distress syndrome.

Methods and compositions for the prevention and treatment of acute radiation syndromes and radiation illnesses from exposure to toxic radiation including radiation therapy treatments, the methods and compositions comprise Indole derivatives and their administration to a living being, where Indole derivative compositions include a racemic mixture of R-Indole derivative and S-Indole derivative enantiomers, or isolated R-Indole derivative enantiomers, or S-Indole derivative enantiomers. The compositions of the invention are suitable for treating and / or preventing radiation injury, and embodiments may comprise functional analogs, derivatives, racemic mixtures and / or chiral forms, S and / or R thereof. Indole derivative compositions include compositions having the formulae: (S)-1-(3-Indolyl)-2-(methylamino) ethanol; (S)-α-[(Methylamino)methyl]-1H- Indole-3-methanol, indolo[a]pyrrolo[3,4-c] carbazole integrin composition. The method involves administering an effective amount of an indole composition in a pharmaceutically acceptable form, to provide a fast-acting medical countermeasure with radioprotective and radiomitigative functionalities for treatment or prevention of radiation illnesses.

The present invention relates to the use of an antibody or an immunologically active fragment thereof, which specifically binds to integrin β2, as an immuno-oncology agent. The chimeric and humanized antibodies of the present invention specifically bind to integrin β2, which is a tumor-specific antigen and is expressed on the cell membrane of M2 tumor-associated macrophages, and thus can be used as an antibody therapeutic agent for cancer treatment using a cancer cell death mechanism by immune cell activation, an antibody therapeutic agent for cancer treatment, or a cell therapeutic agent for cancer treatment, and can also be used for cancer diagnosis.