90 results about "Receptor targeting" patented technology

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided. Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer, methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer.

The present invention generally relates to yeast cell wall microparticles loaded with nanoparticles for receptor-targeted nanoparticle delivery. In particular, the present invention relates to trapping nanoparticles either on the surface or inside a yeast glucan particles, for example, yeast glucal particles. The present invention further relates to methods of making the yeast cell wall particles loaded with nanoparticles. The present invention also relates to methods of using the yeast cell wall particles loaded with nanoparticles for receptor-targeted delivery of the nanoparticles, e.g., drug containing nanoparticles.

New and improved compounds for use in radiodiagnostic imaging or radiotherapy having the formula M-N-O-P-G, wherein M is the metal chelator (in the form complexed with a metal radionuclide or not), N-O-P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and / or providing radiotherapy to a patient using the compounds of the invention are also provided. A method for preparing a diagnostic imaging agent from the compound is further provided. A method for preparing a radiotherapeutic agent is further provided.

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N-O-P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

The invention provides, in a general sense, a new labeling strategy employing compounds that are are N2S2 chelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, a COX-2 inhibitor, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is an optical label or a metal chelator (in the form complexed with a metal radionuclide or not), N-O-P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

The invention belongs to the technical field of high-molecular medicine, and particularly relates to an antitumor medicine conjugate with folic acid receptor-mediated and photoresponsive functions and a preparation method thereof. The preparation method comprises the following steps: firstly, performing amidation reaction on folic acid and amino polyethyleneglycol; then performing amidation reaction on a product obtained in the former step and 7-ethyloic-4-hydroxymethyl coumarin to obtain a polyethyleneglycol flexible chain with a folic acid receptor targeting function and a photoresponse group; finally enabling the polyethyleneglycol flexible chain to be coupled with an antitumor medicine containing amino with an ester activation method to obtain the antitumor medicine conjugate with the folic acid receptor-mediated and photoresponsive functions. The conjugate prepared by the invention can target a tumor cell through a folic acid receptor-mediated function, and enters the cell via the endocytosis to accelerate the accumulation speed of the medicine in the tumor cell; when being irradiated by ultraviolet light with a specific wavelength or near-infrared light, the conjugate is photolyzed to release original medicine, and the medicine quickly reaches the effective concentration, so that controllable 'time / space' treatment is realized; in addition, the method provides a simple and effective manner for preparing target-controllable photoresponsive high-molecular medicine conjugates.

CD44, the receptor for hyaluronic acid, has complex functions in cellular physiology, cell migration and tumour metastasis. The inventors have previously found that human CD44 receptor overexpression in mouse fibrosarcoma cells inhibits subcutaneous tumour growth in mice [Kogerman et al., Oncogene 1997; 15:1407-16; Kogerman et al., Clin Exp Metastasis 1998; 16:83-93]. Here it is demonstrated that a tumour growth inhibitory effect of CD44 is caused by block of angiogenesis. Furthermore, the inventors have found that soluble recombinant CD44 hyaluronic acid binding domain (CD44HABD) inhibits angiogenesis in vivo in cLick and mouse and thereby inhibits human tumour growth of various origins. The anti-angiogenic effect of CD44-HABD is independent of hyaluronic acid (HA) binding, since non-HA-binding mutants of CD44HABD still maintain anti-angiogenic properties. The invention discloses soluble CD44 recombinant proteins as a novel class of angiogenesis inhibitors based on targeting of vascular cell surface receptor. A method of block of angiogenesis and treatment of human tumours using recombinant CD44 proteins as well as their analogues is disclosed. As a further embodiment of the invention, methods for screening for new drug targets using CD44 recombinant proteins and their analogues is presented.

The present invention provides a single-chain antibody targeting CD317, the single-chain antibody targeting CD317 comprises an amino acid sequence shown in SEQ ID NO: 1, and the single-chain antibodytargeting CD317 is a humanized single-chain antibody. The present invention also provides a chimeric antigen receptor T cell comprising the single-chain antibody targeting CD317, wherein the chimericantigen receptor targeting CD317 can specifically target CD317, the expansion of T cells in patients is promoted, the tumor cells can be efficiently and specifically killed, and damage is hardly generated on the normal cells. In addition, the chimeric antigen receptor T cell targeting CD317 produced by humanized single-chain antibody can keep the ability of self-renewal and tumour lethality. The invention also provides a preparation method and an application of the chimeric antigen receptor T cell targeting CD317.

Disclosed herein are drug delivery molecules that comprise a ligand that targets a cell surface molecule; a membrane penetration domain; and a payload binding domain; and pharmaceutical compositions comprising the same. Also disclosed are methods of treating cancer, inhibiting the progression of cancer, preventing cancer metastasis, and delivering a therapeutic compound to the brain in a subject in need thereof, the methods comprising identifying a subject in need thereof; providing a composition comprising the drug delivery molecule as disclosed herein; and administering an effective amount of the composition to the subject.

The invention relates to the technical field of radiopharmaceutical chemistry, and particularly relates to a programmed cell death protein receptor-1 targeted molecular probe and a preparation methodand application thereof. According to the programmed cell death protein receptor-1 targeted molecular probe, the small-molecule probe has medium affinity to target PD-L1, can be selectively taken in aPD-L1 positive tumor site, can well distinguish negative and positive tumors, has response to a PD-L1 high-expression tumor site, and can be used for developing a PD-L1 small-molecule PET developer.

The invention discloses a preparation method of a polysaccharide grafted folic acid copolymer and a nanoparticle thereof. The method includes: using anhydrous dimethylsulfoxide to dissolve folic acid,then adding 1-hydroxybenzotriazole and N-N'-dicyclohexylcarbodiimide for carboxyl activating reaction, mixing a carboxyl activated folic acid solution with a dimethylsulfoxide solution of polysaccharide, carrying out esterification reaction for 24-72h under nitrogen protection and at a temperature of 40-80DEG C, and performing purification to obtain a copolymer mixture; conducting freezing dryingto obtain the polysaccharide grafted folic acid copolymer lyophilized powder, i.e. the polysaccharide grafted folic acid copolymer. The polysaccharide grafted folic acid copolymer can be applied as acarrier in preparation of a nanoparticle preparation with folic acid receptor targeting function, and the nanoparticle preparation can be used for tumor targeted drug delivery.

The invention provides a pH (potential of hydrogen) controlled-release targeted medicine nanometer delivery carrier, a method for preparing the same and application of the pH controlled-release targeted medicine nanometer delivery carrier. Fe3O4 is used as a core for the pH controlled-release targeted medicine nanometer delivery carrier, mSiO2 is used as a shell for the pH controlled-release targeted medicine nanometer delivery carrier, -NH2 is modified on the surface of Fe3O4@mSiO2, a targeted receptor folic acid (FA) and immobilized daunomycin (DNM) are linked up on the surface of the Fe3O4@mSiO2 by means of amide reaction, blocking is ultimately carried out by the aid of CaCO3, pH value response controlled release can be implemented, 'zero-release' effects can be realized in blood circulation, and accordingly toxic and side effects of medicines on human bodies can be reduced. The pH controlled-release targeted medicine nanometer delivery carrier, the method and the application havethe advantages that the pH controlled-release targeted medicine nanometer delivery carrier is combined with the mSiO2 which is excellent in biocompatibility and high in specific surface area and has surfaces easy to modify and wrap Fe3O4 nanometer micro-spheres, modification is carried out by the aid of amine (the -NH2), then the targeted receptor folic acid is grafted, and accordingly the anticancer performance of the targeted medicines can be improved by the aid of multi-targeting generated by magnetic targeting and receptor targeting and is obviously superior to single targeting; the performance of targeted medicine controlled-release systems can be improved by the aid of the physiological pH stability of calcium carbonate.

The invention relates to a GPC3 (glypican-3) receptor targeted polypeptide radioactive diagnosis or therapeutic drug. The GPC3 receptor targeted polypeptide radioactive diagnosis or therapeutic drug includes: polypeptide with an amino acid sequence shown as SEQ ID NO:1; and a radionuclide or positron-emitting nuclide marker coupled to the polypeptide. The invention adopts the radionuclide labeled polypeptide as a hepatocellular carcinoma specific targeting molecular probe to show the expression situation of the GPC3 receptor in hepatocellular carcinoma tumor tissue on a living body level, and improves the effective rate of hepatocellular carcinoma oncotherapy. For lung cancer, melanoma and other GPC3 receptor-positive tumors, the GPC3 receptor targeted polypeptide can also be used for preparation of drugs for diagnosis or treatment of lung cancer and melanoma.

The invention relates to a chemical gene drug co-loaded targeted nano drug delivery system and a preparation method thereof, and in particular relates to a tumor microenvironment hyaluronidase triggered allosteric-charge turnover type chemical / gene drug co-loaded targeted nano drug delivery system and a preparation method thereof. The nano drug delivery system is characterized by being co-assembled by co-loading chemical and gene drugs through a polystyrene-polydimethylbiguanide (PMet) cationic polymer by adopting hyaluronic acid-sulfydryl (HA-SH) with CD44 receptor targeting and tumor microenvironment hyaluronidase (HAase) sensitivity through electrostatic bonding and mercaptan chemical crosslinking. According to the invention, low-toxicity, targeted and efficient treatment of tumors be realized, and a novel multifunctional nano-carrier for treating tumors based on a chemical combined gene drug and a preparation application strategy are provided for anti-tumor research.

The invention belongs to the technical field of biological medicines and specifically relates to a preparation method for a self-assembly nanoparticle with a targeting function and an application thereof. According to the invention, a solvent exchange method is adopted for preparing a self-assembly nano-composite and establishing a UA and EGCG self-assembly nanometer drug-carrying system with pH response and EpCAM receptor targeting ability, so that a nanometer drug delivery system according to the invention creatively utilizes a self-assembly technology to simultaneously prepare UA, EGCG andAptamer; the preparation process is simple and easy; a new research direction is supplied for oncotherapy.

The present invention concerns the use of methods for evaluating β-adrenergic receptor targeting agent treatment for a patient, particularly one with a heart condition. In general, the disclosed methods entail determining the presence or absence of one or more polymorphisms in an endothelin gene system member. Based on the results of this determination, a β-adrenergic receptor targeting agent may be prescribed, administered or a treatment regimen altered, including the administration of a β-blocker. Accordingly, methods of treatment are also described.

The invention discloses a preparation method of microgel based on shear force sensitivity and CD44 receptor targeting, and belongs to the technical field of nano materials. The preparation method comprises the following steps: synthesizing an amphiphilic polymer PAA-b-PEHA, synthesizing an amphiphilic graft copolymer P(AA-g-HEMA)-b-PEHA, synthesizing a hyaluronic acid hydrogel precursor HAGMA, andsynthesizing a double-response microgel HACBC with shear force response and CD44 receptor targeting. According to the prepared nano microgel, mechanical force sensitivity and CD44 receptor targetingare combined, so that an affected part can be more accurately targeted and a therapeutic drug is released at the affected part. In addition, the used raw materials are all degradable materials with good biocompatibility and low toxic and side effects, and the side effects on human bodies are extremely low.

The present invention discloses a Plectin-1 receptor targeting novel cationic KTLLPTPK-lipopeptide. The present invention further discloses a liposomal formulation comprising the cationic KTLLPTPK-lipopeptide, at least two co-lipids, therapeutic agents and a pharmaceutically acceptable carrier. The present invention also provides a method for regressing established pancreatic tumors comprising administering therapeutically effective amount of the liposomal formulation with the therapeutic agents in combination with targeted genetic immunization (DNA vaccination) i.e. by immunizing mice with electrostatic complexes (direct in-vivo DC-targeting cationic liposomes) of DNA vaccines encoding mesothelin (p-CMV-MSLN).

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

The invention relates to a double-receptor targeting drug delivery system realizing the synergistic effect of phototherapy and chemotherapy, as well as preparation and applications of the double-receptor targeting drug delivery system. The system is a compound containing hyaluronic acid, polylactic acid, polypeptide, and chlorambucil / chlorin e6, wherein the molecular weight of polylactic acid is 8000Da, specifically, the compound comprises the following components in parts by weight: 100-2000 parts of hyaluronic acid, 1500-10000 parts of polylactic acid, 21-450 parts of N,N'-dicyclohexylcarbodiimide, 12-240 parts of N-hydroxy succinimide, 1-30 parts of polypeptide, 20-400 parts of 1-(3-(Dimethylaminopropyl)-3-ethylcarbodiimide, 100-1000 parts of chlorambucil, and 50-600 parts of chlorin e6. The double-receptor targeting drug delivery system has the beneficial effects that (1) the synergistic effect of phototherapy and chemotherapy is realized; (2) the multiple targeting properties are realized; (3) the good blood stability is realized; (4) the system has small toxicity and high safety.

The invention discloses a preparation method of a CT imaging molecular probe of folate receptor targeted tumors, which comprises the following steps: dissolving folic acid which is used as a wrapping agent in a solution which contains gold ions and is used for preparing nanogold, adjusting the pH to 7.0-7.5 to obtain a mixed solution, wherein the molar ratio of folic acid to gold ions is 1:2-6; adding a reducing agent into the mixed solution, rapidly stirring and reacting for at least 1 hour, naturally cooling after the reaction, performing dialysis to remove unreacted parts so as to obtain the nanogold coated by folic acid. The nanogold coated by folic acid FA-GNP prepared in the invention has high attenuation capability for X ray, and can be used as a CT imaging contrast agent; the FA-GNP can provide CT images with high contrast for tumors.

The invention relates to the field of medicines, in particular to a PEDF gene composition targeted by a tumor cell folate receptor as well as a preparation method of the PEDF gene composition and a use of the PEDF gene composition. The invention constructs a folate modified PEDF gene composition which can selectively transmit coded PEDF plasmids to the tumor cell by the folate receptor highly expressed by a tumor part, so that the tumor cell is induced to die, multiplication, invasion and transfer of the tumor cell are inhibited, and therefore, the anti-tumor effect is brought into play, and a better anti-tumor effect is achieved.

Disclosed herein are drug delivery molecules that comprise a ligand that targets a cell surface molecule; a membrane penetration domain; and a payload binding domain; and pharmaceutical compositions comprising the same. Also disclosed are methods of treating cancer, inhibiting the progression of cancer, preventing cancer metastasis, and delivering a therapeutic compound to the brain in a subject in need thereof, the methods comprising identifying a subject in need thereof; providing a composition comprising the drug delivery molecule as disclosed herein; and administering an effective amount of the composition to the subject.