95 results about "Molecular targeting" patented technology

The invention relates to the field of molecular targeted therapy, and discloses an application of an SLC16A5 (MCT6) small-molecule inhibitor MCT6-Ai7-2 in preparation of a medicine for treating acute myeloid leukemia (AML). The inhibitor takes an SLC16A5 protein structure predicted by Alphafold as a target spot, and is obtained through compound database screening, molecular docking and druggability optimization. An in-vitro experiment proves that MCT6-Ai7-2 can remarkably inhibit proliferation of AML cell lines such as U937 and MOLM-13, induce cell apoptosis and retard a cell cycle, has an inhibiting effect on a primary AML patient specimen and is relatively low in toxicity to normal cells; in-vivo experiments show that the compound is effective and has good safety in AML model mice. In addition, the MCT6-Ai7-2 and the vinca can be combined to synergistically enhance the inhibition effect on vinca drug-resistant cells, and by reducing the expression of anti-apoptotic protein MCL-1, the activation of pro-apoptotic factors BIM and tBID is promoted to play a role. The invention provides a novel targeting drug and strategy for treatment of AML (especially drug-resistant or recurrent patients).

Disclosed are compositions and methods useful for targeting and internalizing molecules into cells of interest and for penetration by molecules of tissues of interest. The compositions and methods are based on peptide sequences that are selectively internalized by a cell, penetrate tissue, or both. The disclosed internalization and tissue penetration is useful for delivering therapeutic and detectable agents to cells and tissues of interest.

The invention provides an application of a super enhancer inhibitor JQ-1 in preparation of peripheral artery disease related drugs, relates to the technical field of biomedicine, and discloses a core effect of the super enhancer inhibitor JQ-1 in peripheral artery disease ischemia repair. The traditional Chinese medicine composition can significantly accelerate blood flow recovery of ischemic limbs, up-regulate mRNA and protein expression of a vascular marker CD31 in gastrocnemius muscle tissues, effectively increase vascular density and promote angiogenesis. Aiming at the defects of the existing treatment means in the aspect of ischemic tissue angiogenesis, the application provides a brand new molecular targeted treatment scheme for high-risk groups such as patients with diabetes-related peripheral artery diseases, and can significantly reduce the risk of lower limb amputation and the incidence rate of related cardiovascular adverse events such as coronary heart disease and stroke; the technical blank of specific targeted therapy of peripheral artery diseases is filled, a solid scientific basis and a key direction are provided for research and development of novel drugs, and the specific targeted therapy method has extremely high clinical application value and wide research and development prospects.

The invention relates to an SR-B1 targeted polypeptide compound and application thereof in preparation of antitumor drugs and immunotherapy sensitizers, and belongs to the technical field of biological drug manufacturing. In order to solve the problems that an existing PD-L1 inhibitor is single in action mechanism and immune system dysfunction is easily caused, the invention provides an SR-B1 targeted polypeptide compound which is composed of SR-B1 targeted polypeptide and Resiquimod. The SR-B1 targeting polypeptide comprises an SR-B1 targeting peptide fragment, a self-assembly peptide fragment and a hydrophobic molecule which are connected in sequence. The SR-B1 targeting polypeptide can recognize overexpressed SR-B1 in tumor cells, block cholesterol uptake, inhibit tumor progression and inhibit expression of PD-L1 at the same time. The polypeptide compound accurately delivers Resiquimod to a tumor site, anti-tumor immune response is activated, and sensitivity of tumor immunotherapy is greatly enhanced through combination of cholesterol metabolism regulation and immunotherapy.

Anti-CLEC12A polypeptides typically include an amino acid sequence having at least 90% amino acid similarity to SEQ ID NO: 14. In certain embodiments, the anti-CLEC12A polypeptides can be incorporated into an anti-CLEC12A biologic. In some of these embodiments, the anti-CLEC12A biologic can be a bispecific killer cell engager (BiKE), a trispecific killer cell engager (TriKE), a tetraspecific killer cell engager (TetraKE), a pentaspecific killer cell engager (PentaKE), a bispecific T cell engager (BiTE), a trispecific T cell engager (TriTE), a tetraspecific T cell engager (TetraTE), a pentaspecific T cell engager (PentaTE), a chimeric antigen receptor, a whole antibody, an antibody-drug conjugate (ADC) molecule, a targeted delivery construct, or a labeling construct.

The invention belongs to the technical field of biological medicines, and particularly relates to application of dirithromycin in preparation of a product for treating LINC00516 high-expression lung adenocarcinoma. The invention discloses the effect of the long-chain non-coding RNA LINC00516 in abnormal activation of the lung adenocarcinoma cell cycle for the first time. Researches show that LINC00516 is directly combined with CDK1, the kinase activity of CDK1 is remarkably enhanced, and the inhibitory phosphorylation level of CDK1 is reduced, so that lung adenocarcinoma cells are driven to quickly enter a G2 / M phase, and tumor cell proliferation is accelerated. The invention further innovatively proposes that dirithromycin is used as an intervention means, and by blocking the combination of LINC00516 and CDK1, the activity of CDK1 is effectively reduced, and the proliferation capacity of tumor cells is inhibited. In-vivo and in-vitro experiments prove that the dirithromycin can obviously inhibit the growth of lung adenocarcinoma cells with high expression of LINC00516, so that a brand-new molecular targeting treatment strategy is provided for clinic.

Provided herein is technology relating to vaccines and particularly, but not exclusively, to compositions, methods, and uses of a mixture of immunogenic vaccine molecules comprising components for targeting the dimeric vaccine molecules to antigen-presenting cells and components for eliciting an immunogenic response, wherein the components for eliciting an immunogenic response preferably comprise at least three variants of an immunogenic protein, such as variants of immunogenic proteins obtained from three or more different strains of a pathogenic organism.

The present application relates to the field of biological medicine and clinical diagnosis, and more particularly, the present application relates to a polypeptide having binding affinity to AXL protein and application thereof; the polypeptide has binding affinity to AXL protein, and therefore can be used for detecting AXL protein, so that the polypeptide has diagnostic or therapeutic use as a drug or molecular targeting reagent.

The invention discloses an application of miR-26a-5p in preparation of a product for preventing, repairing or treating cell aging. According to the invention, miR-26a-5p is applied to preparation of products for preventing and treating cell aging for the first time, a brand new molecular intervention strategy is provided for cell aging resistance, and the problem of lack of targeted molecular targeting schemes in the prior art is effectively overcome. The miR-26a-5p can be used for remarkably regulating and controlling the expression of cell cycle key factors CDK1, p21, Ki67 and Lamin B1, so that the proliferation state and the aging process of cells are accurately intervened.

Targeting immunosuppressive B cell populations using bispecific or multivalent targeting molecules presents a potential pathway for therapeutic interventions that effectively modulate antitumor immune responses and improve therapeutic outcomes. Therefore, we provide engineered antibody-based therapeutics that can effectively and selectively target immunosuppressive B cell populations for the treatment of cancer. [Solution] A multispecific antibody is provided comprising a CD19 antigen-binding component configured to bind to CD19 and a CD38 antigen-binding component configured to bind to CD38, wherein the CD19 antigen-binding component comprises an antibody or an antigen-binding fragment thereof, and the CD38 antigen-binding component comprises an antibody or an antigen-binding fragment thereof.

The present invention discloses circApbb1 molecules, siRNA targeting circApbb1 expression, adeno-associated virus vectors, preparation methods and applications, belonging to the field of molecular biology applications. A siRNA capable of knocking down circApbb1 expression was designed, and an adeno-associated virus vector HBAAV2 / 9‑cTNT‑mir30‑circApbb1Green of the siRNA was constructed. Detection showed that circApbb1 was significantly upregulated in the hearts of mice with atherosclerosis. The prepared siRNA adeno-associated virus vector can effectively reduce the expression of circApbb1 in the mouse heart, reduce the area of ​​atherosclerotic plaques, inhibit the progression of atherosclerosis and improve cardiac function, thus realizing the use of circApbb1 to treat atherosclerosis, providing an important supplement to the biological function of circApbb1, and providing a new technical means for the treatment of atherosclerosis.

The present invention addresses the problem of providing a novel combination therapy having a potent antitumor effect and few side effects. The present invention provides an antitumor agent containing zipalertinib or a salt thereof as an active ingredient and used so as to be administered to a cancer patient in combination with an additional antitumor agent, wherein the additional antitumor agent is at least one selected from the group consisting of molecular targeting agents, immune checkpoint inhibitors, and antibody-drug conjugates.

The invention relates to the field of medical imaging, in particular to an ultrasonic imaging method and system for observing target area aggregation of a targeted contrast agent in real time. The method comprises the following steps: injecting a contrast agent containing targeting molecules into a target area, and scanning and screening by adopting a specific ultrasonic pulse sequence to only obtain an echo signal of the contrast agent; further processing the ultrasonic echo signal by using a signal decomposition technique to extract a contrast agent signal specifically bound to the tissue target; and finally, monitoring the intensity change characteristics of the specific binding contrast agent signal in a slow time direction in real time by applying a quantitative algorithm, and taking the characteristics as a comparison basis to realize molecular targeting imaging. The ultrasonic imaging method provided by the invention overcomes the defect that the traditional ultrasonic molecular imaging method cannot realize real-time observation of target region aggregation of the targeted contrast agent, and can be more accurately applied to early diagnosis of various diseases such as cardiovascular diseases and tumors and real-time monitoring of molecular level.

Methods, techniques, and kits are provided herein for purifying cells using molecular targeting, at a cellular or subcellular level. The techniques comprise labeling a biological sample comprising cells with a probe capable of producing a protective barrier. The barrier is deposited onto the surface of the labeled cells or structures, to protect and retain the biological material under the barrier. A micropurification solution is applied to the biological sample, wherein the micropurification solution degrades, digests, or otherwise processes cells not covered by the barrier, allowing isolation of the target cells. In some aspects, a plurality of probes, each specific to a different target, may be used. The techniques may be performed without the need for complex instrumentation involving microscopy.

The present disclosure provides methods and related compositions that incorporate a molecularly targeted approach via the integrin subtype αvβ6 using Peptide Receptor Radionuclide Therapy (PRRT) and a theranostic approach.

The invention belongs to the field of molecular targeted therapy, and discloses a small-molecule inhibitor CTPI3 of a targeted mitochondrial citric acid transporter SLC25A1 and application of the small-molecule inhibitor CTPI3 in tumor therapy. On the basis of an existing inhibitor CTPI2 structure, molecular design is carried out through an induced fit docking (IFD) module of Schrdinger software, and CTPI3 is obtained. Experiments show that the median inhibitory concentration (IC50) of CTPI3 on acute myelogenous leukemia (AML) cell lines (such as Kasumi-1 and THP1) and primary AML cells is obviously lower than that of CTPI2, the synergistic effect of CTPI3 and Venetoclax is enhanced, the mitochondrial ATP yield is reduced, and the TCA cycle metabolite level is affected. Animal experiments prove that CTPI3 can significantly prolong the lifetime of AML model mice and reduce leukemia load (spleen weight is reduced, and bone marrow and peripheral blood GFPcells are reduced), and has no significant toxicity (liver, kidney and brain histopathology is normal). The invention provides an efficient and safe new candidate drug for SLC25A1 targeted therapy.

The invention discloses a piperazinyl modified quinazolinyl-aryl urea derivative as well as a preparation method and application thereof, and relates to the field of medicines. According to the piperazinyl-modified quinazolinyl-aryl urea derivative, two pharmacophores of 4-amino quinazolinyl and ureido are connected by adopting benzyl as an intermediate chain, phenyl, substituted phenyl, benzyl or naphthenic base is connected to the ureido, alkoxy is connected to the quinazoline ring 6-site, and # imgabs0 # cancer inhibition activity is high. The demethylation reagent used in the synthetic route can efficiently and selectively remove 6-position methyl of the intermediate 2, and the yield is high. A plurality of synthesized compounds show a good proliferation inhibition effect on cell lines such as human bladder cancer, osteosarcoma, pancreatic cancer and hepatoblastoma, show good tumor inhibition activity in a tumor-bearing nude mouse model, have the potential to become tumor molecular targeting drugs, have good water solubility and fat solubility, are suitable for various drug administration modes, and have wide application prospects. And the bioavailability is improved after modification.

This invention provides hepatocellular carcinoma-derived growth factor (HDGF) as a target for resistance to tyrosine kinase inhibitors and its related applications. This invention provides the application of HDGF as a target in screening and / or preparing drugs that can improve resistance to tyrosine kinase inhibitors in patients. This invention discovers that high expression of HDGF is one of the mechanisms of resistance to molecularly targeted drugs such as gefitinib and other tyrosine kinase inhibitors. Targeting HDGF can effectively improve resistance to gefitinib in NSCLC and enhance therapeutic efficacy.

The invention provides a detection reagent for LXOL2 gene expression quantity and application of LXOL2 as a rheumatoid arthritis treatment target, and relates to the technical field of biological medicines. According to an extracted total RNA sequence, a specific PCR primer is designed and synthesized, an RT-qPCR technology and a sequencing method are utilized, the expression of the LXOL2 in human synovial fibroblast-like cells is found to be remarkably increased, it is proved that the LXOL2 can be applied to preparation of a preparation for auxiliary diagnosis, treatment or prognosis evaluation of rheumatoid arthritis, meanwhile, Si-LOXL2 small in interference with the gene is designed and synthesized, and the application prospect is wide. According to the present invention, the expression of the LXOL2 gene can be knocked down, the expression of pro-inflammatory factors TNF-alpha, IL-1beta and IL-6 can be significantly inhibited, the expression of anti-inflammatory factors TGF-beta can be promoted, and the gene can be used as the RA molecular targeting treatment tool;

The invention discloses a red light-pH dual-response targeted antibacterial and anti-inflammatory nanoparticle as well as a preparation method and application thereof. The nano-particle is prepared from the following raw materials: a porphyrin-zirconium metal organic framework carrier, an antibacterial agent, NO donor molecules and a targeting ligand, the mass ratio of the porphyrin-zirconium metal organic framework carrier to the antibacterial drug to the NO donor molecule to the targeting ligand is 1: (0.8-1.2): (0.3-1): (1-3). The red light-pH dual-response targeted antibacterial and anti-inflammatory nano-particle is of a layered composite structure of'carrier-functional molecule-targeted shell ', and has high efficiency, safety and practicability.

Disclosed is a multi-specific molecule targeting CD16A expressed on NK cells and HER2 or GPC3 expressed on tumor cells, enhanced by a complex formed by IL-15 and IL-15Rα contained in the multi-specific molecule. Also disclosed are polypeptides, compositions and methods relevant to the multi-specific molecule.

The present application provides a polypeptide with binding affinity to HPV18 E6 protein, taking the Z domain of staphylococcal protein A as a scaffold, randomly mutating the surface amino acid residues to simulate antibody binding sites, constructing a mutant library through phage display technology, screening the library through affinity with HPV18 E6 as a target antigen, and finally obtaining a polypeptide with high affinity to HPV18 E6 through a large number of screening work. Through in-depth research, the present application first discloses a polypeptide with binding affinity to the E6 protein of HPV18. In addition, the present application also provides the diagnostic or therapeutic use of the polypeptide as a drug or molecular targeting reagent.

The invention provides application of a super enhancer inhibitor JQ-1 in preparation of a medicine for treating wound healing disorder related diseases. Relates to the technical field of biomedicine, the promotion effect of the super enhancer inhibitor JQ-1 in wound healing and repairing is disclosed for the first time, the super enhancer inhibitor JQ-1 is competitively combined with BET protein bromodomain, combination of the super enhancer inhibitor JQ-1 and acetylated histone is blocked, and super enhancer driven gene transcription is inhibited. Skin regeneration can be obviously accelerated, the wound healing time is shortened, and the healing degree is improved. Aiming at the pain point that the existing wound healing therapy is limited in effect, the invention provides a brand-new molecular targeted therapy scheme for people, such as diabetic patients and old people, which are easy to cause abnormal wound healing, can effectively reduce serious sequelae, such as amputation, and provides a scientific basis and a key direction for developing a novel medicine for promoting wound healing; the technical blank in the related treatment field is filled up, and important clinical application value and research and development prospects are achieved.

The invention discloses a prediction model for predicting a liver cancer combined treatment effect based on multi-mode MRI radiomics characteristics and a construction method and application thereof, and belongs to the technical field of liver cancer treatment effect prediction. In order to solve the problem that only part of liver cancer patients can benefit from an arterial chemoembolization combined targeted immunotherapy scheme at present, the invention proposes that before combined therapy, MRI radiomics characteristics and clinical factors are enhanced through noninvasive multi-modal comparison, multiple machine learning models are established, and the model learning model is used for learning the liver cancer patients. The tumor treatment response of arterial chemoembolism combined with molecular targeting and immunotherapy is predicted, and the applicability of the radiomics model is verified by using an external data set; besides, the radiomics model is combined with a clinical model, so that the method has more excellent prediction efficiency, and the radiomics features provide incremental prediction value for clinical factors. According to the method, the combined treatment effect of the liver cancer patients can be predicted, so that more effective and reasonable treatment schemes can be selected for different patients before treatment.

The present invention discloses a preparation method of a self-assembled zearalenone-14-glucoside gel, comprising mixing zearalenone-14-glucoside and methanol in a mass ratio of (10-20): 1 to obtain a zearalenone-14-glucoside methanol solution; adding distilled water to the zearalenone-14-glucoside methanol solution in a volume ratio of 2: 8 to obtain a zearalenone-14-glucoside methanol-water mixed solution, stirring thoroughly, heating at 50-90° C. for 1-2 hours, and then standing and cooling at room temperature to obtain a uniform translucent gel. The present invention uses a glycoside-type hidden fungal toxin with an estrogen-like effect as a gelling substance and a methanol-water mixed solvent to construct a natural self-assembled supramolecular gel with gel properties such as biocompatibility, sustained release, and molecular targeting.

The invention belongs to the technical field of biological medicine, and provides a novel gold nanoparticle-based targeting preparation as well as a preparation method and application thereof. The targeting preparation provided by the invention contains a gold nanoparticle core, a connecting molecule, a targeting ligand and a therapeutic agent, the connecting molecule and the targeting ligand sequentially modify gold nanoparticles, the therapeutic agent is loaded at the drug loading capacity of 1-50wt%, and the mass ratio of the targeting ligand to the gold nanoparticles is (1: 5)-(1: 100). The targeting preparation provided by the invention can efficiently cross the blood brain barrier, obviously reduce Abeta deposition in the brain, is high in enrichment degree of a targeting region in the brain, can down-regulate miR-146a-5p to inhibit neuroinflammation, and can be used for treating neurodegenerative diseases.

Methods, techniques, and kits are provided herein for purifying cells using molecular targeting, at a cellular or subcellular level. The techniques comprise labeling a biological sample comprising cells with a probe capable of directing the deposition of a hydrophobic protective barrier. The hydrophobic protective barrier is deposited onto the surface of the labeled cells or structures, to protect and retain the biological material under the barrier. A micropurification solution is applied to the biological sample, wherein the micropurification solution dissolves, degrades, digests, or otherwise processes cells not covered by the barrier, allowing for; 1) isolation and collection of the target cells for molecular analysis, 2) isolation and collection of the non-target cells for molecular analysis, 3) removal for the purpose of disposing of the non-target cells. In some aspects, a plurality of probes, each specific to a different target, may be used. The techniques may be performed without the need for complex instrumentation involving microscopy.

Methods, techniques, and kits are provided herein for purifying cells using molecular targeting, at a cellular or subcellular level. The techniques comprise labeling a biological sample comprising cells with a probe capable of directing the deposition of a hydrophobic protective barrier. The hydrophobic protective barrier is deposited onto the surface of the labeled cells or structures, to protect and retain the biological material under the barrier. A micropurification solution is applied to the biological sample, wherein the micropurification solution dissolves, degrades, digests, or otherwise processes cells not covered by the barrier, allowing for; 1) isolation and collection of the target cells for molecular analysis, 2) isolation and collection of the non-target cells for molecular analysis, 3) removal for the purpose of disposing of the non-target cells. In some aspects, a plurality of probes, each specific to a different target, may be used. The techniques may be performed without the need for complex instrumentation involving microscopy.

The invention provides a small peptide for preventing and treating colon cancer and application thereof, and belongs to the technical field of biological medicine. Through structural simulation and functional verification, a polypeptide capable of specifically inhibiting G3BP1 lactylation in colon cancer cells in a targeted manner is screened out. The polypeptide inhibits the lactic acid modification level of G3BP1 by simulating a G3BP1 lactic acid recognition site and competitively combining with lactic acid enzyme, so that the G3BP1 mediated autophagy process is blocked, and finally proliferation and migration of colon cancer cells are inhibited. In-vitro cell experiments (including cell proliferation, migration and autophagy level analysis) and in-vivo transplantation tumor animal experiments prove that the oligopeptide can significantly inhibit growth and tumor formation of colon cancer cells. The discovery provides a new strategy and candidate drug molecules for molecular targeted therapy of colon cancer.