19 results about "GLUT1" patented technology

The invention discloses application of an HIF1A inhibitor in preparation of a medicine for preventing and / or treating hypertrophic cardiomyopathy, and belongs to the field of biological medicine. For a rat model of spontaneous hypertrophic cardiomyopathy caused by MYH7B gene knockout, hypertrophic cardiomyopathy can be significantly relieved by intraperitoneal injection of the HIF1A inhibitor LW6, heart remodeling can be relieved, heart functions can be improved, and myocardial hypertrophy caused by silent MYH7B genes can be effectively resisted by using siRNA of mRNA transcribed by the HIF1A gene. The key mechanism of the HIF1A inhibitor for treating the hypertrophic cardiomyopathy is that the hypertrophic cardiomyopathy is prevented and treated by reducing the expression level of glycolysis key enzymes GLUT1, HK2 and the like, inhibiting the formation and accumulation of cardiac lactic acid and improving the ventricular remodeling of the hypertrophic cardiomyopathy. The results show that the HIF1A inhibitor can be used for treating and / or preventing the human hypertrophic cardiomyopathy and has the potential of being developed into the medicine for clinically preventing and treating the hypertrophic cardiomyopathy.

The invention discloses a glucan-based MMAE conjugate as well as a preparation method and application thereof, and relates to the technical field of medicines. The conjugate takes glucan with good biocompatibility as a carrier, and is covalently connected with a cytotoxic drug MMAE through a VC peptide linker capable of being cut by cathepsin B. The conjugate has good serum stability, can specifically release drugs at a tumor site, and realizes efficient tumor uptake by virtue of the stealth effect of glucan and potential GLUT1 targeting. In-vitro and animal experiments show that the conjugate has a remarkable treatment effect on pancreatic cancer and is low in systemic toxicity.

A PAMAM-based protein degradation system and a method of preparation and use thereof are provided. The protein degradation system comprises: a silica nanoparticle core; and a poly(amidoamine) dendrimer (PAMAM) layer coated on a surface of the silica nanoparticle, wherein the PAMAM layer is linked via amide bonds to three small-molecule ligands: MDM2 protein ligand Idasanutlin, GLUT1 protein ligand Lavendustin B and E3 ubiquitin ligase ligand Thalidomide-NH—CH2—COOH. The nanoparticle protein degradation system cooperatively degrades MDM2 protein and GLUT1 protein. This cooperative degradation strategy not only effectively suppresses proliferation and energy metabolism of tumor cells, but also significantly enhances the stability of p53 protein. By restoring the normal function of p53 protein, tumor cell growth is further inhibited, providing a new strategy for cancer therapy.

The application discloses application of aurantiamarin in preparation of a GLUT1 protein targeting inhibitor with high affinity, and belongs to the technical field of medicinal chemistry. It is found that aurantiamarin shows micromolar (muM) level high-efficiency inhibitory activity on GLUT1, and the aurantiamarin may play a role through a new mechanism different from existing competitive inhibitors, such as allosteric inhibition or state-dependent blockage, effectively blocks glucose uptake, and is not prone to drug resistance.

The present invention relates to a novel antisense transcript to the human SLC2A1 (Glut1) gene, variants and fragments thereof. This antisense transcript can be used to modulate Glut1 expression and serve to restore Glut1, and as a therapeutic for treating or preventing Glut 1 deficiency syndrome, or other Glut1 related conditions including certain cancers, diabetes, Alzheimer's disease, and retinitis pigmentosa.

The invention discloses a preparation method and application of glucose transporter 1 targeting brucea javanica fatty acid prodrug liposome, and belongs to the technical field of pharmaceutical preparations. Specifically, the invention relates to a targeting material based on glucose transporter 1 (GLUT1), a tumor sensitive bond bridged brucea javanica-fatty acid prodrug, construction of an active targeting liposome containing the prodrug, and application of the active targeting liposome in preparation of antitumor drugs. The anti-liver cancer effect of the liposome is investigated. Results show that the lipidosome designed by the invention can realize targeted drug delivery to tumor tissues, the anti-tumor efficacy of the brucea javanica terpene drug is remarkably improved, the biosafety is high, and the toxicity is reduced by two times compared with that of the original drug brucea javanica bitter alcohol. The tolerance dose of the chemotherapeutic drug is expected to be increased, the anti-tumor effect of the chemotherapeutic drug is improved, and a new direction and a new thought are provided for the delivery of the chemotherapeutic drug.

Provided herein are methods of stratifying oral lesions based on the risk of progressing into a malignant tumor, and methods of treating subjects involving selective removal of oral lesions identified as high risk. In some aspects, the methods provided herein include assessing risk based on expression of SLC2A1 on a lesion.

The application provides an application of PTN and an extracellular vesicle loaded with PTN in preparation of a medicine for treating diabetic nephropathy, and belongs to the technical field of biological medicine; the application finds and confirms that small extracellular vesicles derived from human umbilical cord mesenchymal stem cells interact with glucose transporter 1 (GLUT1) in renal tubular epithelial cells through the multi-effect protein (PTN) carried by the small extracellular vesicles and down-regulate the expression of the glucose transporter 1, so as to inhibit abnormal aerobic glycolysis induced by high glucose, reduce lactic acid accumulation, and then repair the damage of diabetic nephropathy by reducing the lactic acid level; the application further verifies the role of PTN in the repair of the damage of diabetic nephropathy, and compared with a broad-spectrum HDAC inhibitor, the treatment strategy is more targeted, and is expected to reduce off-target effects and systemic toxicity; the PTN and the extracellular vesicle loaded with PTN can be developed for preparing a medicine for diabetic nephropathy, and have good practicability.

The application discloses an NAD + The application discloses a related nanopharmaceutical brain-targeting delivery system, a preparation method and application thereof, and the delivery system is composed of a carrier shell containing NAD + The related active ingredient is composed of a core of the related active ingredient and a carrier shell of a surface-modified brain-targeting ligand, NAD + The related active ingredient is complexed and coordinated to realize high drug loading and stable encapsulation, and multiple types of brain-targeting ligands are jointly modified to make the delivery system have the ability of transporting across the blood-brain barrier and locating in brain cells. + The application combines the supplement with a GLUT1 / RVG double-ligand brain-targeting strategy to construct a safe, high-drug-loading and high-stability NAD + The related nanopharmaceutical system can improve the NAD(H) content of brain tissues, improve mitochondrial function, reduce oxidative stress and neural inflammation, and reverse or reduce the aging phenotype of astrocytes, and provides a new drug delivery strategy for Parkinson's disease and aging-related neurodegenerative diseases.

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a WZB117 nano preparation and a preparation method thereof. In the treatment of uveal melanoma, there is a lack of effective treatment scheme. The application provides a novel ophthalmic preparation and a preparation method thereof, and utilizes hemoglobin and dopamine to simultaneously carry a glucose transporter 1 (Glut1) inhibitor WZB117 and copper ions. The nano preparation can form a positive feedback cycle through a copper death-induced active oxygen burst and an antioxidant system collapse caused by WZB117 double-sulfur death, so as to accelerate tumor cell death.

The invention belongs to the field of drug delivery system construction, and particularly relates to a target-drug self-adaptive transformation cross-linking self-assembly nano platform as well as a preparation method and application of the target-drug self-adaptive transformation cross-linking self-assembly nano platform. The doxorubicin is creatively taken as a carrier and a targeting ligand for oral delivery of the doxorubicin, so that the specific targeting and treatment effects of a tumor part are realized. The doxorubicin hydrochloride is subjected to stable self-assembly by virtue of disulfide bond crosslinking through a specific crosslinking material, a hydrophilic end sugar ring of the doxorubicin hydrochloride is anchored on the surface of a nanoparticle, and an intestinal epithelial cell barrier and a blood brain barrier are crossed by recognizing SGLT1 and OCTN2 which are highly expressed on a top side membrane of an intestinal epithelial cell, GLUT2 on a substrate side and GLUT1 on the surfaces of brain microvascular endothelial cells and glioma cells. The nanoparticles not only significantly improve the oral bioavailability of adriamycin, but also have an efficient accumulation effect in the brain, further break disulfide bonds and release adriamycin in a high-GSH environment, and achieve a safe and efficient anti-tumor effect.

This invention provides a screening method for occludin expression-promoting components, using the expression level of GLUT1 in skin tissue as an indicator. [Solution] A screening method for occludin expression-promoting components using the expression level of GLUT1 in skin tissue as an indicator.

IMPROVED GLUT1-BINDING POLYPEPTIDES The present invention relates to a glucose transporter protein type 1 (GLUT1)-binding polypeptide comprising, or consisting of, an amino acid sequence selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 22 to 26, and variants or fragments thereof, wherein the sequences of said variants or fragments comprise a serine (S) residue at position corresponding to position 95 of SEQ ID NO: 1, 23 and 25, or to position 97 of SEQ ID NO: 22, 24 and 26. The present invention further relates to in vitro and in vivo methods of specifically detecting or / and measuring the level of GLUT1, and to the use of said polypeptides in diagnosis and therapy.

The present invention relates to the use of the proportion of plasma cells, lymphocytes or blasts expressing GLUT1 among total plasma cells, lymphocytes or blasts in a method for stratifying prognosis of subjects suffering from a hematologic disorder, and in a method for determining whether a subject suffering from a hematologic disorder will achieve or is achieving a response with a modulator of the BCL-2 family proteins. The present invention also relates to a kit for detecting GLUT1, and optionally ASCT2, for implementing one of these methods.

The invention discloses a GLUT1 glucose injection device for sepsis cardiomyopathy, and relates to the technical field of injection devices.The GLUT1 glucose injection device comprises a main body mechanism, the main body mechanism comprises a shell, a controller is fixedly connected to one side of the shell, and two positioning plates are fixedly connected to the top of the shell; the GLUT1 glucose injection device comprises two positioning plates, the inner walls of the two positioning plates are fixedly connected with damping rotating shafts, the rotating ends of the damping rotating shafts are fixedly connected with positioning hooks, and one sides of the two positioning hooks are jointly and fixedly connected with a transparent cover. A plurality of injection barrels can be installed at a time, automatic switching and butt joint of the injection barrels and independent setting of parameters of the injection barrels are achieved, the injection precision of a glucose solution is guaranteed, meanwhile, the working difficulty of medical workers is lowered, the continuity and timeliness of injection are guaranteed, simultaneous working of a plurality of injection pumps is avoided, and the working efficiency is improved. Therefore, the space is saved.

The invention relates to the technical field of biological medicines, and relates to application of circPTK2 as a marker in preparation of a product for bladder cancer diagnosis or prognosis. Researches show that the CAFs-derived exosome can deliver circPTK2 to bladder cancer cells, the circPTK2 can be combined with C-Myc protein and promote nuclear translocation of the C-Myc protein, then expression of C-Myc downstream Warburg effect related proteins GLUT1 and LDHA is regulated and controlled, and migration, invasion and lymph node metastasis of the bladder cancer cells are affected. Meanwhile, the circPTK2 level in serum and urine exosomes is closely related to prognosis and lymphatic metastasis of bladder cancer patients and can be used as an effective marker for diagnosis and prognosis of bladder cancer and prediction of lymphatic metastasis, and a new thought and tool are provided for clinical diagnosis and treatment of bladder cancer.

The application discloses an anti-tumor hydrogel based on a starvation therapy and a preparation and application thereof. After simple mixing of a DHA solution, an AI solution, an Ink solution and an ALG solution, a DHA / AI / Ink@ALG is formed, an in-situ hydrogel is formed by simple injection in a tumor tissue, under 1064nm laser irradiation, alkyl radicals are generated by starting AI decomposition by using a low-temperature photothermal effect, damage of DHA-induced mitochondrial oxidative stress is intensified by using the alkyl radicals, and glucose uptake is reduced by strengthening DHA inhibition on GLUT1, so that DHA-induced cell starvation therapy is enhanced, the effect of anti-tumor treatment is significantly improved, and a new way is provided for high-efficiency and low-toxicity cancer treatment.

The invention relates to an anti-cancer drug for synergistically regulating and controlling pyroptosis of pancreatic cancer cells based on magnolol and glucose metabolism and application of the anti-cancer drug. The anti-cancer drug is a key enzyme GLUT1 inhibitor for magnolol and glucose metabolism. By combining magnolol with a glucose deprivation / GLUT1 inhibitor (such as BAY-876) and by inhibiting mitochondrial autophagy (PINK1 degradation) and mitochondrial ROS accumulation and triggering a new mechanism of apoptosis-pyroptosis conversion, the limitation that a traditional natural product only depends on an apoptosis pathway is broken through; the immunoregulation of mitochondrial autophagy inhibition and pyroptosis induction is creatively associated; metabolic intervention induced pyroptosis is directly associated with pancreatic cancer'immune cold 'microenvironment remodeling, and an important theoretical basis is provided for natural product combined immunotherapy. Meanwhile, a CDX model (magnolol combined with a GLUT1 inhibitor) and ketogenic diet simulation metabolism intervention are combined, and a closed-loop verification system from a molecular mechanism to in-vivo treatment is established, so that clinical development of metabolism intervention-natural product-immune combined treatment can be promoted.

The attachment of glucose to drugs and imaging agents enables cancer cell targeting via interactions with GLUT1 overexpressed on the cell surface. The present technology describes a biomimetic approach for the design of a multivalent glucose moiety (mvGlu). We showcase the utility of this new group by developing aza-BODIPY-based contrast agents boasting a significant PA signal enhancement greater than 11-fold after spectral unmixing. Moreover, when applied to targeting cancer cells, effective staining could be achieved with ultra-low dye concentrations (50 nM) and compared to a non-targeted analog, the signal intensity was >1000-fold higher. Also, we employed the mvGlu technology to develop a logic-gated acoustogenic probe to detect intratumoral Cu(I), which is an emerging cancer biomarker, in a murine model of breast tumor. This application was not possible using other acoustogenic probes previously developed for copper sensing.