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152 results about "Glucocorticoid" patented technology

Glucocorticoids are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure to the right). A less common synonym is glucocorticosteroid.

Nitric oxide data analysis method and system for bronchial asthma assessment

The invention relates to a nitric oxide data analysis method and system for bronchial asthma assessment. According to the method, exhaled air nitric oxide and pulmonary alveolar nitric oxide of a patient, omics data and clinical information are acquired in a standardized manner, and multi-dimensional features are constructed after data cleaning and fusion; comprise an inflammation level index, an inflammation region entropy, an inflammation synergy index, a glucocorticoid response factor, an infection-smoking synergy influence factor and a heredity-symptom distribution index. And outputting initial risk assessment based on an explainable elevator EBM model, and finally generating an asthma risk probability through a weighted integration formula to realize three-level layering: low / medium / high risk. The system dynamically associates treatment decisions, for example, the drug dosage and the monitoring frequency are improved when the risk is upgraded, and the medication scheme is optimized when the risk is degraded. According to the scheme, the limitation of traditional single marker static analysis is broken through, multiple mechanisms of dissection, immunity and pharmacology are fused, the evaluation precision and clinical applicability are remarkably improved, the acute attack rate is reduced, and accurate typing treatment is guided.
Owner:FUDING CITY HOSPITAL

Drug combination of purinostat mesylate and analog thereof for preventing and treating multiple myeloma, and use thereof

A drug combination of purinostat mesylate and an analog thereof for preventing and treating multiple myeloma, and the use thereof. Specifically, provided is a three-drug or four-drug combination of purinostat mesylate and an analog thereof, dexamethasone and other drug, which drug combination has significantly enhanced synergistic anti-tumor activity in vitro and in vivo, synergistically inhibits the expression of the key survival protein in multiple myeloma, is superior to existing clinical combination regimens, and has no significant toxic side effects. In addition, the drug combination significantly down-regulates the expression of CDK6, and overcomes the drug resistance to an immunomodulator. In particular, the three-drug combination of puisostat mesylate, a glucocorticoid and an immunomodulator has an excellent prevention and treatment effect on multiple myeloma, especially relapsed / refractory multiple myeloma.
Owner:CHENGDU ZENITAR BIOMEDICAL TECH CO LTD

Construction method of glucocorticoid induced diabetes risk prediction model based on LASSO algorithm

InactiveCN120674064AMedical data miningDrawing from basic elementsHospitalized patientsAlgorithm
The invention relates to the technical field of medical data analysis and clinical risk prediction, provides a construction method of a glucocorticoid induced diabetes risk prediction model based on an LASSO algorithm, and belongs to the technical scheme of data processing executed on computing equipment. Clinical data of inpatients receiving systemic glucocorticoid treatment are collected, key variables are screened through LASSO regression, and a Logistic regression model is constructed to achieve risk prediction. The model is composed of four conventional clinical indexes, has good distinction degree and calibration degree, and finally realizes individualized risk assessment through column diagram form output. The method is simple, practical and accurate, and is suitable for SDM prediction and intervention management of clinical high-risk groups.
Owner:XUZHOU MEDICAL UNIVERSITY

Application of ganoderma lucidum spore oil in preparation of medicine or health food for improving sarcopenia

The invention discloses an application of ganoderma lucidum spore oil in preparation of a medicine or health food for improving sarcopenia. Ganoderma lucidum spore oil can effectively improve weight loss and muscle hypofunction induced by glucocorticoid, and improve the holding power and exercise tolerance level of the body; meanwhile, the skeletal muscle mass and the muscle fiber cross sectional area can be increased, and the skeletal muscle tissue morphological structure is improved; in addition, the ganoderma lucidum spore oil can improve the oxidation resistance of the body and skeletal muscle and reduce the oxidative stress level, so that the skeletal muscle injury related to aging is relieved on the whole. Therefore, the ganoderma lucidum spore oil has a definite application value in the aspect of improving the skeletal muscle function.
Owner:SOUTHEAST UNIV

High-potency glucocorticoid compound as well as preparation and application thereof

The invention provides a high-potency glucocorticoid compound as well as a preparation method and application thereof. Specifically, the invention provides a high-potency glucocorticoid compound as shown in a formula I as well as a preparation method and application of the high-potency glucocorticoid compound. The glucocorticoid compound of the present invention can achieve the same effect at a lower dose, thereby minimizing side effects. # imgabs0 #
Owner:ZHEJIANG PALOALTO PHARMA TECH CO LTD

High-efficacy glucocorticoid polymorph, preparation method therefor, and use thereof

PendingAU2024396409A1FuranDodecane
The present invention relates to a novel polymorph of (1R,2R,3aS,3bR,10aS,10bR,11S,12aS)-5,10b-difluoro-1-(((fluoromethyl)thio)carbonyl)-11-hydroxyl-2,10a,12a-trimethyl-7-phenyl-1,2,3,3a,3b,7,10,10a,10b,11,12,12a-dodecylhydrocyclapenta[5,6]napththo[1,2-F]indazole-1-furan-2-carboxylate ester as shown in formula (I), a preparation method therefor, and a use thereof. The crystal form of the present invention has characteristics such as a significant pharmaceutical effect, good stability, high yield, and high purity, and is beneficial for the selection and design of a drug administration route and the determination of a drug preparation process parameter, thereby improving drug production quality.
Owner:ZHEJIANG PALOALTO PHARMA TECH CO LTD

Application of ginkgetin in treatment of chronic pulmonary obstruction

The invention discloses application of ginkgetin in treatment of chronic pulmonary obstruction, and relates to the field of medical technical methods of ginkgetin. According to the invention, by constructing a model of cigarette extract on airway epithelial cell injury, the biflavone compound is found to have a protective effect on epithelial cell injury caused by smoking; through transcriptomics research, biflavone compounds such as ginkgetin and the like are found to have pharmacological activity of inhibiting CEBP beta protein high expression caused by cigarette extracts, so that the effect of protecting airway inflammation caused by smoking is achieved. More importantly, the ginkgetin and the glucocorticoid are jointly used, so that the treatment effect on chronic pulmonary obstruction is remarkably improved compared with that of independently using the ginkgetin and the glucocorticoid, and the ginkgetin and the glucocorticoid have wide medical application.
Owner:HUAZHONG UNIV OF SCI & TECH

Novel glucocorticoid, method for preparing same, and use thereof

The present disclosure relates to the technical field of medicinal chemistry, and particularly, to a novel glucocorticoid, a method for preparing same, and use thereof. The novel glucocorticoid comprises a compound represented by formula I, an optical isomer thereof, a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein the structure of the compound represented by formula I is shown herein. The compound provided by the present disclosure exhibits a high plasma clearance rate, a short half-life, reduced systemic exposure, and enhanced glucocorticoid receptor (GR) selectivity, thereby significantly reducing the adverse effects associated with systemic absorption of the glucocorticoid drug. The present disclosure has significant anti-inflammatory activity in animals with asthma, uveitis, dry eye syndrome, inflammatory bowel disease, psoriasis, and the like. The compound provided by the present disclosure demonstrates good safety, with no abnormal intraocular pressure observed after continuous ocular administrations in guinea pigs and no significant changes in the thickness of the epidermal layer after continuous dermal administrations in rats.
Owner:TIANJIN PHARM BIOTECHNOLOGY CO LTD

Combination therapy for prostate cancer

ActivePH12019502317B1GlucocorticoidProstate cancer
Provided are methods and compositions, for treating prostate cancer by administering to a patient in need thereof a therapeutically effective amount of a PARP inhibitor, e.g., niraparib; a therapeutically effective amount of a CYP17 inhibitor, e.g., abiraterone acetate, and a therapeutically effective amount of a glucocorticoid, e.g., prednisone.
Owner:JANSSEN PHARMA NV

Methods and compositions for treating glucocorticoid excess

The disclosure provides a method of treatment for glucocorticoid excess in a patient in need thereof, comprising administering to the patient a pseudo-irreversible HSD-1 inhibitor.
Owner:SPARROW PHARMACEUTICALS INC

Multifunctional selenium nanoparticle for treating inflammatory bowel disease as well as preparation method and application of multifunctional selenium nanoparticle

The invention discloses multifunctional selenium nanoparticles for treating inflammatory bowel diseases as well as a preparation method and application of the multifunctional selenium nanoparticles, and relates to the technical field of biological medicines. The multifunctional selenium nanoparticle is of a core-shell structure and comprises an inner core and an outer layer coating the inner core, the inner core is selenium nanoparticles; and the outer layer is a polydopamine shell embedded with chitosan oligosaccharide. The multifunctional selenium nanoparticles provided by the invention have good stability and dispersibility, can target intestinal inflammation parts, prolong the in-vivo time of the nanoparticles, and show strong antioxidant and anti-inflammatory activity on cell and animal levels. The whole nanoparticle is based on low toxicity and colon targeting of a natural material, is higher in safety compared with a traditional glucocorticoid / biological preparation, relieves intestinal inflammation by adjusting a redox steady state, prolonging drug action time and the like, and is expected to become a novel colitis treatment strategy with high efficiency, targeting property and safety.
Owner:INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI

A method for preparing CCR2+ gamma delta T cells with anti-tumor activity and migration ability

The application discloses a preparation method of CCR2+ gamma delta T cells with anti-tumor activity and migration ability, and belongs to the technical field of cells; the method comprises the following steps: step (1), PBMC of peripheral blood of a healthy person is extracted, inoculated into complete culture medium, and added with zoledronic acid, IL-15 and metformin, and then is cultured in a T25 culture bottle; step (2), complete culture medium is supplemented, the cell concentration is adjusted, and then the cells are transferred into a T75 culture bottle for culture; step (3), complete culture medium is supplemented, the cell concentration is adjusted, glucocorticoid and nicotinamide are added, and then the cells are transferred into a T150 culture bottle for culture; step (4), cells are collected at D6, rinsed with normal saline, resuspended with complete culture medium, the cell concentration is adjusted, and then the cells are inoculated into a T300 culture bottle for culture; and step (5), complete culture medium is supplemented every two days from D8 to D16, the cell concentration is maintained, and then the cells are harvested at D16 to obtain CCR2+ gamma delta T cells.
Owner:BEIJING WEICHUANG BOJING BIOTECHNOLOGY CO LTD

Three-channel bionic bone organ chip and method thereof

The invention discloses a three-channel bionic bone organ chip and a method thereof.The three-channel bionic bone organ chip comprises a three-channel model and a carrier, the three-channel model comprises a blood vessel channel in the middle and bone channels located on the two sides of the blood vessel channel, the width of the blood vessel channel is 500 micrometers, the width of the bone channels is 1000 micrometers, and the width of the carrier is 100 micrometers. The two sides of the blood vessel channel are separated from the bone channels on the two sides through long barriers respectively. The carrier is used for bearing the three-channel model. According to the invention, a novel bone organ chip (Bone Orga-on-a-Chip, BOC) is constructed, which is convenient for simulating an OP microenvironment induced by glucocorticoid and the influence of mechanical mechanics on treatment of OP by MSCs. On the basis, a candidate gene TPD52L1 is further analyzed and screened through bioinformatics, the candidate gene TPD52L1 is remarkably up-regulated in MSCs induced osteogenic differentiation, and the effect of the gene in MSCs osteogenic adipogenic fate choice is discussed.
Owner:JILIN UNIVERSITY

Biomarker, kit, system and method for phenotypic typing of acute respiratory distress syndrome inflammation and application of biomarker, kit, system and method

The invention discloses a biomarker, a kit, a system, a method and application for acute respiratory syndrome (ARDS) inflammation phenotype typing. The biomarker combination is selected from any two or a combination of more than two of PLAUR, BSG, TNFRSF14, DFFA, IFNGR1, ENAH, LAIR1, NUB1, AGRN, LTBR, BTN3A2 and F2R, and the biomarker combination is a combination of any two or more of PLAUR, BSG, TNFRSF14, DFFA, IFNGR1, ENAH, LAIR1, NUB1, AGRN, LTBR, BTN3A2 and F2R. By detecting the expression level of the marker in serum of a subject and utilizing a machine learning classification model (such as XGBoost) for analysis, ARDS patients can be divided into three phenotypes of C1 (high inflammation and high injury), C2 (low inflammation repair) and C3 (intermediate). The typing method can accurately predict clinical outcomes such as the 90-day death rate of the patient and guide individualized application of glucocorticoid and PEEP ventilation strategies, and has important significance for achieving accurate treatment of ARDS.
Owner:ZHONGSHAN HOSPITAL FUDAN UNIV

Use of metformin to mitigate corticosteroid-associated osteonecrosis or osteoporosis

Compositions and methods are provided for the prevention of osteonecrosis or osteoporosis associated with corticosteroid administration in an individual. The methods of the disclosure comprise administration of an effective dose of a metformin agent, or a derivative, mimetic or analog thereof in combination with administration of a corticosteroid. The effective dose of metformin agent decreases oxidative stress and restores osteogenic capacity of mesenchymal stem cells exposed to a glucocorticoid.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV

Method of treatment for prevention of glucocorticoid toxicity and / or enhancement of muscle regeneration via neutrophil elastase inhibition

The present disclosure is directed to methods of treatment, including treatment of a myopathy by administering to a subject in need thereof an elastase inhibitor in combination with a glucocorticoid. The present disclosure is also directed to pharmaceutical compositions that include an elastase inhibitor that can be used in such treatment.
Owner:UNIV OF LIVERPOOL +1

Pharmaceutical composition for preventing esophageal stenosis

The invention discloses a pharmaceutical composition for preventing esophageal stenosis. The pharmaceutical composition consists of glucocorticoid and sesame oil, the glucocorticoid is triamcinolone acetonide or dexamethasone. The pharmaceutical composition provided by the invention is prepared from 1-5 parts by weight of triamcinolone acetonide and 10-15 parts by weight of sesame oil; or 5-10 parts by weight of dexamethasone and 100 parts by weight of sesame oil. The medicine composition is simple, raw materials are low in price, and mass production and use are facilitated. Practical research finds that the pharmaceutical composition provided by the invention can be used for preventing esophageal stenosis caused by disease reasons, such as esophageal stenosis after large-area endoscopic submucosal dissection (the dissection area is 2 / 3 or above) of esophageal premature cancer, esophageal restenosis after benign esophageal stenosis dilation treatment and the like.
Owner:CHENGDE CENT HOSPITAL

Achyranthes bidentata sterone compound as well as preparation method and application thereof

The invention discloses a sterone compound derived from achyranthes bidentata as well as a preparation method and application of the sterone compound. Belongs to the technical field of biological medicine. The invention aims to solve various side effects and defects of the existing medicine for treating glucocorticoid-induced osteoporosis in long-term use. The molecular formula of the compound (SSA) is C33H48O9, the compound (SSA) has a beta-ecdysterone skeleton, and acetal type 5-hydroxymethylfurfural groups are introduced at the positions of side chains C20 and C22. SSA has a remarkable protection effect in a DEX-induced osteoblast injury model, can improve cell viability decline and G1 phase retardation caused by glucocorticoid, and recovers osteogenic differentiation and mineralization ability. The SSA effectively reverses the inhibition effect of DEX on osteoblasts by activating a Wnt / beta-catenin signal channel and up-regulating the expression of RUNX2. SSA has a remarkable anti-osteoporosis function potential.
Owner:HEILONGJIANG UNIV OF CHINESE MEDICINE

Immunochromatography test strip for detecting clobetasol propionate in cosmetics

The invention provides an immunochromatography test strip for detecting clobetasol propionate in cosmetics and a method for quantitatively detecting clobetasol propionate in cosmetics. According to the invention, a hollow gold nano-labeled material is applied to immunodetection of glucocorticoid clobetasol propionate for the first time, and an immunochromatography test strip with high sensitivity, quantitative function and strong specificity is constructed. The test strip can complete detection within 15 minutes, has high detection sensitivity, and realizes accurate quantification in a range of 0.01-25 ng / mL; meanwhile, the method is high in anti-interference capacity, the detection recovery rate of actual cosmetic samples reaches up to 89%-107%, the false positive rate and the false negative rate are both 0, reliability is good, and a powerful screening analysis tool is provided for rapid screening and quantitative detection of clobetasol propionate addition in cosmetics.
Owner:WUXI DRUG SAFETY INSPECTION & TESTING CENT (WUXI DRUG INSPECTION INST)

Cell culture fluid and method for detecting glucocorticoid in biomass

The invention provides a cell culture fluid and a method for detecting glucocorticoid in biomass, and relates to the technical field of food detection. According to the detection method, ethyl acetate is used for extracting glucocorticoids in a cell culture fluid and biomass, then the cell culture biomass is purified through an HLB solid-phase extraction column, ultra-high performance liquid chromatography-tandem mass spectrometry is adopted for detection, and simultaneous detection of 40 glucocorticoids in the cell culture fluid and biomass can be achieved. The method successfully separates and accurately quantifies seven pairs of isomers difficult to separate including dexamethasone and betamethasone, and has the remarkable advantages of simplicity and convenience in operation, high accuracy, wide applicability and the like.
Owner:INST OF QUALITY STANDARD & TESTING TECH FOR AGRO PROD OF CAAS

A dexamethasone-loaded hydrogel for injection, a preparation method and application thereof

PendingCN122351142ADiseaseGlucocorticoid
This invention discloses a sodium alginate cross-linked matrix metalloproteinase-sensitive peptide-loaded dexamethasone sodium phosphate hydrogel and its preparation method. The dexamethasone-loaded hydrogel has good injectability. After injection, it is cleaved by MMPs at the site of inflammation in an inflammatory environment to release dexamethasone, exhibiting good sustained-release effect. It achieves targeted and long-acting treatment of inflammatory arthritis, osteoarthritis or other inflammatory diseases, and reduces the frequency of repeated intra-articular injections of glucocorticoids.
Owner:ZHONGSHAN LAIBO RUICHEN BIOMEDICINE CO LTD

Method for non-targeting screening of hydroxyl esterification-derived glucocorticoids in cosmetics by using low-resolution mass spectrometry

The invention discloses a method for non-targeting screening of hydroxyl esterification-derived glucocorticoid in cosmetics by using a low-resolution mass spectrum, which specifically comprises the following steps: adding sodium hydroxide with the concentration of 10 mg / mL into an acetonitrile solvent system under an alkaline condition, and adding a quantitative stabilizer consisting of EDTA (Ethylene Diamine Tetraacetic Acid) and sodium ascorbate into a reaction system, the method comprises the following steps: controlling the reaction time at room temperature to be 1 hour, adding an acetonitrile aqueous solution containing acetic acid to adjust the reaction system to be in an acidic environment and metering the volume, performing hydrolysis deesterification on glucocorticoids derived from different esterification of hydroxyl groups at 21 site and (or) 17 site of a D ring, returning to the state before esterification and derivation, and enabling the product to be stable; furthermore, only one kind of hydroxyl esterification-free glucocorticoid is adopted as a standard substance, and the hydroxyl esterification-derived glucocorticoid in cosmetics can be screened in a non-targeted manner through high performance liquid chromatography-tandem triple quadrupole mass spectrometry.
Owner:大连市检验检测认证技术服务中心

Method for lymphotropic treatment of lymphoedema

The invention relates to clinical medicine, and more particularly to lymphology, surgery, plastic surgery and oncology, for treating lymphatic swelling in the case of primary or secondary lymphoedema in adults and children, inter alia accompanied by infectious complications, and even more particularly relates to methods for treating lymphoedema and to the use of accessible drugs in the treatment of lymphatic swelling at any stage and in any location. The claimed method for the lymphotropic treatment of lymphoedema involves consecutively preparing an injectable drug composition A containing an adrenergic alpha-1 receptor agonist and a glucocorticoid, administering same by lymphotropic interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest and introducing the drug composition, preparing an injectable drug composition B containing a cholinesterase inhibitor, administering same by lymphotropic interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest and introducing the drug composition, and also, if necessary, preparing an injectable drug composition C containing bovhyaluronidase azoximer, and administering same by interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest. The technical result consists in improving the drainage of free fluid from the tissues and reducing limb swelling in the case of lymphoedema.
Owner:INDIVIDUALNIY PREDPRINIMATEL GARYAEV KONSTANTIN PAVLOVICH

Detection for determining corticosteroid responsiveness

The present invention relates to methods, kits, and compositions for testing a sample from a subject with asthma to determine: i) if the subject is A / A or A / C at position 1245 in the HSD3B1 gene, and / or if the subject expresses a 367N version of the 3β-HSD1 protein (e.g., and should be administered a non-corticosteroid for their asthma), or ii) if the subject is C / C at position 1245 in the HSD3B1 gene, and / or if the subject expresses only the 367T version of the 3β-HSD1 protein (e.g., and should be administered a corticosteroid for their asthma). In certain embodiments, the corticosteroid is a glucocorticoid.
Owner:THE CLEVELAND CLINIC FOUND +1

Steroids and protein-conjugates thereof

Described herein are protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.
Owner:REGENERON PHARMACEUTICALS INC

Therapeutic combinations of an AKT inhibitor, a BCL-2 inhibitor, and a glucocorticoid

Therapeutic combinations of an AKT inhibitor and a BCL-2 inhibitor; an AKT inhibitor and a glucocorticoid; and an AKT inhibitor, a BCL-2 inhibitor and a glucocorticoid are described. The combinations can be useful in the treatment of acute lymphoblastic leukemia (ALL).
Owner:ASTRAZENECA AB

Traditional Chinese medicine composition for preventing or treating progressive hearing loss of large vestibular aqueduct syndrome as well as preparation method and application of traditional Chinese medicine composition

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for preventing or treating progressive hearing loss of large vestibular aqueduct syndrome as well as a preparation method and application of the traditional Chinese medicine composition. The traditional Chinese medicine composition is prepared from fructus psoraleae, herba cistanche, rhizoma drynariae, poria peel, polyporus umbellatus, cortex mori radicis, plantain herb, radix salviae miltiorrhizae, ligusticum wallichii, caulis spatholobi and honey-fried licorice root. The traditional Chinese medicine composition disclosed by the invention has the effects of tonifying kidney and strengthening primordial qi, and tonifying spleen and promoting urination, and is mainly used for preventing or treating patients with progressive hearing loss caused by large vestibular aqueduct syndrome. Compared with western medicine glucocorticoid, the traditional Chinese medicine composition has no adverse reaction, the health risk is reduced, and the treatment tolerance and compliance of patients are improved. A standardized scheme for preventing or treating progressive hearing loss of large vestibular aqueduct syndrome by traditional Chinese medicine is formed, clinical popularization is facilitated, more patients are benefited, a reference basis is provided for subsequent research, and related medical research is promoted.
Owner:HANGZHOU RENAI DEAFNESS REHABILITATION INSTITUTE

Treatment of lupus nephritis with Anti-type i inf receptor antibody anifrolumab

To provide a new method for treating lupus nephritis (LN), which improves renal response, reduces recurrence, prevents eventual end-stage renal disease (ESRD), and reduces the need for glucocorticoids.SOLUTION: WHAT IS CLAIMED IS: 1. A method of reducing lupus nephritis (LN) disease activity in a subject in need thereof, comprising administering to the subject a type I IFN receptor (IFNAR1) inhibiting agent. Preferably, the IFNAR1 inhibitors are human monoclonal antibodies specific for IFNAR1, such as anifrolumab.SELECTED DRAWING: None
Owner:ASTRAZENECA AB

Application of isogarcinol compounds combined with dexamethasone in the preparation of drugs for treating leukemia

The present invention provides the use of isogaminol compounds in combination with glucocorticoids in the preparation of a leukemia treatment drug, belonging to the technical fields of biology and medicine. The isogaminol compounds described herein, when used in combination with glucocorticoids, can enhance the sensitivity of Jurkat cells to glucocorticoids, induce G1 cell cycle arrest in Jurkat cells, and induce apoptosis in Jurkat cells. The combined use of isogaminol compounds and glucocorticoids in the present invention provides a research foundation for overcoming glucocorticoid resistance in acute lymphoblastic leukemia.
Owner:THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI

Protein degradation targeting chimera compound targeting 11 beta-HSD1 and medical application of protein degradation targeting chimera compound

The invention relates to the field of biological medicine, and discloses a protein degradation targeting chimera (PROTAC) compound targeting 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) and medical application of the protein degradation targeting chimera (PROTAC) compound. The compound comprises a structural unit shown as a formula I, X is a 11 beta-HSD1 binding ligand, Y is a connecting chain, Z is an E3 ubiquitin ligase ligand, ubiquitination degradation of 11 beta-HSD1 can be induced, and therefore the function of the compound can be regulated and controlled at the protein level. Different from a traditional small-molecule inhibitor, the degradation agent can significantly reduce expression of 11 beta-HSD1 in cells and improve glucocorticoid signal abnormality, and shows a novel action mode at molecular and cellular levels. In diabetes, obesity, lipid metabolism disorder and related complication models, the compound can reduce blood sugar, improve insulin sensitivity, regulate blood fat and relieve inflammation, and shows a good treatment prospect. The half degradation concentration of a representative compound in vitro is about 1000 nM, and feasible degradation efficiency is achieved. The compound can be synthesized by Click chemistry and other methods, and can be prepared into a pharmaceutical composition for prevention and treatment of type II diabetes, metabolic syndrome, polycystic ovarian syndrome and other diseases, and a new strategy is provided for research and development of related drugs.
Owner:BEIJING DIABETES RES INST (BEIJING DIABETES PREVENTION & CONTROL OFFICE)