83 results about "Competitive binding" patented technology

The invention discloses a method for restoring soil heavy metal pollution by coupling soybean urease with a charcoal cementing agent, and relates to the technical field of soil heavy metal pollution restoration, and the method comprises the following steps: dynamic microbiome regulation and control: introducing photosensitive protein into soil functional bacteria; the acyl homoserine lactone analogue is synthesized and applied to soil, and is competitively combined with a microbial quorum sensing receptor to block an inhibitor to secrete a signal channel; according to the method, microbial urease secretion is regulated and controlled through optogenetics, an inhibitor signal is blocked through quorum sensing interference, and a microbiome is precisely regulated and controlled; the pH-responsive nanocapsule releases an inhibitor in a targeted manner, and the magnetic-responsive nanochain dynamically captures interfering bacteria, so that the limitation of passive adsorption is broken through; the gene editing plant releases coumarin to inhibit fungal metabolism, and the engineering mycorrhizal fungi physically shields an inhibitor to construct cross-biosphere cooperative defense; the urease activity and the heavy metal removal rate are remarkably improved, meanwhile, the soil microbial diversity is maintained, and the soil specificity interference problem is solved.

The invention discloses an antibody for detecting indol sulfate, a detection kit and application of the antibody, and the antibody can be specifically combined with indol sulfate and has high combination activity. The detection kit detects the content of indoxyl sulfate in a to-be-detected sample through a competitive binding reaction of an immunomagnetic bead coated indoxyl sulfate antibody, an antigen in the sample and an alkaline phosphatase labeled indoxyl sulfate antigen, and has important economic value and social significance.

The invention provides a method for analyzing interaction between procambarus clarkia arginine kinase and shark source nano antibody. The method comprises the following steps: performing three-dimensional structure prediction on a VNAR sequence, and screening a high-confidence VNAR model by using a Laplace map; docking an amino acid sequence corresponding to the VNAR model with an arginine kinase sequence to obtain an optimal compound model, and analyzing an interaction site of an arginine kinase epitope region and a nanometer antibody complementary determining region CDR3; performing molecular dynamics simulation on the compound model, calculating conformational change indexes and binding free energy through energy optimization, system balance and extended simulation sampling, and outputting a binding stability sequence of the nano antibody and arginine kinase; the method comprises the following steps: screening out a high-stability nano antibody, pre-incubating a fusion protein of the high-stability nano antibody and immobilized arginine kinase to form a compound, adding serum of an allergic patient for competitive binding, quantifying the binding activity of residual IgE through an immunodetection technology, and verifying the inhibition effect of the shark source nano antibody on the sensitization effect of arginine kinase.

The invention belongs to the technical field of pharmacotherapeutics, and particularly relates to application of theaflavin-3 '-gallate and a medicine prepared from theaflavin-3'-gallate. The theaflavin-3 '-gallate is used as a KEAP1-NRF2 inhibitor and is competitively combined with the KEAP1 to destroy the inhibition effect of the KEAP1 on the NRF2, so that the content of the NRF2 is increased, and the expression of downstream NQO1 and GCLC is improved. Besides, the theaflavin-3 '-gallate protects the liver function by inhibiting the increase of the contents of AST and ALT, and reduces the oxidative stress and lipid accumulation of the liver, so that the theaflavin-3'-gallate has the potential to become a medicine for treating the ethanol-induced liver injury.

The present application relates to an antigen-binding protein and use thereof, and specifically relates to an antigen-binding protein capable of inhibiting competitive binding of IGF-IR to ligands thereof with an IC50 value of about 1.0 μg / mL or less in a competitive ELISA.

The invention discloses an application of a Brazilian strongylus FAR-1 protein as an anti-nematode drug target. A fluorescent ligand competitive binding experiment shows that the Japanese strongylus Brazil FAR-1 protein has the capability of binding various fatty acids and retinol; the Nbfar-1 gene is in high expression in the whole development stage of the Brazilian strongylus; nbfar-1 gene expression is inhibited through RNAi, the lipid content of larvae can be reduced, the adult egg laying rate, the egg hatching rate, larva development and adult epidermis formation are affected, and therefore growth and development of Brazilian strongylus are remarkably affected. Therefore, the Brazilian circular nematode FAR-1 protein can be used as a drug target for screening or identifying anti-parasitic nematode drugs, a method is provided for development of the anti-parasitic nematode drugs, and the Brazilian circular nematode FAR-1 protein has important significance on prevention and treatment of infection of parasitic nematodes.

The invention relates to the fields of pharmacology and molecular biology, and discloses an autophagy inhibitory polypeptide competitively combined with an LIR docking site of an autophagy-related protein LC3 and application of the autophagy inhibitory polypeptide. Through molecular docking simulation, through LIR docking sites of targeted LC3 protein, 794 bioactive polypeptides which can be combined are screened out. Functional result analysis shows that peptide 3 #, peptide 4 # and peptide 5 # are competitively combined with LIR docking sites of the LC3 protein, so that formation of autophagy vesicles is inhibited in a targeted manner, and proliferation and survival of autophagy-dependent pancreatic cancer cells are effectively inhibited; the strategy is combined with chemotherapeutic drugs to show a synergistic effect, and the pancreatic cancer resisting curative effect is remarkably enhanced.

The present invention belongs to the field of biomedicine technology, and relates to small molecule inhibitors and preparation methods and their applications in the preparation of anticancer drugs. Its chemical structural formula is shown in formula (I), and the small molecule inhibitors provided by the present invention have good competitive affinity for the β-catenin / BCL9 target, and can be tightly bound to the target, and have a strong ability to competitively bind to destroy the β-catenin / BCL9 complex. Among them, some small molecule inhibitors have excellent inhibitory effects on the expression of the target gene Axin and better biological activity.

The invention discloses a label-free proportional type luminous aptamer biosensor for staphylococcus aureus enterotoxin A (SEA). The label-free proportional type luminous aptamer biosensor comprises the following steps: (1) advanced evolution screening of a complex matrix high-adaptability aptamer; (2) rationally cutting the aptamer assisted by computer simulation; (3) a construction strategy of the label-free proportional biosensor; (4) a label-free proportional SEA bifunctional biosensor sequence; (5) optimizing conditions of the label-free proportional SEA biosensor; and (6) SEA detection. The design principle is that fluorescence of SEA and ThT is excited to different degrees on the basis of a competitive binding effect between an SEA target and a small molecule nucleic acid dye thioflavin T (ThT) as well as a luminous nucleic acid aptamer, so that the ratio of fluorescence signals of the SEA and the ThT is in a linear relationship with the target concentration, and finally, rapid, label-free and low-cost proportional fluorescence detection of the SEA is realized.

The invention provides an intelligent drug interaction prediction method and system based on a knowledge graph, and relates to the technical field of medical information, and the method comprises the steps: extracting drug molecular structure and metabolic data, calculating the conformation overlapping degree, determining a metabolic pathway overlapping site, calculating the competitive binding probability, analyzing the drug distribution state, and judging a metabolic cycle overlapping interval. Determining a concentration accumulation range, evaluating a metabolic inhibition level, generating early warning data and updating the knowledge graph. The drug interaction can be accurately predicted, the medication safety is improved, and the adverse reaction risk is reduced.

A method for identifying an aptamer suitable for use in an electrochemical sensor for sensing a target analyte. The method includes determining whether the target analyte competitively binds with the analyte recognition element. Competitive binding in favour of the target analyte is indicative of the suitability of the aptamer.

The invention discloses application of inhibiting combination of Hic-5 and SMAD7 and / or inhibiting Hic-5 in treatment of pulmonary arterial hypertension, and finds that PLEKHH2 and SMAD7 have competitive combination with Hic-5 protein in lung tissue, more SMAD7 can be released into cytoplasm by preventing combination of Hic-5 and SMAD7, and SMAD2 / 3 phosphorylation is inhibited for the first time, so that the purpose of treating the pulmonary arterial hypertension is achieved. The invention provides a new research and development direction for the development of pulmonary arterial hypertension treatment medicines.

This invention provides a monoclonal antibody 6D11 and its applications. The CDR amino acid sequence of the heavy chain of the anti-monoclonal antibody 6D11 is shown in SEQ ID No. 1, and the CDR amino acid sequence of the light chain is shown in SEQ ID No. 2. This invention also provides the application of monoclonal antibody 6D11 in the preparation of drugs for treating dengue virus infection. The monoclonal antibody 6D11 of this invention has advantages such as competitive binding to DENV1-4NS1 protein, inhibition of vascular leakage symptoms, and protection against lethal damage from DENV infection in vivo, and has significant potential therapeutic value against dengue virus.

The application discloses a preparation method and application of an amphiphilic tyrosinase copper competitive binding agent. Two new compounds P4TA or P2TA are synthesized by coupling tyramine TA with 4,4',4'',4'''-(porphyrin-5,10,15,20-tetrayl) tetrakisbenzoic acid TCPP or 3,7,12,17-tetramethyl-8,13-diethyl-2,18-porphyrin dipropionic acid PPIX. An optimal synthesis process of P4TA and P2TA is provided, and an experience is provided for related synthesis. The obtained P4TA and P2TA can recognize tyrosinase and are good copper ion binding reagents, and the two compounds exhibit a significant inhibitory effect on TYR. The application can be used for tyrosinase targeted inhibition and copper ion metabolism intervention in biological medicines and food.

The invention provides a screening method of a targeted Nedd4-2 intermediary hERG potassium channel degradation small-molecule inhibitor and the inhibitor thereof. According to the invention, through a molecular docking virtual screening technology, cell culture, plasmid transfection, an FLIPR ion channel screening technology, a Western Blot technology and a patch clamp technology, a method for high-throughput screening of a targeted Nedd4-2 intermediate hERG potassium channel degradation small molecule inhibitor is established. The screened compound LACCAIC ACID A (number 17) can reduce the degradation of hERG potassium channel on the basis of overexpression of Nedd4-2, increase Ikr current, obviously antagonize the extension of repolarization time history caused by ET-1, and reduce the occurrence rate of cell arrhythmia. The results show that the LACCAIC ACID A compound obtained by the screening method is competitively combined with the PY sequence of the hERG channel with Nedd4-2, so that the ubiquitination degradation of the hERG channel by the Nedd4-2 is reduced, and a research and development basis is provided for further developing hERG potassium channel degradation prevention and treatment drugs.

The invention discloses a compound and application thereof. The invention provides a series of novel compounds with chemical structures reported for the first time. An activity research result shows that the series of novel compounds can competitively inhibit the combination of a natural substrate simulant of an SH2 substructural domain in a Cbl-b TKB structural domain and the SH2 substructural domain in the Cbl-b TKB structural domain. The competitive inhibition effect of the series of novel compounds can reduce the function of the Cbl-b protein, so that the continuous activation of T cells can be caused, and the tumor removal capability mediated by the T cells can be enhanced. Therefore, the series of novel compounds have the prospect of being developed into antitumor drugs. In addition, the series of novel compounds can also be developed into a reagent which is competitively combined with the SH2 substructural domain in the Cbl-b TKB structural domain, and the effect of the reagent includes but is not limited to a competitive inhibitor reference substance of the SH2 substructural domain in the Cbl-b TKB structural domain.

The application discloses a ricin toxin detection sensor based on competitive binding of ricin to mitochondrial adenine nucleotide translocator (ANT) and a detection method, which comprises ANT protein, hollow dialysis fiber, chemical cross-linking agent and fluorescently labeled ATP. When in use, the ANT is first fixed on the inner wall of the hollow fiber dialysis membrane and the fluorescently labeled ATP (cy5-12-ATP or cy3-12-ATP or DEPC-12-ATP) is added; then, it is placed in the to-be-detected solution for 30-60 seconds, and then is placed under a fluorescence detection instrument (such as a fluorescence microscope) for observation, so that the presence or absence of the ricin toxin and the approximate concentration of the toxin are determined; then, the relative intensity of the fluorescence of the to-be-detected solution is determined; a standard curve of the corresponding relationship between the concentration of the fluorescent group and the concentration of the toxin is established; and the concentration of the ricin toxin in the to-be-detected solution is obtained by substituting the concentration of the fluorescent group of the to-be-detected solution into the above standard curve and performing calculation. The application can effectively improve the detection efficiency, simplify the detection method and be widely applied in the society.

The invention discloses an application of long-chain non-coding RNA (Ribonucleic Acid) Cslnc256 in regulating and controlling an anti-colletotrichum gloeosporioides posttranscriptional mechanism of a tea tree. According to the application of the long-chain non-coding RNA Cslnc256 in regulating and controlling the colletotrichum gloeosporioides resisting post-transcription mechanism of the tea tree, the long-chain non-coding RNA Cslnc256 can accurately act on Cslnc256-CsmiR395-CsSultr2 in the tea tree body; therefore, the defense mechanism of the plant is efficiently activated. When the expression of the Cslnc256 is inhibited, the competitive binding capacity of the Cslnc256 and the CsmiR395 is reduced, so that the concentration of the free CsmiR395 is increased, and further, the activity of the Cslnc256 on the target gene CsSultr2; 1 is an inhibitory effect. The regulation and control process can reduce the activity of sulfate transporter protein in the tea tree body, so that sulfate ions are accumulated in leaves, and the sulfate ions serving as important defense signal molecules can effectively improve the resistance of the tea tree to colletotrichum gloeosporioides and relieve scab expansion and tissue damage caused by pathogenic bacterium infection.

The application discloses a competitive binding method for evaluating the interaction between trypsin and flavonoids, wherein the interaction between different flavonoids and trypsin is analyzed by means of electrospray ionization mass spectrometry (ESI-MS) in a competitive mode of mass spectrometry; the parameter R can be introduced to compare the relative strength of the affinity, to judge whether the different flavonoids compete with each other in the binding to trypsin, and to further infer whether the binding sites of the different flavonoids on trypsin are the same; the method is simple, fast and high in accuracy, and can provide a feasible scheme for rapidly screening trypsin inhibitors.

The present invention relates to a bispecific fusion protein targeting TNF-α and IL-17A, a polynucleotide encoding the same, a method for preparing the same, and uses thereof. The bispecific fusion protein targeting TNF-α and IL-17A is a dimer with a symmetric structure and contains, from the N-terminus to the C-terminus, three structural functional regions: a soluble TNF receptor or a portion thereof, a human IgG Fc fragment, and a functional domain that competitively binds to IL-17A or an anti-IL-17A domain. The fusion protein can effectively bind to both TNF-α and IL-17A and has the effect of blocking their signaling pathways. The fusion protein has good stability, specificity, and biological activity.

The present invention is applicable to the field of biomedicine and provides the use of lncRNA MCM3AP-AS1 as a biomarker and therapeutic target for diabetic cardiomyopathy. The present invention reveals the mechanism of action of the long noncoding RNA (lncRNA) MCM3AP-AS1 in diabetic cardiomyopathy (DCM). Bioinformatics screening revealed that MCM3AP-AS1 is significantly downregulated in DCM. It can act as a competitive endogenous RNA (ceRNA) to competitively bind to miR-155-5p, targeting the miR-155-5p / DHCR24 axis and promoting the expression of DHCR24 (24-dehydrocholesterol reductase), thereby enzymatically hydrolyzing H₂O₂ and alleviating oxidative stress and apoptosis in cardiomyocytes. This mechanism makes MCM3AP-AS1 a biomarker with diagnostic and therapeutic potential, providing a new target and theoretical basis for the clinical diagnosis and treatment of DCM.

The invention discloses a DNA (Deoxyribose Nucleic Acid) probe ATP-3 and application thereof. The DNA (Deoxyribose Nucleic Acid) probe ATP-3 disclosed by the invention comprises DOX-3 and DOX-3-CP (Chlorinated Drug detection can be realized by using the DNA probe ATP-3 based on a non-label method DNA biosensor. Based on a double-strand competitive binding mechanism (DOX-3 and DOX specific binding leads to double-strand dissociation) of a DNA probe ATP-3, and in combination with a fluorescence switching characteristic (fluorescence enhancement during double-strand binding and quenching during dissociation) of an embedded fluorescent agent DAPI, trace detection of drugs is realized. By using a fluorospectro photometer as a detection auxiliary instrument, the method has the advantages of sensitive result, simplicity in operation, lower cost and the like.

The invention relates to the technical field of pharmaceutical preparations, and discloses a doxorubicin and cyclophosphamide liposome compound injection which is prepared from doxorubicin hydrochloride, cyclophosphamide, hydrogenated soybean phosphatidylcholine, cholesterol, polyethylene glycol derivative phospholipid, anhydrous magnesium sulfate, L-arginine and a sucrose octasulfate ammonium solution. Magnesium ions introduced into an inner water phase participate in competitive binding, doxorubicin and sucrose octasulfate are induced to form a loose co-precipitation structure with lattice defects, hydrophilic cyclophosphamide is physically filled and cured by using micro gaps, and efficient encapsulation of non-gradient dependent drugs is realized. Meanwhile, an in-situ pH buffer system is constructed by using L-arginine, protons generated in a drug loading process are neutralized, an internal water phase is maintained in a neutral environment, and acid-catalyzed hydrolysis of cyclophosphamide is effectively inhibited. According to the invention, the double-drug encapsulation efficiency and storage stability of the compound liposome are obviously improved.

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.

The application discloses a method for screening multifunctional peptides of perilla albumin source for treating diabetes and hypertension, which comprises the following steps: obtaining perilla albumin sequence, predicting the potential of perilla albumin as DPP-Ⅳ and ACE inhibitory peptide source, performing computer simulation digestion, and screening DPP-Ⅳ and ACE inhibitory peptides. Through the bioactive peptide database BIOPEP-UWM, 40 perilla albumin sequences are predicted for active fragments, and it is found that perilla albumin is rich in a large number of fragments with DPP-Ⅳ and ACE inhibitory activity. Perilla albumin is subjected to computer simulation digestion, polypeptides capable of resisting gastrointestinal digestion are obtained, and perilla albumin source multifunctional peptides with DPP-Ⅳ and ACE inhibitory activity are screened through related activity prediction and molecular docking. The practicability of the multifunctional peptides is predicted, and two multifunctional peptides without toxicity, allergenicity, bitterness and hemolytic activity, namely CDAF and CCAL, are screened. The two multifunctional peptides inhibit the catalytic activity of DPP-Ⅳ and ACE by competitively combining with the active centers of DPP-Ⅳ and ACE, so as to play the roles of reducing blood sugar and blood pressure.

The present invention provides antibodies that specifically bind to FGFR3, as well as methods for treating or preventing cancer, such as bladder cancer. Also provided herein are isolated antibodies or antigen-binding fragments thereof that specifically bind to FGFR3 or its antigen-binding fragments, which bind to the same FGFR3 epitope as the antibodies or antigen-binding fragments described herein or compete for binding to FGFR3. The present invention also provides complexes comprising such antibodies or antigen-binding fragments bound to FGFR3 or its antigen-binding fragments, which are also part of the present invention.

The invention belongs to the technical field of oligopeptide pharmacology, and particularly discloses a Maged1 competitive oligopeptide and application thereof. The Maged1 competitive short peptide is a short peptide MP1 or a short peptide MP2, and the amino acid sequence of the Maged1 competitive short peptide is as shown in SEQ ID No. 1 or SEQ ID No. 2. Experiments prove that the Maged1 competitive oligopeptide and Maged1 can be competitively combined with a P2X3 receptor, so that activation of the Maged1 on the P2X3 receptor is inhibited, and the Maged1 competitive oligopeptide has a good clinical application prospect in treatment of chronic pain.

A computer-implemented framework for designing high-efficiency and high-specificity nucleic acid molecules targeting transfer RNA (tRNA) and its derivatives (tDRs). The framework comprises two primary algorithms. The first, tBOND-G, designs guide RNAs (gRNAs) for Cas13-mediated tRNA cleavage by calculating physical parameters, including target site accessibility and binding energy, and processing them through a Support Vector Machine (SVM) model to predict cleavage efficiency. The second algorithm, tBOND-L, designs therapeutic Locked Nucleic Acid-modified antisense oligonucleotides (LNA-ASOs) that specifically target a tDR without binding to its parent tRNA. This method utilizes a processor to derive an efficiency score based on relative binding affinity and a specificity score based on simulated competitive binding environments.

The invention relates to a radiolabeled Exendin-4 polypeptide probe precursor and application thereof, and belongs to the technical field of radiopharmaceutical chemistry and nuclear medicine diagnosis and treatment. The radioactive labeled Exendin-4 polypeptide probe precursor is R-HBED-CC-PEGn-Exendin-4, the general formula structure of the radioactive labeled Exendin-4 polypeptide probe precursor is shown in the specification, and n is equal to 3, 6 or 12; r is-OH or PEG chains with different lengths are introduced into R-HBED-CC-Exendin-4 to modify the medicine, so that the pharmacokinetics of the medicine is changed. Through a radionuclide labeling experiment, an in-vitro cell uptake experiment, an in-vitro receptor competitive binding experiment, biological distribution, model mouse imaging and other experiments, the targeting and in-vivo metabolism level of the novel probe are explored. And a novel targeted GLP-1R diagnosis and treatment drug with a clinical application prospect is screened out.

The invention provides an aptamer colorimetric sensor based on Au (at) Ce MOF and a preparation method and application thereof, the aptamer colorimetric sensor comprises a signal probe and a capture probe, the signal probe is obtained by mixed incubation of activated cDNA and Au (at) Ce MOF, and the capture probe is obtained by co-incubation of streptavidin modified magnetic beads and an aptamer. According to the aptamer colorimetric sensor based on Au-Ce MOF, Au-Ce MOF with high oxidase-like activity is synthesized on Ce MOF through a chemical reduction method, a rapid colorimetric aptamer sensor is developed on the basis of the competitive binding principle of MB-Apt, and the aptamer sensor is used for efficiently detecting DON and Au-Ce MOF-cDNA and target specificity, so that the aptamer colorimetric sensor has the advantages of high recovery rate, low detection limit and excellent anti-interference capability, and the sensor can be used for detecting DON and Au-Ce MOF-cDNA and target specificity. The huge practical application potential is realized in the aspect of detecting DON pollution in a food matrix.