54 results about "Tubulin" patented technology

The invention discloses a tumor treatment molecule with a curative effect self-amplification function. Belongs to the technical field of biotechnology and new medicine, and comprises a peptide sequence Ac-Asp-Glu-Val-Asp-Cys (StBu)-Lys combined to a CBT part and a paclitaxel chemotherapy molecule connected to a lysine side chain. After the probe enters a tumor cell, the probe is specifically recognized by reducing glutathione highly expressed in the tumor cell, and an Ac-DEVDCK (PTX)-CBT structure is generated; then, a weak cell apoptosis phenomenon is initiated through a molecular grafted paclitaxel structure; the Ac-DEVD fragment is used as a high-specificity polypeptide substrate of cysteine-aspartic acid specific protease 3 which is necessary in a cell apoptosis pathway, and can be specifically cut by the cysteine-aspartic acid specific protease 3, so that the Ac-DEVDCK (PTX)-CBT is converted into CK (PTX)-CBT; then, CK (PTX)-CBT molecules are subjected to a CBT-Cys click reaction to form a cyclic dimer, and the cyclic dimer is self-assembled to form particles. According to the method, the affinity of the paclitaxel to the tubulin in the cytoskeleton is utilized, so that the tubulin in the cell is aggregated, the self-amplification effect of the curative effect of the cell is realized, and the cell is triggered to generate a pan-apoptosis effect.

The present disclosure relates to compositions for increasing acetylated alpha-tubulin levels in peripheral neuronal cells. The present disclosure also relates to the use of tubulin deacetylase inhibitors, or activators of tubulin acetylation for increasing acetylated tubulin levels in the cells. The present disclosure also relates to methods for assessing risk of developing peripheral neuropathy by assessing the levels of acetylated alpha-tubulin. The present disclosure further relates to methods for treating a subject suffering from a peripheral neuropathy using the compositions described herein.

Novel and useful compounds, such as 2,4-dihydropyrazolo[3',4':4,5]pyrano[2,3-b]pyridines, are disclosed herein. Such compounds may be employed in various treatments, alleviation, or prevention of a group of disorders, such as disorders associated with Tau (tubulin associated unit) protein aggregates, such as neurofibrillary tangles (NFTs), such as Alzheimer's disease (AD).

The invention discloses a polycyclic compound as a tubulin stabilizer and a preparation method thereof, the structure of the polycyclic compound is shown in a general formula (I), and the definitions of Ar, W, Z, X, Y and heterocyclic ring A are shown in the specification. The invention also discloses a preparation method of the compound. The compound shown in the general formula (I) can be used for preparing medicines for preventing and / or treating tumors and neurodegenerative diseases. # imgabs0 #

Compounds comprising an amide-linked coumarin scaffold, compositions comprising same, and method of using such compounds and compositions to inhibit tubulin-associated unit (tau) protein aggregation or alpha-synuclein ( α-syn) protein aggregation in a subject having, or at risk for, tau protein aggregation or α-syn protein aggregation, respectively.

The present invention relates to biological detection technology, and discloses a biosensor and its application and a method for high-throughput screening of zingerone-producing bacteria. The biosensor contains a first sensing element and a second sensing element, wherein the first sensing element contains α-tubulin and a first signal protein expressed by fusion with the α-tubulin, and the second sensing element contains β-tubulin and a second signal protein expressed by fusion with the β-tubulin; the end of one of the first signal protein and the second signal protein is the N-terminus and the end of the other is the C-terminus, and the first signal protein and the second signal protein can be combined to form a reporter signal. The biosensor can couple zingerone with a fluorescent signal, efficiently and accurately respond to the concentration of zingerone, and realize high-throughput screening of the intracellular product zingerone in microorganisms.

The invention discloses application of human dental pulp stem cells in enhancing neurogenesis in a brain region and treating neurodegenerative diseases, including stem cells for enhancing neurogenesis of adult hippocampus, and the human dental pulp stem cells have the following functional characteristics: flow cytometry detection shows that the Netin positive rate is not lower than 90%, and the beta-tubulin III positive rate is not lower than 85%; in a conditioned culture medium after in-vitro culture for 24 hours, the secretion amount of BDNF reaches more than 500pg / mL / 106 cells, and the secretion amount of GDNF reaches more than 200pg / mL / 106 cells; the alizarin red dyeing positive area accounts for not less than 60% after osteogenesis induction, and the oil red O dyeing positive area accounts for not less than 50% after adipogenesis induction; according to the quantitative standard that the number of dentate gyrus DCX + newborn neurons of the adult hippocampus is increased by more than 50% compared with that before treatment, the dual-mechanism targeted therapy 1 specifically activates hippocampus neural stem cells and promotes newborn neurons to differentiate by highly expressing neural markers and secreting neurotrophic factors, so that the neurogenesis of the adult hippocampus is enhanced, and the neurogenesis of the adult hippocampus is enhanced. Meanwhile, A beta deposition and p-Tau phosphorylation are reduced.

Disclosed are compositions and / or methods of use of the compositions for patients with neuronal diseases such as AD, Parkinson's, Huntington's, multiple sclerosis, and ALS. In certain embodiments flavonoids alone, or in a pharmaceutical preparation, are administered through the nasal olfactory route. In certain embodiments the flavonoid is apigenin and the neural disease is Alzheimer's. In some embodiments a porosome complex is administered for reconstitution into a neural cell. In certain embodiments, a co-administered blood-brain barrier traversing peptide is configured as a mimic of a domain of ATP 1 A3 and / or Tubulin.

A determination has been made that apicomplexan tubulin, an essential parasite component, is an excellent drug target. Here, it is shown that it is possible to specifically target parasite tubulins, without harming the mammalian host. A compound has been identified that destabilizes specifically parasite MTs and inhibits essential parasite processes of replication and host cell invasion. This provides a new strategy to tackle the issue of drug resistance development. Specifically, the use of the compound parabulin and / or its derivates in the process of targeting protozoan tubulin for the inhibition of the replication of protozoans in mammalian organism, wherein parabulin has the following molecular weight, sum formula, name and structure:MW: 373.4 Da;Formula: C20H23NO6, ⋅Name (s): 3-(3,4-dimethoxyphenyl)-N-[(3,4,5-trimethoxyphenyl)methyl]prop-2-enamide; (2E)-3-(3,4-Dimethoxyphenyl)-N-(3,4,5-trimethoxyphenyl)acrylamid;SMILES:0(C1═C(OC)C═CC(═C1)C═CC(═0)N(CC2═CC(═C(OC)C(═C2)OC)OC)[H])C.

The application discloses a class of podophyllotoxin triazole ether derivatives, a preparation method and application thereof, belongs to the technical field of chemical pharmacy, and particularly relates to a class of podophyllotoxin triazole derivatives and application thereof in preparation of antitumor drugs. The application combines a triazole structure with a podophyllotoxin parent body by using a click chemistry reaction, designs and synthesizes a series of novel 1,2,3-triazole podophyllotoxin derivatives, optimizes the kinetic characteristics of the podophyllotoxin by introducing the triazole structure, and improves the anticancer effect and drug property. Molecular docking shows that the series of compounds have strong binding energy on AKT1 and tubulin, can target inhibit tubulin / AKT1, and in-vitro antitumor activity research shows that the molecules have strong inhibitory activity on the proliferation of human colon cancer cell strains, and can provide a new strategy for structural derivatization of podophyllotoxin.

The application discloses an Aspergillus luchuensis YZ-1 and application thereof, and belongs to the field of microorganism safety.The application separates a new strain from a black tea in Guilin, Guangxi, identifies the strain by ITS, beta tubulin and calmodulin, and the identification result is Aspergillus luchuensis, and the preservation number is CCTCC NO: M 20221462.It is verified by experiments that the strain can inhibit various bacteria and fungi, the water extract and fermentation liquor of the strain can significantly inhibit the growth of Aspergillus flavus, the fermentation liquor has a strong inhibiting effect on the growth of Aspergillus flavus, and the strain has a strong adsorbing effect on aflatoxin B1.Therefore, the Aspergillus luchuensis disclosed by the application has important application value in preventing and controlling mold pollution in grain crops and food.

The invention discloses a specific PCR (Polymerase Chain Reaction) detection primer TKF10 / TKR10 of Karst colletotrichum gloeosporioides and an application of the specific PCR detection primer TKF10 / Wherein the sensitivity of primers TKF10: 5 '-GCGGGGCTAACTCTGAAT-3' and TKR10: 5 '-CGCCAGAGATGTTTGCCTG-3' based on a TUB2 (beta-tubulin) gene is 1 ng * [mu] L <-1 >, and the sensitivity of the primers TKF10: 5 '-GCGGGGCTAACTCTGAAT-3' and TKR10: 5 '-CGCCAGAGATGTTTGCCTG-3' based on the TUB2 (beta-tubulin) gene is 1 ng * [ Research results show that the pair of primers can efficiently and specifically detect the Karst colletotrichum in the mango leaves, and a reliable technical tool is provided for early diagnosis of mango anthracnose, analysis of a disease occurrence rule and construction of a precise prevention and control strategy.

The invention relates to the cross technical field of molecular biology and parasitology, and particularly discloses a giardia living body marking method based on fluorescent protein UnaG, which comprises the following steps: firstly, optimizing and synthesizing a UnaG gene sequence according to the codon use preference of giardia; then, constructing a marker plasmid pGT-UnaG-neo on a double expression framework containing an alpha2-tubulin promoter and a gdh promoter, and introducing the plasmid into the giardia giardia trophozoite through electroporation. And carrying out resistance screening in a culture medium containing geneticin to obtain an insect strain capable of stably integrating and expressing UnaG. Through bilirubin induction, efficient maturation and green fluorescence emission of the UnaG protein in giardia cytoplasm are realized. The stably transferred strain obtained by the method has no significant difference from a wild strain in the aspects of growth curve and survival rate, and UnaG and bilirubin have no obvious toxic effect. The limitation that traditional fluorescent protein is inactivated under the anaerobic condition is broken through, and a reliable tool is provided for dynamic imaging, functional research and drug screening of giardia and other anaerobic protozoa.

The application relates to the technical field of medicines, and discloses a 4-methyl quinazoline PI3K-Tubulin dual-target inhibitor and a preparation method and application thereof. Specifically disclosed are a PI3K-Tubulin dual-target inhibitor compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition and preparation containing the compound or the pharmaceutically acceptable salt thereof, a method for preparing the compound or the pharmaceutically acceptable salt thereof, and application of the compound or the pharmaceutically acceptable salt thereof in preparing medicines for treating and / or preventing diseases mediated by PI3K-Tubulin and related diseases.

The invention belongs to the technical field of plant molecular biology, and particularly discloses a diatom RNA extraction method and a method for evaluating influence of pollutants on diatom gene expression. The invention firstly provides a diatom RNA extraction method, RNA is extracted by virtue of a cell homogenate physical crushing method and according to an improved TRIzol method, the release amount of RNA is high, and the purity reaches the standard. The invention also provides a method for evaluating the influence of pollutants on gene expression of diatom, which is based on the diatom RNA extraction method, takes Tubulin as a reference gene, takes one or more of iron redox protein, ferrithionein, ketoacyl coenzyme A thiolase, ethanol dehydrogenase, lipoprotein and acetyl coenzyme A carboxylase as target genes, and evaluates the influence of pollutants on gene expression of diatom. The relative expression level of a target gene is detected through qPCR and can be used for evaluating the acute toxicity of pollutants. The method effectively solves the problems that diatom RNA is difficult to extract, the diatom gene expression level is difficult to detect through qPCR, and the molecular mechanism of pollutant action is difficult to evaluate.

A formulation of conjugates of tubulysin analogs with a cell-binding molecule having a structure represented by Formula (I), wherein T, L, m, n, , R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 are as defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.

The invention discloses application of polypeptide in preparation of a diabetic nephropathy alleviator, and belongs to the technical field of medicines. The cordyceps sinensis beta-tubulin polypeptide is synthesized by analyzing the structure of the cordyceps sinensis beta-tubulin and selecting amino acid peptide fragments from the 84th site to the 107th site. The apoptosis of the glomerular mesangial cells is induced by using 50 mmol / L of glucose, and meanwhile, the apoptosis of the glomerular mesangial cells induced by high glucose can be relieved by adding the cordyceps sinensis beta-tubulin polypeptide. A treatment test of the cordyceps sinensis beta-tubulin polypeptide on diabetic nephropathy model mice shows that the body mass and fasting blood-glucose levels of the mice in the cordyceps sinensis beta-tubulin polypeptide group are remarkably reduced, the 24-hour urine protein content of the mice is remarkably reduced, and the kidney injury of the mice in the cordyceps sinensis beta-tubulin polypeptide group is remarkably relieved.

The invention discloses a multifunctional nanoprobe for lung cancer drug resistance diagnosis and treatment and a preparation method and application thereof, and relates to the technical field of DNA nanoprobes, the multifunctional nanoprobe comprises a Y-shaped structure formed by self-assembly of three nucleic acid chains S1, S2 and S3 and PTX, the Y-shaped structure and PTX are self-assembled to form a spherical structure, and the particle size of the spherical structure is 80-120nm; the S1 nucleic acid chain is loaded with an anti-ABCB1 sequence, is modified with a Cy5 fluorophore and is subjected to fluoro modification treatment; the S2 nucleic acid chain is loaded with an S6 sequence of a targeted A549 cell membrane surface specific structure; and the S3 nucleic acid chain is loaded with an anti-beta III-tubulin sequence. By integrating multiple functions of targeting recognition, gene silencing and chemotherapy drug delivery, diagnosis and treatment integration of the paclitaxel drug-resistant lung cancer is realized.

The present invention relates to a method for detecting a 217-phosphorylated tubulin fragment on the basis of a chemical derivatization method, and the use thereof. The detection method comprises the following steps: S1, adding TMPP-Ac-OSu and a triethylamine solution to a p-Tau 217 solution, mixing same and then performing a derivatization reaction, and then adding an aqueous ammonia solution to perform a quenching reaction so as to obtain a sample solution; and S2, performing LC-MS / MS detection on the sample solution. In the present invention, TMPP-Ac-OSu is innovatively utilized to perform a specific chemical derivatization reaction with p-Tau 217, such that the signal intensity of the resulting chemical derivatization product is significantly enhanced, and the detection capability is improved. Analysis can be performed under Vanquish UHPLC liquid phase conditions, and paired with a more cost-effective TSQ AltisTM Triple Quadrupole instrument, thereby greatly reducing the detection costs. Moreover, the method involves short time consumption and thus can be used for rapid extraction of a large number of samples. The detection method of the present invention is of great significance for the early detection of Alzheimer's disease.

The application belongs to the technical field of medicine, and particularly relates to application of a beta-lactam compound in preparation of anti-inflammatory drugs. The application is found through research and verified through experiments that the beta-lactam compound is combined with the surface of alpha and beta tubulin proteins, inhibits tubulin aggregation, and thus inhibits various cell processes in which microtubules participate; the beta-lactam compound inhibits inflammatory reactions through the following pathways: inhibiting immune activation, NLRP3 inflammasome activation and Caspase-1 activation; inhibiting neutrophil recruitment, adhesion and chemokine release; inhibiting vascular endothelial growth factor secretion and endothelial cell proliferation, and thus can be used for preparing anti-inflammatory drugs, including for treating local inflammatory reaction diseases such as acute gout, familial Mediterranean fever, chronic kidney disease, pancreatitis, sarcopenia and the like caused by inflammation, and inflammation-related cardiovascular diseases such as ischemia-reperfusion injury, diabetes, atherosclerosis, pericarditis, acute coronary syndrome and the like.

To provide a pharmaceutical composition of a conjugate of a tubulysin analog and a cell surface binding ligand for longer stability and storage as well as easier shipment.SOLUTION: Provided is a pharmaceutical composition that is a liquid composition prior to lyophilization, or in a formulated lyophilized solid, or the re-constituted formulation from the lyophilized solid, comprising the following compositions: a conjugate of a tubulysin analog to a cell-binding agent of Formula (I); a polyol selected from sucrose or trehalose; a surfactant selected from polysorbates; 1 or more preservatives; 1 or more amino acids; 1 or more antioxidants; one or more metal chelating agents; one or more buffer salts to adjust the pH of the formulation from pH 4.5 to 8.5; and one or more of isotonic agent for adjusting osmotic pressure between about 250 to 350 mOsm after reconstituted for administration to a patient.SELECTED DRAWING: None

The invention discloses an application of isosteviol containing a hydroxamic acid group and a steviol derivative in nerve injury protection, relates to the field of nerve injury protection medicines, and aims to provide an HDAC6 inhibitor capable of improving nerve dysfunction. Isosteviol and steviol derivatives containing hydroxamic acid groups are applied in the field of nerve injury protection, especially in the treatment of neurodegenerative diseases. The isosteviol and the steviol derivative containing the hydroxamic acid group enhance the antioxidant defense capability of cells and reduce oxidative stress induced cell apoptosis by regulating and controlling an Nrf2 / HO-1 signal channel, a Bcl2 / Bax signal axis and an HDAC6 / Ac-Tubulin microtubule stabilizing signal axis, so that the neuroprotective effect is achieved. Important theoretical support is provided for development of tetracyclic diterpenoid natural compounds in the field of neuroprotection, and the application prospect of the tetracyclic diterpenoid natural compounds in treatment of neurodegenerative diseases is expanded.

This invention relates to the field of cell biology, and more particularly to a method for constructing an artificial cell model in vitro based on extracts from Xenopus laevis egg cells. The method includes: mixing cytoplasmic extracts from Xenopus laevis egg cells, demembranous sperm, and tubulin, dispersing the mixture in an oil phase to obtain a reconstructed system; reacting the reconstructed system at 20-24°C for at least 30 minutes, resulting in the formation of a phospholipid bilayer-based cytoplasmic membrane structure around the cell. This invention provides a method for constructing artificial cells by selecting cytoplasmic extracts from Xenopus laevis egg cells, adding specific substances, and reacting under specific conditions to allow the extracts to self-assemble into cell structures in vitro, simultaneously forming a cytoplasmic membrane. The method provided by this invention offers important clues to the origin and evolution of cells, and the resulting artificial cell structures are highly similar to normal cells, possessing significant application value.

The invention discloses a podophyllotoxin structure-based tubulin / EGFR (epidermal growth factor receptor) dual-targeting podophyllotoxin triazole derivative and application thereof in antitumor drugs, and belongs to the technical field of medicinal chemistry. A triazole group is introduced into a podophyllotoxin mother nucleus through click chemistry, and a series of novel derivatives are designed and synthesized. Molecular docking studies show that the compound can target tubulin and EGFR kinase structural domains at the same time, and tumor cell proliferation is inhibited through a double-target synergistic effect. In-vitro experiments prove that the derivative has significant inhibitory activity on non-small cell lung cancer cells and has low toxicity on normal pulmonary epithelial cells. The dual-targeting strategy can overcome the drug resistance problem of the EGFR inhibitor, optimizes the pharmacokinetic characteristics, has the advantages of high oral availability, good in-vivo stability and the like, and is suitable for treatment of solid tumors such as non-small cell lung cancer and the like.

The invention provides a parasite expelling composition and application thereof in yak breeding, the parasite expelling composition comprises albendazole and myrobalan acid, through the synergistic effect of albendazole and myrobalan acid, on one hand, the myrobalan acid inhibits the activity of liver microsome metabolic enzymes, prolongs the half-life period of albendazole, improves the bioavailability and optimizes the pharmacokinetic process, on the other hand, the myrobalan acid inhibits the activity of liver microsome metabolic enzymes, and on the other hand, the myrobalan acid inhibits the activity of liver microsome metabolic enzymes; on the other hand, the two act on parasite tubulin synthesis and a body surface biofilm structure respectively to form double-target synergistic killing, so that the parasite expelling effect is remarkably improved; chebulinic acid can repair gastrointestinal mucosa, regulate flora balance, enhance appetite and effectively counteract irritant injury of albendazole to gastrointestinal tracts; the parasite expelling rate reaches 95% or above, the average daily gain reaches 369 g / d, and no obvious influence is caused to the blood system and liver and kidney functions of yaks; the composition has the characteristics of simple formula, gastrointestinal protection and convenience in administration, is adaptive to the current breeding situation of high parasite infection rate of yaks in plateau pasturing areas, and has a good industrial application prospect.

The present invention discloses a polycyclic compound as a tubulin stabilizer having a structure represented by general formula (I) and a preparation method thereof, wherein the definitions of Ar, W, Z, X, Y, and heterocycle A are as described in the specification. The present invention also discloses a preparation method for this type of compound. The compound represented by general formula (I) of the present invention can be used to prepare a medicament for preventing and / or treating tumors and neurodegenerative diseases.

The invention discloses dsRNA (double-stranded ribonucleic acid) related to beta-tubulin protein and application of the dsRNA in insect killing, and belongs to the technical field of biology. The dsRNA is a double-stranded RNA, and the dsRNA targets mRNA of a coding gene of a protein with an amino acid sequence of SEQ ID NO: 7. Experiments prove that the dsRNA provided by the invention has high efficiency and specificity, and can effectively kill corresponding mosquitoes from the dsRNA.

Disclosed are compositions and / or methods of use of the compositions for patients with neuronal diseases such as AD, Parkinson's, Huntington's, multiple sclerosis, and ALS. In certain embodiments flavonoids alone, or in a pharmaceutical preparation, are administered through the nasal olfactory route. In certain embodiments the flavonoid is apigenin and the neural disease is Alzheimer's. In some embodiments a porosome complex is administered for reconstitution into a neural cell. In certain embodiments, a co-administered blood-brain barrier traversing peptide is configured as a mimic of a domain of ATP1A3 and / or Tubulin.

The invention discloses quantum dot fluorescent microsphere immunochromatography test paper for detecting fish meat texture and a preparation method of the quantum dot fluorescent microsphere immunochromatography test paper, and belongs to the technical field of food detection. The test paper comprises a bottom plate, a sample pad, a combination pad, a detection pad and a water absorption pad, a detection line (T line) and a quality control line (C line) are arranged on the detection pad, beta-tubulin is sprayed on the T line, and a goat anti-mouse IgG polyclonal antibody is sprayed on the C line; and a beta-tubulin monoclonal antibody probe marked by quantum dot fluorescent microspheres is sprayed on the combination pad. The change condition of the fish meat structure is reflected through the quantum dot fluorescent microsphere probe, and the freshness of the sample is objectively and accurately evaluated; the test paper sampling amount is small, and damage to samples is small; the detection sensitivity is high and the operation is simple; detection time is short, and interpretation is visual; the target analyte is clear, and the protein can be specifically combined with the antibody, so that high-specificity detection is realized; the test paper has excellent stability and long-term retention of experimental results.