323 results about "Tubulin" patented technology

The present invention relates to compounds, and methods utilizing compounds, which exhibit one or more of the following properties: i) disrupts organization of an actin cytoskeleton of a cell; ii) disrupts organization of a microtubule network of a cell; iii) induces accumulation of tubulin at centrosomes but does not induce accumulation of tubulin in a nucleus of a cell; iv) induces accumulation of tubulin at centrosomes at a concentration of 500 nM or less within four hours; v) induces accumulation of Hsp70 and has weak-to-moderate proteasome inhibitory activity; and vi) does not have proteasome inhibitory activity when assayed on purified proteasomes.

Disclosed are nucleic acid and amino acid sequences for acetolactate synthase, acetolactate synthase regulatory regions, α-tubulin promoter, a promoter from a Thraustochytriales polyketide synthase (PKS) system, and fatty acid desaturase promoter, each from a Thraustochytriales microorganism. Also disclosed are recombinant vectors useful for transformation of Thraustochytriales microorganisms, as well as a method of transformation of Thraustochytriales microorganisms. The recombinant nucleic acid molecules of the present invention can be used for the expression of foreign nucleic acids in a Thraustochytriales microorganism as well as for the deletion, mutation, or inactivation of genes in Thraustochytriales microorganisms.

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.

Disclosed inter alia is the use of quinazolinone derivatives, which are modulators of a mitotic kinesin such as KSP, in the treatment of cellular proliferative diseases. The quinazolinone derivatives are administered with another chemotherapeutic agent selected from alkylating agents, antimetabolites, platinating agents, topoisomerase inhibitors, tubulin agents and signalling inhibitors (e.g., kinase inhibitors). Pharmaceutical compositions comprising one or both types of active agents are also disclosed.

The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4′ position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3′ thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3′ to form amino acid amide water soluble prodrug having the structure shown as formula (I)

the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.

The invention relates to a method for screening real-time fluorescence quantitative PCR internal reference molecules of a desert plant Eremosparton songoricum (Litv.) Vass.. The invention is characterized in that homologous clone is used for cloning 8 internal reference molecules in Eremosparton songoricum (Litv.) Vass., and a real-time fluorescent quantitative PCR internal reference gene specific primer is designed, 10 types of seedling grown for two weeks with abiotic stress and non stress (contrast) are taken as the experimental materials for carrying out a fluorescent quantitative PCR experiment to verify, analysis of fluorescent quantitative data is carried out by using geNorm software, so that the optimum and the stablest internal reference molecules screened for fluorescent quantitative researches under various abiotic stresses developed by the seedling of Eremosparton songoricum (Litv.) Vass. are EF and alpha-tubulin. The method of the invention is capable of avoiding the errors on RNA quality, output, inverse transcription efficiency and the like of the seeding material of Eremosparton songoricum (Litv.) Vass. under different abiotic stresses, better correcting and standardizing the data obtained by the real-time fluorescent quantitative determination and enhancing the accuracy and reliability of researches.

The present invention relates to an Aspergillus niger strain ANUV90 with high stable resistance to carbendazim obtained by mutagenesis, and the resistance of the strain to carbendazim is 1000 times higher than that of the original starting strain AN. Aspergillus niger ANUV90 can still grow normally under the treatment concentration of active ingredient carbendazim up to 1000 μg/mL, and the fermentation broth of this strain also has nematicidal activity. After testing, the strains before and after mutagenesis have no significant difference in colony morphology and other characteristics. At the same time, they have certain biological activity against tomato root-knot nematode. The preliminary research results of the analysis of the molecular mechanism of drug resistance of the mutant strains show that the gene encoding β-tubulin has a site-directed mutation , leading to the generation of drug resistance in biological characteristics of ANUV90. The bacterial strains specifically involved in the present invention have been preserved in the General Microorganism Center of China Microbiological Culture Collection Management Committee on October 30, 2007, with the preservation number CGMCC No.2234, and the classification name: Aspergillus niger. This feature of the strain allows it to be used synergistically with most commonly used pesticides to control a variety of harmful organisms, providing a way to solve the problem of unstable control effects of biocontrol strains in the field, and has a good development and application prospect.

The present invention relates to a tumor marker for diagnosis of ovarian cancer, which is selected from the group consisting of alectin-1, cathepsin B, MHC class I antigen, heat shock protein (HSP) 27, ubiquitin carboxy-termal esterase L1, cellular retinol-binding protein (CRBP), transthyretin, SH3 binding glutamate-rich protein, tubulin-specific chaperone A, RNA binding protein regulatory subunit, γ-actin, tropomyosin and calcium/calmodulin-stimulated cyclic nucleotide phosphatase. The ovarian cancer is diagnosed effectively and efficiently based on detecting the expression levels of the tumor markers in the invention from the ovarian tissue sample of an individual to be diagnosed.

FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

The ciliated protozoan Tetrahymena exemplifies a recombinant system for the expression of heterologous nucleic acids, preferably on the plasma membrane surface. Integration of a heterlogous nucleic acid into the β-tubulin gene, BTU1, of a paclitaxel-sensitive T. thermophila mutant that possesses btu1-IK350M β-tubulin allele allows screening for transformants using negative selection, as transformants have restored paclitaxel resistance. Transgenic ciliated protozoa of the invention can serve as live vaccines. For example, transgenic Tetrahymena expressing Ichthyophthirius multifiliis i-antigen protein on their surface are effective vehicles for vaccination of freshwater fish against infection by I. multifiliis.

The invention belongs to the field of agricultural and biological technology and relates to a Laodelphax striatellus lethal gene fragment thereof. The invention is to screen the Laodelphax striatellus lethal gene fragment Tubulin, which can lead to the death of Laodelphax striatellus after interference and has a sequence represented by SEQ ID No.1, from Laodelphax striatellus by using a laboratory improved dsRNA feeding method. When the dsRNA of the gene fragment is used for feeding Laodelphax striatellus, the maximum adjusted mortality of the Laodelphax striatellus may reach 67.4 percent, and a sequence basis and a data basis are provided for the construction of a new policy of controlling pests by using RNA interference technology.

Compositions comprising a cancer drug, a continuous oral dosing schedule with a drug which binds to the colchicine site of tubulin β-subunits, and methods of treating cancer in a pediatric patient using continuous dosing schedules are disclosed.

The invention relates to a 1-substituted benzylidene-2-naphthalenone derivative, a preparation method thereof and use thereof, and particularly discloses a derivative shown in the formula (I) or pharmaceutical acceptable salt thereof. The preparation method is as follows: reflux of dimethoxy naphthalene and metallic sodium is conducted in ethanol, and 3, 4-dihydro-2-naphthalenone is generated after the dimethoxy naphthalene and the metallic sodium are acidized; the 3, 4-dihydro-2-naphthalenone is dissolved in dichloromethane and catalyzed by acetic acid piperidine, and then is stirred and reacts at room temperature, and 1-benzylidene-3, 4-dihydro-2-naphthalenone is generated; and the 1-benzylidene-3, 4-dihydro-2-naphthalenone is dissolved in 10% of dichloromethane methanol solution, sodium borohydride is added, and then the 1-substituted benzylidene-2-naphthalenone derivative can be obtained by reduction. The 1-substituted benzylidene-2-naphthalenone derivative has the good effect of treating leukemia, further has the effect of inhibiting microtubulin, and can be used for treating various cancers responding to cell toxicity and cell viability, such as breast cancer or colon cancer, and for treating disease cancer related to abnormal angiogenesis.