12 results about "Topoisomerase" patented technology

The invention belongs to the technical field of medical chemistry, and discloses a 5-O-carbon mould amine tylosin lactone derivative with a double-target combined antibacterial effect as well as a preparation method and application of the 5-O-carbon mould amine tylosin lactone derivative. The derivative is a compound as shown in a formula I, and pharmaceutically acceptable salt, eutectic, tautomer, polymorphic substance, solvate, prodrug or isotope labeled compound thereof. The compound can act on a bacterial ribosome 50S subunit and DNA topoisomerase IV at the same time, and shows an excellent antibacterial effect in an antibacterial activity test, and the minimum inhibitory concentration (MIC) reaches 0.0625 mu g / mL. The compound has the advantages of being high in antibacterial activity, wide in antibacterial spectrum and capable of achieving rapid sterilization, and a new choice is provided for developing drugs with antibacterial activity.

This invention discloses a method for rice to withstand heat stress. RMI1 Genes and their applications. Among them... RMI1 The nucleotide sequence of the gene is shown in SEQ ID No. 1, and the amino acid sequence of the protein it encodes is shown in SEQ ID No. 2; this invention verifies RMI1 The function of the gene, RMI1 protein is located in the cell nucleus, rmi1-1 In mutants RMI1 The deletion of 33 base pairs in the gene results in the loss of 11 amino acids in the RMI1-1 protein, making... rmi1-1 High temperatures during the seedling stage cause a large number of abnormal chromosomes to adhere and fragment during the late mitotic phase of root tip cells, resulting in stunted plant growth and development. rmi1-1 High temperatures during the reproductive growth period of plants lead to a large number of chromosome fragments and adhesions in the late stage of meiosis I, resulting in sterility; high temperatures also affect the interaction between RMI1-1 protein and topoisomerase TOP3α and helicase RECQ4. rmi1-cr3 Frameshift mutations lead to abnormal embryo and endosperm development; overexpression RMI1 This invention can enhance the heat resistance of rice. RMI1 The analysis of gene function provides genetic resources for the breeding of heat-resistant rice varieties.

The invention discloses a recombinant topoisomerase and an application of the recombinant topoisomerase in plasmid linearization. The invention discloses a recombinant topoisomerase with an amino acid sequence as shown in SEQ ID NO.1 at first. The invention further discloses an application of the recombinant topoisomerase in plasmid linearization. The recombinant topoisomerase does not depend on recognition of a specific DNA sequence, cutting sites can be formed on plasmids in a super-spiral form, then a linear product is obtained through the cutting effect of T7 endonuclease I, and linearization of plasmids with unknown sequences can be achieved. The plasmid linearization kit developed by using the recombinant topoisomerase has the characteristics of rapidness, high efficiency and wide applicability, and can realize full-length sequencing of unknown plasmids by combining with a three-generation sequencing technology.

The invention relates to the technical field of medicinal chemistry, and further discloses a folium eriobotryae extract, a preparation method of the folium eriobotryae extract and application of the folium eriobotryae extract in preparation of a medicine with an anti-breast cancer effect. The preparation method of the folium eriobotryae extract comprises the following steps: taking folium eriobotryae, adding the folium eriobotryae into an ethanol aqueous solution according to a material-liquid ratio of 1g: (80-120mL), carrying out ultrasonic extraction, separating an extracting solution after the extraction is finished, and concentrating and drying to obtain the folium eriobotryae ultrasonic extract; and taking the folium eriobotryae ultrasonic extract to obtain the folium eriobotryae extract. Researches show that the loquat leaf extract prepared by the method disclosed by the invention has an inhibition effect on topoisomerase I. Therefore, the folium eriobotryae extract has potential application value when being used for preparing the medicine with the anti-breast cancer effect.

This invention relates to the use of small molecule compounds that allosterically inhibit ALC1 (CHD1L), particularly two classes of ALC1 (CHD1L) allosteric inhibitors of formulas (I) and (II). When combined with inhibitors of several classes of cancer drugs, namely topoisomerase I, topoisomerase II, ATM, ATR, Wee1, BRD, and MEK, or when combined with mitomycin C, paclitaxel, ionizing radiation, or antibody-drug conjugates having tumor-specific antibodies conjugated to TOP1 inhibitors, the small molecule compounds and the allosteric inhibitors exhibit enhancing, preferably additive, effects in the treatment of proliferative diseases. Furthermore, this invention relates to the ALC1 inhibitor of formula (II), which, when combined with PARP inhibitors (poly(ADP-ribose)-polymerase inhibitors (PARPi)), exhibit synergistic effects in the treatment of pancreatic cancer or fallopian tube cancer. By synergizing with the functions of the aforementioned cancer drugs, the ALC1 inhibitors, particularly those of formulas (I) and (II) that enhance the cancer cell killing properties of the aforementioned cancer drugs, are particularly capable of achieving treatments in which any of the aforementioned inhibitors have already been used as part of standard care.

The expression of the ATXN2 gene can be modulated to reduce the amount of ataxin-2 protein produced by a cell. This can be accomplished by administering to the cell an effective amount of an ATXN2 modulating agent. Screening was performed with 428,749 compounds for lowering expression of an ATXN2-luciferase reporter in HEK-293 cells, with a multiplexed cell viability assay to ensure target reduction in the absence of cytotoxicity. Secondary qHTS assays included a CMV-luciferase reporter expressed in HEK-293 cells as well as a biochemical assay using recombinant luciferase to detect inhibitors of the reporter enzyme. A diverse set of compounds were found to reduce ATXN2 expression, including compounds targeting HSP90, cardiac glycosides, NaK-ATPases and topoisomerases.

The present invention relates to a method for determining whether a sample comprises a pathogen or not, such as for determining whether a subject is likely to be infected with a pathogen, said pathogen expressing DNA modifying enzymes capable of cleaving and ligating DNA, such as topoisomerases and integrases. The invention also relates to kits of parts for performing such methods and uses thereof.

The application discloses a kind of bionic composite nanomedicine and its preparation method and application, which is composed of platelet membrane, chemotherapeutic drug DX8951f And topoisomerase II siRNA;The chemotherapeutic drug DX8951f With topoisomerase II siRNA self-assemble to form composite nanoparticles by electrostatic interaction, and the platelet membrane is coated on the surface of the composite nanoparticles.The application successfully constructs a kind of platelet membrane coated DX8951f With topoisomerase II siRNA The carrier-free bionic nanomedicine, overcomes DX8951f Clinical drug resistance problem by chemotherapy-gene synergistic effect, realizes the stable bionic modification of carrier-free nanoparticle by mechanical extrusion coating process, significantly improves drug in-vivo stability, tumor targeting and biological safety.

The application discloses a method for synthesizing a structure monomer of a topological protein in a cell-free system, comprising the following steps: synthesizing a basic sequence comprising a gene sequence for expressing a target protein, a gene sequence for expressing SpyTag or a gene sequence for expressing SpyCatcher; and adding the basic sequence into a cell-free system to synthesize the structure monomer comprising the target protein. The application also provides a method for synthesizing a topological protein in a cell-free system. The purpose of the application is to provide a method for synthesizing a protein which is simpler and faster than a cell system, has an unprecedented design freedom in an open environment, and is controllable in polymerization degree and length of the synthesized protein.

Disclosed herein are topoisomerase I compounds represented by Formula I, or a pharmaceutically acceptable salt thereof, and methods of treating proliferative disorders in a subject, comprising administering a compound disclosed herein:

The invention discloses an aza-tricyclic amide compound as well as a preparation method and application thereof, and belongs to the technical field of synthesis of organic compounds. The aza-tricyclic amide compound is prepared by taking an o-aminobenzaldehyde compound, ethyl 3-bromopyruvate and the like as raw materials through a one-step reaction. The target compound is prepared through condensation, acylation, methylation, cyclization, substitution, hydrolysis and other multi-step reactions. The compounds can significantly inhibit the growth of human colon cancer HCT116 cells, the ICC of the compound B2 reaches 0.45 mu g / mL, and the compounds can effectively act on a DNA-topoisomerase system and inhibit the proliferation of tumor cells, and can be used for the development of antitumor drugs.

The invention relates to a clarithromycin derivative containing a quinolone structure as well as a preparation method and application of the clarithromycin derivative. The compound provided by the invention has antibacterial activity equivalent to that of telithromycin in constitutive streptococcus pneumoniae drug-resistant bacteria and streptococcus pyogenes drug-resistant bacteria. And the antibacterial activity on haemophilus influenzae is better than that of Thailimycin. Furthermore, the anti-streptococcus pyogenes 12-206 activity of part of the compounds disclosed by the invention is obviously superior to that of the existing compounds. In addition, the compound provided by the invention not only can act on ribosome, but also can act on topoisomerase, and is a double-target compound at the cellular level. Therefore, the compound disclosed by the invention is not easy to induce bacteria to generate mutation, and the service life of the compound as an antibacterial agent can be prolonged.