44 results about "Polo-like kinase" patented technology

The present invention provides compositions comprising interfering RNA (e.g., siRNA, aiRNA, miRNA) that target polo-like kinase 1 (PLK-1) expression and methods of using such compositions to silence PLK-1 expression. More particularly, the present invention provides unmodified and chemically modified interfering RNA molecules which silence PLK-1 expression and methods of use thereof. The present invention also provides serum-stable nucleic acid-lipid particles (e.g., SNALP) comprising an interfering RNA molecule described herein, a cationic lipid, and a non-cationic lipid, which can further comprise a conjugated lipid that inhibits aggregation of particles. The present invention further provides methods of silencing PLK-1 gene expression by administering an interfering RNA molecule described herein to a mammalian subject. The present invention additionally provides methods of identifying and / or modifying PLK-1 interfering RNA having immunostimulatory properties. Methods for sensitizing a cell such as a cancer cell to the effects of a chemotherapy drug comprising sequentially delivering PLK-1 interfering RNA followed by the chemotherapy drug are also provided.

The invention relates to an LRR-RLK (leucine-rich repeat receptor-like kinase) gene AhRLK6 associated with bacterial wilt resistance of arachis hypogaea.L and a construction method of an over-expression vector of the gene and in particular relates to an application of the gene AhRLK6 in arachis hypogaea.L to tobacco bacterial wilt resistant gene engineering, belonging to the technical field of plant gene engineering. The gene contains nucleotide sequences shown in SEQ ID No.1. The over-expression vector is constructed to transform Cuibi-1 tobaccos, the transgenic plants are inoculated with ralstonia solanacearum through molecular detection, and over-expression of the over-expression vector in the tobaccos can conduce to obviously improving the resistance of the transgenic tobaccos to bacterial wilt, thereby indicating that AhRLK6 possibly participates in the defence reaction of the plants to ralstonia solanacearum, which lays the foundation for bacterial wilt resistant genetic breeding of the plants and strongly promotes the development and application of the tobacco bacterial wilt resistant gene engineering.

The invention relates to the field of pharmaceutical chemistry, in particular to medical use of 34 compounds and medicinal composition containing the compounds, particularly use as Polo like kinase 1 inhibitor. Diseases associated with the Polo like kinase 1 inhibitor include melanoma, liver cancer, kidney cancer, acute leukemia, non-small-cell lung cancer, prostatic cancer, cancerous goiter, skin cancer, colorectal cancer, pancreatic cancer, ovarian cancer, breast cancer, myelodysplastic syndromes, esophageal cancer, gastrointestinal tract cancers or mesothelioma.

The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumour growth, rheumatoid arthritis, restenosis and atherosclerosis.

The invention relates to the field of the pharmaceutical chemistry, in particular to aromatic dihydrazide compounds, a preparation method of the compounds, pharmaceutical composites with the compounds and medical applications of the compounds, especially the applications of the compounds used as Polo like kinase 1 inhibitor.

The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.

The invention relates to salt tolerance related LRR-RLK (leucine-rich repeats-receptor-like kinase) in arabidopsis thaliana and an application thereof to cultivation of salt tolerant transgenic plants. The amino acid sequence of LRR-RLK of a protein is shown in SEQ ID No.2 and a coded nucleotide sequence is shown in SEQ ID No.1. The protein related to salt tolerance of plants and a coding gene thereof, which are provided by the invention, have important significance in improving and reinforcing the stress resistance of arabidopsis thaliana and then accelerating the stress resistant molecular breeding process and have realistic application values in agricultural production in China.

The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

The invention provides an amion thiazolidone compound, as shown in a formula I, wherein A1 is aryl or ceteroary; A2 is benzene ring or substituted benzene ring, double benzene nucleus or substituted double benzene nucleus, pyridine ring (including 2-, 3-, 4-pyridine) or substituted pyridine ring; and R1, R2, R3, R4, R5 and R6 are respectively H, halogen, hydroxy, cyan, amino or nitro or C1-C6 alkyl or C1-C6 alkoxy and the like; and R7 and R8 are respectively H, C1-C6 alkyl or C3-C6 naphthene base. The compound in the formula I comprises hydrate of the compound, solvate, stereoisomer, N-oxide, salt and crystalline forms which exist in various forms. Bioactivity tests show that: the compound in the formula I can restrain the activities of polo-like kinase 1 (PLK1) inside and outside the human body, and can be used for preparing antitumor drugs. The invention further provides a method for preparing the compound in the formula I.

The invention relates to the field of medicinal chemistry, and in particular relates to 2-phenylaminopurine compounds, a preparation method for the compounds, a medicinal composition containing the compounds, and medical applications for the compounds, and in particular an application for the compounds as Polo-like kinase 1 inhibitors.

The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor / polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.

Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser / Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.

Antisense compounds, compositions and methods are provided for modulating the expression of polo-like kinase. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding polo-like kinase. Methods of using these compounds for modulation of polo-like kinase expression and for treatment of diseases associated with expression of polo-like kinase are provided.

The invention relates to the field of medicinal chemistry, and particularly relates to 2-amino-quinazolines compounds, preparation methods of the 2-amino-quinazolines compounds, medicinal compositions containing the compounds, and medical applications of the 2-amino-quinazolines compounds and the medicinal compositions, especially applications of the 2-amino-quinazolines compounds and the medicinal compositions serving as Polo-like kinase1 inhibitors.

The invention relates to the field of medicinal chemistry, and particularly relates to pyridino-miazines compounds, preparation methods of the pyridino-miazines compounds, medicinal compositions containing the compounds, and medicinal applications of the pyridino-miazines compounds and the medicinal compositions, especially applications of the pyridino-miazines compounds and the medicinal compositions serving as Polo-like kinase 1 inhibitors.

The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.

The invention relates to modulating Cdc14B levels (cell division cycle 14 homolog B) and / or Cdh1 (Fzr1 protein, CDC20-like 1b, or fizzy-related protein) levels to sensitize cells to DNA damage by increasing the abundance of Plk1 (polo-like kinase 1) in a target cell. In certain embodiments, the invention relates to modulating Plk1 levels, and in particular to increasing Plk1 levels, to sensitize target cells such as cancer cells to cell death or apoptosis. In certain embodiments, the invention relates to inhibitors of Cdc14B and Cdh1 that sensitize tumor cells to chemotherapy or radiation induced cell death or apoptosis. In addition to applications relating to cancer therapies and diagnostics, the Plk1 modulators and assays will be employed for identifying novel drugs or drug candidates useful for various proliferative and / or differentiative disorders such as major opportunistic infections, immune disorders, cardiovascular diseases and inflammatory disorders.

The invention relates to the field of medicinal chemistry, and in particular relates to 2-imidazole ring-substituted thiophene PLK1 (Polo-like kinase 1) inhibitors, a preparation method for the inhibitors, a medicinal composition containing the compounds, and medical applications for the compounds, and in particular an application for the compounds as Polo-like kinase 1 (PLK1) inhibitors.

The present invention relates to 4-pyrimidinylamino-benzenesulfonamide derivatives of general formula (I) and pharmaceutically acceptable salts, solvates, hydrates, regioisomeric and polymorphic forms thereof, processes for manufacturing of them, the use of them, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and / or diluents, especially for the inhibition of polo-like kinases (PLKs) and the treatment of cancer. Said 4-pyrimidinylamino-benzenesulfonamide compounds have been also identified as new drug candidates for the prevention and / or treatment of infectious diseases like bacterial diseases e.g. tuberculosis, including the currently multidrug-resistant tuberculosis (MDR-TB), extensively drug-resistant tuberculosis (XDR-TB) as well as for preventing tuberculosis.

The invention relates to a device for detecting bladder cancer. The device comprises a sample receiving pad, a detecting reagent pad, a display film and an absorbing pad, wherein the sample receiving pad is used for absorbing a urine sample; the detecting reagent pad is connected to the sample receiving pad and comprises a first antibody of Polo-like kinase 2 and a metal grain combined with the first antibody; the display film is connected to the detecting reagent pad and comprises a detecting area and a quality control area; the absorbing pad is connected to the quality control area of the display film; the detecting area is located between the quality control area and the detecting reagent pad and comprises a protein fixed on the detecting area and a Polo-like kinase 2 combined with the protein; and the quality control area comprises a second antibody fixed thereon and the second antibody is the antibody of the first antibody. The device can be used for conveniently, quickly and accurately detecting bladder cancer.

The present invention provides compounds having a structure according to Formula (I):or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.

This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).

The invention discloses a construction method and application of complementary deoxyribonucleic acid (cDNA) of a somatic embryogenesis receptor-like kinase (SERK) coding gene for regulating somatic embryogenesis of anthurium andraeanum. Initiation codon of a coding gene cDNA sequence is located at 19 base pairs, termination codon of the coding gene cDNA sequence is located at 1888 base pairs, and 622 amino acids are coded in total. The tender leaf of a mature anthurium andraeanum plant is taken as an explant, and through three stages of initiating culture, subculture and development culture, a regeneration plantlet is successfully obtained through an indirect somatic embryogenesis method; the induction callus period of the explant is shorter, and the plant has a high survival rate, quick propagation speed and stable heredity and is not easy to generate cytometaplasia; and the whole SERK gene cDNA sequence of the anthurium andraeanum is separated and cloned, and the SERK gene expression in various periods of different culture stages are analyzed at a transcriptional level to deepen the understanding on the somatic embryogenetic mechanism of the anthurium andraeanum, thereby disclosing the SERK coding gene cDNA for regulating the somatic embryogenesis of the anthurium andraeanum and the construction method of the SERK coding gene cDNA, and providing a high reference value for the function of SERK genes in somatic embryo sex transformation.

The present invention is directed to methods for treating cancer in a subject, such as a cancer of the endocrine system. In some aspects, the method includes administering to the subject one or more of a polo-like kinase 1 inhibitor, a mouse double minute 2 inhibitor, and / or a mitotic catastrophe inducing compound. In other aspects, the method includes measuring an expression level of one or more markers, including caspase 8 and caspase 9, to assess the functionality of the caspase cascade in the subject.

The invention discloses functions and application of activin receptor-like kinase 4 (ALK4) in treatment of cardiac hypertrophy. The ALK4 has the functions of restraining cardiac hypertrophy and fibrosis thereof and improving the cardiac function in a cardiac hypertrophy model caused by an aortic coarctation operation and Ang II stimulation. Accordingly, an ALK4 gene can be used as a medicine target to be applied to screening of medicine for protecting the cardiac function, resisting cardiac fibrosis and / or preventing, relieving and / or treating cardiac hypertrophy. The ALK4 can be used for preparing the medicine for protecting the cardiac function, resisting cardiac fibrosis and / or preventing, relieving and / or treating cardiac hypertrophy, and a new path for treating cardiac hypertrophy is provided.

The invention relates to the field of medicinal chemistry, in particular to application of 4-aminopyrimidine compounds, 4 compounds (1-4), medical application of medicinal compositions containing the compounds, and especially application of the medicinal compositions serving as Polo-like kinase 1 inhibitors.