42 results about "Casein kinases" patented technology

The present invention discloses and claims compounds of formula (I) as inhibitors of human casein kinase IF, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.

A method of inhibiting angiogenesis in a mammal is disclosed, which employs a pharmaceutically acceptable composition containing a selective inhibitor of protein kinase CK2 (also known as casein kinase II) enzymatic activity, such as emodin, aloe-emodin, 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB), and 4,5,6,7-tetrabromobenzotriazole (TBB). Also disclosed is a use of a selective inhibitor of protein kinase CK2 enzymatic activity in the manufacture of a medicament for inhibiting angiogenesis. An in vitro method of screening a potential antiangiogenic agent is also disclosed. A kit for the treatment of a disease by inhibiting angiogenesis is disclosed that contains the pharmaceutically acceptable composition containing a selective inhibitor of protein kinase CK2 enzymatic activity.

The present invention includes the disclosure of the hPER2 gene and a mutant of the hPER2 gene that participates in the human circadian biological clock. The product of the mutant hPER2 gene found in some familial advanced sleep phase syndrome patients is hypophosphorylated by casein kinase epsilon due to the serine-to-glycine mutation caused by the point mutation of the genomic sequence. Specifically, this serine-to-glycine mutation affects the casein kinase epsilon binding region of the hPER2 protein, thus blocking the phosphorylation cascade ordinarily caused by the binding of casein kinase epsilon to hPER2.

The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and / or casein kinase (CK) pathways (e.g., CK1δ, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and / or CK pathways (e.g., CK1δ, and upstream and downstream protein kinases).

The invention discloses joint application of three types of monoclonal antibody-coupled immunomagnetic beads to sorting tumor cells and a method for sorting breast cancer tumor cells. The three types of monoclonal antibody-coupled immunomagnetic beads include anti-HLA-G (human leukocyte antigen-G) monoclonal antibody-coupled immunomagnetic beads, anti-EpCAM (epithelial cell adhesion molecule) monoclonal antibody-coupled immunomagnetic beads and anti-CK8 / 18 (casein kinase 8 / 18) monoclonal antibody-coupled immunomagnetic beads. The joint application and the method have the advantages that the three types of jointly applied antibody-coupled immunomagnetic beads are high in breast cancer tumor cell enrichment ratio and good in sensitivity and repeatability, and the relevant tumor cells can be detected; the three types of immunomagnetic beads (the anti-EpCAM immunomagnetic beads, the anti-HLA-G immunomagnetic beads and the anti-CK8 / 18 immunomagnetic beads) are jointly applied to enriching the tumor cells, so that the circulating tumor cell coverage rate can be increased to the greatest extent, the enrichment ratio can reach 80%, and a technology is international pioneer; the tumor cell enrichment specificity and sensitivity can be particularly guaranteed owing to usage of the anti-HLA-G monoclonal antibody-coupled immunomagnetic beads.

Disclosed are methods related to label-free biosensor cellular assays to classify multienzyme complex modulators in live cells. Disclosed are also methods related to the identification of purinosome disrupting Casein Kinase II (CK2) inhibitors, and methods related to the use of purinosome disrupting CK2 inhibitors as therapeutic agents for modulating CK2 activity and purine synthesis pathway, and for improving prevention and treatment of CK2 associated cancers, viral infection and inflammation conditions.

The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and / or casein kinase (CK) pathways (e.g., CK1δ, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and / or CK pathways (e.g., CK1δ, and upstream and downstream protein kinases).

The present invention discloses and claims compounds of formula (I)as inhibitors of human casein kinase IF, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.

The invention relates to peptides including DEDE(SSD)nDEG indicated by SEQ NO. 1, RRRDEDE(SSD)nDEG indicated by SEQ No. 2, RRRGDEDE(SSD)nDEG indicated by SEQ No. 3, and LKKLKKLDEDE(SSD)nDEG indicated by SEQ NO. 4, wherein n is an integer from 2 to 20. The invention also relates to phosphorylating these peptides at multiple amino acid sites by employing casein kinases. These phosphorylated peptides may be used in various applications such as forming mineralized collagen fibrils and biomimetic composites for use in tissue repair and regeneration.

The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and / or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents.

This invention is related to the Molecular Pharmacology field and especially to the development of peptides useful for treating epithelial tumors and mainly those associated to oncogenic types of HPVs. The main objective of this invention is to identify peptides whose structure permits to block the Casein Kinase II (CKII) phosphorylation domain by direct interaction with such a site. In the present invention it is shown eleven cyclic peptides with different aminoacid sequences which inhibit the CKII phosphorylation in vitro, exhibit cytotoxicity on HPV-16 transformed cells (CaSki) and also increase the sensitivity of these cells to the cytostatic effect of interferon (IFN). Furthermore, the invention relates to the use of these peptides conjugated or fused to other peptides and chemical compounds which penetrates into cells as well as with the use of both peptide and chemical mimetic molecules.

A transgenic plant transformed by a casein kinase Stress-Related Polypeptide (CKSRP) coding nucleic acid, wherein expression of the nucleic acid sequence in the plant results in increased tolerance to environmental stress as compared to a wild type variety of the plant. Also provided are agricultural products, including seeds, produced by the transgenic plants. Also provided are isolated CKSRPs, and isolated nucleic acid coding CKSRPs, and vectors and host cells containing the latter.

The invention discloses a cotton casein kinase gene and its application, and relates to a separation cloning, a function verification and an application of a gene GhCKI used for controlling anther growth and identified in a cotton anther expression spectrum. There is a 72% homology between the protein coded by the GhCKI gene and the protein coded by an Arabidopis thaliana ATCKL2 gene, and the GhCKI gene preferentially expresses in the anther, has an anther growth controlling function, can be applied to the sterile line cultivation of a plurality of plants through genetic transformation, and simultaneously can be used as a marker gene of the plant anther fertility stability under high temperature stress.

The invention relates to chemical compounds which are obtained by means of in silico molecular modelling and which have a structure that can be used to block phosphorylation by interacting said compounds with the phosphorylation domain or the environment thereof in the substrates of the Casein Kinase II enzyme. The invention also relates to pharmaceutical compositions that contain said compounds and to the use thereof in the preparation of medicaments for the treatment of diseases associated with neoplastic processes.

The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1δ) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.

Disclosed in the present invention are an acrylanilide compound represented by general formula (I) and a pharmaceutically acceptable salt thereof. The acrylanilide compound and the pharmaceutically acceptable salt thereof are used for treating clinical diseases by mainly acting on EGFR family casein kinases.

There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and / or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof:[wherein, in the formula (1), each of R1 and R2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]

The invention relates to the field of biological medicine, and discloses a phosphorylation modification LEA (late embryogenesis abundant) protein as well as a preparation method and application thereof. The phosphorylation modification LEA protein is connected with phosphate groups at Ser, Thr and Tyr sites, and the preparation method of the phosphorylation modification LEA protein comprises the steps of cloning an LEA protein gene; constructing a prokaryotic expression vector, and connecting the LEA protein gene to the prokaryotic expression vector; converting the prokaryotic expression vector into Escherichia coli, inducing the expression of the LEA gene in the Escherichia coli to synthesize the LEA protein, and collecting and purifying the LEA protein; performing phosphorylation modification on the LEA protein by using casein kinase. The protective effect of the prepared phosphorylation modification LEA protein on protein products is significantly enhanced, so that the phosphorylation modification LEA protein can be widely applied to preparation of a protective agent of the protein products.

This invention is related to the Molecular Pharmacology field and especially to the development of peptides useful for treating epithelial tumors and mainly those associated to oncogenic types of HPVs. The main objective of this invention is to identify peptides whose structure permits to block the Casein Kinase II (CKII) phosphorylation domain by direct interaction with such a site. In the present invention it is shown eleven cyclic peptides with different aminoacid sequences which inhibit the CKII phosphorylation in vitro, exhibit cytotoxicity on HPV-16 transformed cells (CaSki) and also increase the sensitivity of these cells to the cytostatic effect of interferon (IFN). Furthermore, the invention relates to the use of these peptides conjugated or fused to other peptides and chemical compounds which penetrates into cells as well as with the use of both peptide and chemical mimetic molecules.

Methods and related compositions are disclosed for treating an array of myeloproliferative disorders and hematological malignancies. In particular, treatment methods and compositions for treating chronic myelogenous leukemia are disclosed. The methods and compositions utilize certain casein kinases, and specifically CK2α agents.

The invention provides an application of a casein kinase PPK related to the growth and development of plants. The casein kinase PPK is PPK1, PPK2, PPK3 or PPK4, and the sequence registration numbers thereof are At3G13670, At5G18190, At3G03940 and At2G25760 respectively. The casein kinase PPK is used for improving the growth and development of the plants, and then is applied to crop production.

The invention provides a method of inhibiting casein kinase 1 DETA (CK1 DETA), comprising contacting the CK1 DETA with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and / or overexpressed in human breast tumors and that CK1 delta can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1 DETA and BETA-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.

A transgenic plant transformed by a casein kinase Stress-Related Polypeptide (CKSRP) coding nucleic acid, wherein expression of the nucleic acid sequence in the plant results in increased tolerance to environmental stress as compared to a wild type variety of the plant. Also provided are agricultural products, including seeds, produced by the transgenic plants. Also provided are isolated CKSRPs, and isolated nucleic acid coding CKSRPs, and vectors and host cells containing the latter.

Provided is a novel oxazolone derivative having an inhibitory activity on casein kinase 1[delta] and casein kinase 1[epsilon]. The inhibitor can inhibit casein kinase 1[delta] and casein kinase 1[epsilon], and therefore can provide a medicinal agent useful for the treatment and / or prevention of diseases of which the disease condition are associated with the mechanism of activation of casein kinase 1[delta] or casein kinase 1[epsilon]. Particularly, the inhibitor can provide a medicinal agent useful for the treatment of circadian rhythm disorders (including sleep disorder), central nervous system degenerative diseases and cancer. An inhibitor of casein kinase 1[delta] and casein kinase 1[epsilon], which comprises an oxazolone derivative represented by general formula (1), a salt of the derivative, or a solvate or hydrate of the derivative or the salt as an active ingredient. [In formula (1), X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom and an iodine atom).]

There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and / or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof:wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).

The invention discloses corn casein kinase 2CK2[alpha]2 and application of a coding gene of the corn casein kinase 2CK2[alpha]2 based on high-temperature stress response, and aims to solve the technical problem that high-temperature-resistant gene resources and germplasm resources of corn are deficient at present. Based on the discovery that a corn casein kinase 2[alpha] subunit can respond to high temperature stress, overexpression vectors OE-ZmCK2[alpha]2 and pFGC5941-ZmCK2[alpha]2 overexpression vectors are constructed, ZmCK2[alpha]2 overexpression homozygous strains are obtained by using a corn genetic transformation technology, and strains with high expression quantity are screened out by using qRT-PCR (quantitative reverse transcription-polymerase chain reaction) detection and are used as breeding materials for breeding high-temperature-resistant corn varieties / lines. The invention determines that the corn casein kinase 2[alpha] subunit can respond to high-temperature stress, and preliminarily analyzes the action mechanism of the corn casein kinase 2[alpha] subunit under high-temperature stress, thereby being beneficial to understanding the heat-resistant mechanism of corn, and providing important gene resources and related germplasm resources for cultivating high-temperature-resistant corn varieties.

The invention relates to the technical field of biomedicines, and particularly relates to application of complete sequence protein of a human-derived ribosomal protein L22 (RPL22) in anti-cancer anti-tumor medicines. For the complete sequence protein of recombinant human-derived RPL22 in medicines for treating non-small cell lung cancer or anti-tumor medicines, the sequence of the RPL22 is as shown in a sequence 1. The recombinant human-derived RPL22 can be used as an endogenous casein kinase inhibitor to achieve the anti-cancer activity, and has an effect of individually inhibiting cancer cell activity in the field of non-small cell lung cancer inhibition. The protein is a human own endogenous protein, has good biological safety, and can be combined with other anti-cancer medicines on the premise that relatively strong anti-cancer activity is ensured so as to reduce dosage of other anti-cancer medicines and toxic and side effects of other anti-cancer medicines.

There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and / or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of, particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof:wherein X represents a halogen atom which is fluorine, chlorine, bromine or iodine.