38 results about "Methionine aminopeptidase" patented technology

The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.

Methods are provided for detecting methionine aminopeptidase (MAP) activity and for detecting inhibitors of MAP. The methods utilize a peptide comprising an N-terminal methionine which can be cleaved from the peptide by MAP, and a C-terminal detection moiety which is released by a second peptidase only if the N-terminal methionine has been cleaved from the peptide. When the peptide is combined with MAP and the second peptidase, the detection moiety is released, while the addition of a MAP inhibitor will inhibit the release of the detection moiety. Reaction mixes, peptides, and kits which are useful for practicing the methods are also provided.

Inhibitors of type 2 methionine aminopeptidases (“MetAP2”), specifically dominant negative variants of MetAP2, both polypeptides and encoding polynucleotides, are provided. Also provided are methods of treating subjects suffering from cancer, diseases mediated by the immune system or opportunistic infections using inhibitors of MetAP2. Also provided are high through put screens and assays to detect and identify inhibitors of MetAP2 and downstream effectors of MetAP2.

Disclosed are compounds which are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

Disclosed are compounds of the formula:

wherein the formula variables are as defined herein. The compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase. Also disclosed is the use of such compounds in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

The instant invention provides methods and compositions for treating a subject suffering from bone associated diseases, such as osteoporosis.

Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.

The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of inducing an immunosupressed condition and/or treating chronic allograft vasculopathy in a subject undergoing or who has undergone a transplant, by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.

Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

Provided is a high-copy-number, high-expression vector capable of producing a protein having satisfactory functions and activity of the same level as that of a natural form of the protein, in a large quantity and in a simple manner. Also provided is a vector including: (A) a target gene or a cloning site of the target gene, (B) a sequence element necessary for the high copying of the target gene, (C) a sequence element necessary for the expression of the target gene and a methionine aminopeptidase gene; a method of producing the vector; a transformant having the vector introduced therein; and a process for producing a protein using the transformant.

Provided herein are formulations and co-solvent formulations and methods for treating an infectious disease utilizing the same. The formulations and co-solvent formulations may comprise a hydroxyquinoline analog or its pharmaceutically acceptable salt, a solvent and at least two surfactants. Also provided are methods of quantitating a hydroxyquinoline analog in a sample via chromatographic/spectrometric measurements.

The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.

The invention provides a compound especially used for inhibiting methionine aminopeptidase (MetAP) in mycobacterium tuberculosis (Mtb). The compound is ceftiofur hydrochloride, and possesses obvious inhibition activity on methionine aminopeptidase in mycobacterium tuberculosis. The compound can be used for preparing small molecular inhibitors used for inhibiting methionine aminopeptidase (MetAP) in mycobacterium tuberculosis (Mtb), and is promising to be prepared into drugs used for preventing Mtb infection.

The invention specifically relates to a preparation method for recombinant human interferon alpha-2b free of methionine, which belongs to the field of preparation of interferon. According to the method, primers are designed to amplify gene segments of methionine aminopeptidase, the gene segments of methionine aminopeptidase are cloned into the expression plasmid of pACYCDuct-1 to obtain the recombinant expression plasmid of pACYCDuct-1-MetAP which is introduced into the recombinant expression plasmid of pJW2-rhIFN-alpha-2b containing human interferon alpha-2b genes, 0.1 mu M IPTG is utilized to induce methionine aminopeptidase to express, human interferon alpha-2b protein is induced to express at a temperature of 40 DEG C, and methionine at N terminal of the human interferon alpha-2b protein is resected in the process of expression. The preparation method provided in the invention enables unnecessary Met residue at the N terminal of human interferon alpha-2b to be removed, stability and antiviral activity of human interferon alpha-2b to be improved, immunogenicity of human interferon alpha-2b to be reduced and an incidence rate of adverse reactions during utilization of human interferon alpha-2b by patients to be reduced.

The invention discloses a kit for detecting mycoplasma genitalium. The invention provides two schemes; in a scheme I, the kit comprises two reagents, namely methionine aminopeptidase and leucocyte esterase, wherein an enzyme substrate for detecting the activity of the methionine aminopeptidase is a methionine derivative containing a chromogen, and an enzyme substrate for detecting the activity ofthe leucocyte esterase is an ester derivative containing the chromogen; in a scheme II, the kit comprises three reagents, i.e., the kit is also comprises a proline aminopeptidase reagent on the basisof the scheme I, and an enzyme substrate for detecting the activity of proline aminopeptidase is a proline derivative containing the chromogen. According to the kit disclosed by the invention, autosynthetic enzyme or enzyme generated by stimulating parasitic cells during a growth process of the Mg can be detected through a dry chemical enzyme method, the purpose of detecting the mycoplasma genitalium can be achieved, and the kit has the advantages of quickness, simpleness, accuracy and the like. By adopting the kit for detecting the mycoplasma genitalium, the sensitivity and the specificity are higher, properties of the kit are similar to properties of existing like detection reagents, and clinical test needs can be completely met.