112 results about "Competitive inhibitor" patented technology

A substantially purified substance having the properties of a bacterial microcin methionine analog, methionine synthesis inhibitor, tRNA-methionine synthase inhibitors or methionine competitive inhibitor capable of inhibiting tumor cell growth without inhibiting the growth of normal cells or treating neoplastic diseases, and may be used alone or in combination with other anti-cancer agents. The purified substance may also have anti-hyperhomocysteineuria and/or anti-infective properties, such as antifungal activity. The purified substance can be safely administered to animals including humans for the treatment of neoplastic, hyperhomocysteinemia and/or infectious diseases for the treatment of those diseases.

There is provided compounds of formula I,wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Novel peptide inhibitors of GSK-3, compositions containing same and uses thereof are disclosed. The novel peptide inhibitors are substrate-competitive inhibitors and have an amino acid sequence designed so as to bind to a defined binding site subunit in GSK-3. Also disclosed are GSK-3 substrate competitive inhibitors which bind to the defined binding site subunit in the enzyme. Also disclosed are mutants of GSK-3 and uses thereof for identifying a putative GSK-3 substrate competitive inhibitor.

There is provided compounds of formula Iwherein R1, R2, Y, R3 and R4 have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

There is provided compounds of formula I,wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.

The present invention is related to a pharmaceutical composition for modulating angiogenesis comprising a therapeutically effective amount of an angiogenesis modulating compound and a pharmaceutically acceptable excipient, wherein said modulating compound is a recombinant of caveolin-1, a nucleic acid encoding the partial or total amino acid sequence of caveolin-1, or an analogue thereof or a pharmacologically acceptable derivative thereof, a compound modulating the expression of caveolin-1, an agonist or an antagonist or a competitive inhibitor of caveolin-1, a recombinant hsp90, a nucleic acid encoding the partial or total amino acid sequence of hsp90 or an analogue thereof or a pharmacologically acceptable derivative thereof, a compound modulating the expression of hsp90, an agonist or an antagonist or a competitive inhibitor of hsp90, a recombinant of Akt, a nucleic acid encoding the partial or total amino acid sequence of Akt, or an analogue thereof or a pharmacologically acceptable derivative thereof, a compound modulating the expression of Akt, an agonist or an antagonist or a competitive inhibitor of Akt.

The present disclosure describes methods for treating or preventing Type 1 diabetes mellitus in juveniles, particularly in juveniles newly diagnosed with Type 1 diabetes. This prevention or treatment of Type 1 diabetes is achieved by administering one or more therapeutic agents to a juvenile in need, wherein the therapeutic agent is, for example, a competitive inhibitor of mevalonate synthesis, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, or an inducer of AMP protein kinase (AMPK) activity. In certain embodiments, juveniles with Type 1 diabetes are treated with an HMG-CoA reductase inhibitor such as a statin, thereby decreasing the destruction of islet cells, or maintaining endogenous insulin production, in the juvenile.

The invention provides novel single stage competitive inhibitors of plasmin from the Australian brown snake Pseudonaja textilis textilis. The invention also features polynucleotides and polynucleotide homologues encoding these inhibitors. Pharmaceutical compositions containing the plasmin inhibitors of the invention are also disclosed as well as methods useful for treatment of blood loss.

The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, cancer, Alzheimer's disease, allergic disease, transplant and cell graft rejection, HIV infection and other viral, bacterial, and parasitic infection, and AIDS. Methods are also provided for preparing a peptide having the property of being able to displace CLIP by feeding one or more peptide sequences into software that predicts MHC Class II binding regions in an antigen sequence and related products.

A composition comprising a competitive inhibitor and an edible long chain polyunsaturated oil or a blend of edible oils, wherein the edible long chain polyunsaturated oil or the blend of edible oils comprises one or more long chain polyunsaturated fatty acids and a pro-oxidant.

The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of E. coli TrxR with K_i of 0.14 μM and 0.46 μM, respectively. E. coli mutants lacking glutathione reductase or glutathione were much more sensitive to inhibition by ebselen. Since either glutaredoxin or thioredoxin systems are electron donors to ribonucleotide reductase, ebselen targets primarily glutathione and glutaredoxin-negative bacteria, a class which includes major pathogens. Ebselen, and similar compounds are therefore useful as antibacterial agents, even for multiresistant strains. Two major pathogenic bacteria, which previously had not been known to be sensitive to ebselen, Mycobacterium tuberculosis (tuberculosis) and Helicobacter pylori (stomach ulcer and cancer), were shown to be excellent targets. Helicobacter pylori was also sensitive to ebsulfur.

A composite medicine in the form of form of dispersing tablet, oral disintegrating tablet, capsule, liniment, ointment, etc contains phenandrostamine and additional cyclodextrin or its derivative for higher biologic utilization rate.

There is provided a compound of formula (I) wherein R<1>, R<2a>, R<2b>, R<3a>, R<3b>, R<4>, R<5>, R<6>, A, G and L have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competetive inhibitors of trypsin-like proteases, such as trombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e,g. conditions, such as thrombo-embolisms, where inhibition of trombin is required or desired, and/or conditions wherea anticoagulant thererapy is indicated).

The invention discloses a fusion polypeptide. The fusion polypeptide is prepared from polypeptide I and polypeptide II, wherein the polypeptide I is a specific amino acid sequence on NFAT2, and is selected from one or combination of sequences as shown in SEQ ID NO.2, SEQ ID NO.3 and SEQ ID NO.4; the polypeptide II is an HIV-TAT protein transduction domain, and the sequence of the polypeptide II is as shown in the SEQ ID NO.1. The fusion polypeptide is a competitive inhibitor against DYRK1A phosphorylated NFAT2; in-vitro tests indicate that the fusion polypeptide is capable of lowering the protein level of NFAT2 in tumor cells, so that metastasis of the tumor cells can be inhibited. According to the fusion polypeptide, a new target is provided for design of novel anti-tumor medicines, and a new thought is provided for reverse of multidrug resistance of tumors.

The invention relates to broomcorn glyphosate resistance 5-enolpyruvoyl shikimic acid-3-phosphosynthase (EPSPS) which has tolerance higher than that of other specie variants to competitive inhibitor glyphosate of the synthetic substrate phosphoenolpyruvic acid (PEP). The invention also relates to application of the variants in cultivation of glyphosate resistance corn.

The invention provides FGFR1 (Fibroblast Growth Factor Receptor1) non-ATP (Adenosine Triphosphate) competitive inhibitor acrylamide compounds. Besides, the invention also provides a medicine composite of the compounds, anti-tumor application of the compounds, and the like.

This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.

The invention discloses a method for detecting an activity of an endoglycosidase. The method includes providing the endoglycosidase with a substrate of the endoglycosidase and detecting cleavage of the substrate. The method further includes at least partly inhibiting the transglycosidase activity of the endoglycosidase. The transglycosidase activity may be inhibited by chemically modifying the substrate such that transglycosylation of the substrate by the endoglycosidase is at least partly inhibited while the endoglycosidase is still capable of cleaving the substrate. In one embodiment, the substrate comprises an oligosaccharide chain. Compounds and kits suitable for use in a method of the invention are also disclosed. Methods involving competitive inhibitors are also disclosed as are methods for the synthesis of glycosylated substrates involving the transglycosidase activity of an endoglycosidase.