244 results about "Enzyme inhibition" patented technology

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.

Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

The invention discloses application of CRISPR / nCas9 mediated site-directed base substitution in a plant. The invention provides a plant genome site-directed edition system. The system comprises a BE3 plant expression carrier (expressing a fusion protein composed of nCas9(D10A), deaminase and a uracil DNA glycosylase inhibitory protein), and rice OsPDS and OsSBEIIb are taken as target genes for verifying the system. Results show that an expected site-directed mutant plant is respectively obtained in the three selected target spots, accurate site mutation of a base is realized in rice, and the highest efficiency reaches about 20%, so that a feasible and effective base substitution method is provided for crop breeding, the method has strong application potential in the aspect of agricultural breeding, and a foundation is provided for rapidly improving important agronomic traits of crops.

The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and / or dosing purposes.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.

The invention provides a full-automatic and high-throughput micro-fluidic chip system and method for detecting pesticide residue, used for field detection of pesticide residue based on enzyme inhibition reaction. The full-automatic and high-throughput micro-fluidic chip system is mainly composed of a portable analytical detector and a disposable micro-fluidic chip; the plastic polymer material of the micro-fluidic chip is manufactured through existing micro-machining technology; the micro-fluidic chip is composed of a central clamping groove, an extraction chamber, a sample chamber, a reaction chamber, a detection chamber, a micro-groove, a micro-hole and a quality control bar code; reagents (comprising an extracting solution, enzyme, a colour developing agent and the like) required for detecting pesticide residue are fixed in the micro-fluidic chip; the functions of sampling automatically and quantitatively, distributing a fluid, carrying out biochemical reaction and molecular recognition and the like can be realized; a fluid operation and control module, a photoelectric detection module, a data analyzing and processing module and an information storage and communication module are integrated in the portable analytical detector; operation and control of biochemical reaction in the micro-fluidic chip and rapid analysis and detection of to-be-detected indexes and pesticide residue can be realized; and thus, the micro-fluidic chip system and the method provided by the invention are particularly applied to full-automatic and high-throughput detecting and screening of pesticide residue in the samples, such as fruits, vegetables, soil and water.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and / or dosing purposes.

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

The compounds of the present invention relate to chain-extended and chain-modified analogues of salacinol, including embodiments where the sulfate moiety has been substituted with a carboxylate or phosphate moiety. In other embodiments the sulfate moiety has been shifted by one carbon atom in the zwitterionic structure. In another embodiment the polyhydroxylated side chain may be replaced with a lipophilic alkyl chain and a suitable counterion. The invention also encompasses methods for synthesizing the salacinol analogues and using the analogues for enzyme inhibition applications.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

The invention provides a metal organic framework Uio-66-based photoelectric sensor for detecting the activity of protein kinase. The photoelectric sensor constructed through replacing a precious metal by a metal organic framework is provided for the first time, and comprises a conductive electrode coupled with a polypeptide, and a metal organic framework arranged on the conductive electrode, wherein the metal organic framework is loaded with a photoresponse substance; the metal framework can be specifically bound to a phosphorylated polypeptide; and the polypeptide undergoes a phosphorylation reaction in the presence of the activity of a biological enzyme to be detected and adenosine triphosphate (ATP). Photoelectric current changes with the activity of the protein kinase in visible lights, so super-sensitive and highly-accurate detection of the activity of the kinase is realized. The sensor has very high sensitivity; and enzyme inhibition experiments show that the sensor realizes efficient and sensitive detection of the activity of the kinase PKA, and meets use requirements under extremely severe conditions.

The present invention discloses a photoelectric sensor for detection of kinase activity on the basis of local area surface plasma resonance. The biosensor is prepared as follows: a semiconductor material metal oxide is modified onto an indium tin oxide electrode (ITO), then Kemptide, PKA, and a probe are assembled onto the electrode layer by layer, since the probe contains noble metal nanoparticles and photosensitizer tris (bipyridine) ruthenium, under visible light irradiation, the photosensitizer tris (bipyridine) ruthenium captures more photons, local area surface plasma resonance effect of the noble metal nanoparticles occurs under photon excitation, so that more electrons jump onto a semiconductor metal oxide conduction band to produce photocurrent. The biosensor quantitative detection is based on that different concentrations of PKA cause different extents of phosphorylation of Kemptide, so that the amount of the probe connected to the modified electrode is also different, and photocurrent changes are caused. The method has high sensitivity and selectivity, enzyme inhibition experiments also show that the method achieves the purpose of efficient and sensitive detection of the kinase PKA activity.

Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least one of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Met, and KDR kinases in animals, including humans, for the treatment and / or prevention of various diseases and conditions such as cancer.

The invention relates to a processing method for sterilization and enzyme-inhibition of non-thermal fruit vegetable condensed juice, which is characterized in that the fruit and vegetable juice is prepared by high-tension pulse electric field sterilization technology and freeze concentration process, viz. the fresh fruit and vegetable juice is processed by the steps of 1) at room temperature, making the juice flow across a high-tension pulse electric field with electric field intensity not less than 10kv / cm, pulse number not less than 10, pulse width not less than 2mus and no more than 100mus, for sterilization; 2) freeze concentration of the processed fruit and vegetable juice at the temperature below 0DEG C. The invention employs high-tension pulse electric field sterilization technology and freeze concentration process, wherein microorganism is effectively killed and partial enzymes in fruit and vegetable juice are deactivated by using the high-tension pulse electric field sterilization technology firstly at room temperature, and then activity of enzyme is inhibited by freeze concentration process, said two processes are carried out at lower temperature, thereby implementing sterilization and enzyme-inhibition, and solving the problem of juice quality reduction caused by thermal method.

The invention discloses a method for detecting pesticide residues in sulfur-containing vegetables by an enzyme inhibition method. The method comprises the following steps of 1, preparing a standard solution, 2, preparing a sample, 3, testing control groups through the processes of adding a buffer solution into a beaker, adding dropwisely acetate or sodium hydroxide into the beaker, adjusting a pH value of the mixed solution to a pH value of 9, adding an enzyme solution and a color-developing agent into the mixed solution with a pH value of 9, shaking up, standing at a temperature of 37 DEG C for 15 minutes, adding a substrate solution into the mixed solution treated by the previous step, shaking up, and detecting an absorbance variation value delta A0 of the mixed solution undergoing a reaction at wavelength of 410 nanometers for 3 minutes by a spectrometer, 4, adding sulfur-containing vegetable sample extract into a beaker, carrying out processes same as the processes of the step 3, and detecting an absorbance variation value delta A1 of a vegetable sample mixed solution undergoing a reaction at wavelength of 410 nanometers for 3 minutes by a spectrometer, and 5, calculating an enzyme inhibition percentage according to a formula of an enzyme inhibition percentage=[(delta A0-delta A1) / delta A0]*100, wherein when the calculated enzyme inhibition percentage is great than or equal to 50%, it is shown that there are pesticide residues in the detected sulfur-containing vegetable. The method eliminates the interference of sulfides in a sulfur-containing vegetable on pesticide residue detection through adjustment of a pH value of a vegetable sample solution, can rapidly, simply and accurately detect a pesticide residue ratio of a sulfur-containing vegetable, has a low cost, and is suitable for on-site detection.

The invention discloses a paper-based micro-fluidic system and method for detection of pesticide residues. The paper-based micro-fluidic system is composed of a paper-based micro-fluidic chip, a three-electrode system and a data collection device, wherein a substrate and a pesticide extract liquid are injected into the paper-based micro-fluidic chip; a detection signal is transmitted to the data collection device through the three-electrode system; and the pesticide residue detection result is rapidly obtained on the basis of an enzyme inhibition principle. The paper-based micro-fluidic system is simple and convenient to operate; the automatic degree of an enzyme inhibition method detection process is improved; meanwhile, the cost is greatly reduced by use of a paper-based material; and the paper-based micro-fluidic system and the method can be applied to rapid and automatic field detection of the pesticide residues in samples such as fruits and vegetables, soil and water bodies.

The invention discloses a Fuc3S4S substituted oligo-glycosaminoglycan with the weight-average molecular weight of about 4.5-9kD, a medicine composition containing the Fuc3S4S substituted oligo-glycosaminoglycan, preparation methods thereof and an application thereof in preparing medicines for preventing or treating thrombotic diseases. The oligo-glycosaminoglycan has a structure shown as the formula (I); in the formula (I), a substituent group is defined as the specification. The Fuc3S4S substituted oligo-glycosaminoglycan and the medicine composition thereof have strong-effect factor X enzyme inhibition activity and HC-II depended antithrombase activity, and can be used for preparing antithrombus medicines.

The invention belongs to the field of medicinal chemistry, and discloses a pyrimidine and triazole containing compound and a preparation method and application thereof in preparation of anti-cancer medicine with lysine specific demethylase 1 (LSD1) being a target. The general formula of the compound is shown in the drawing I. In-vitro LSD1 enzyme inhibition activity experiments prove that by inhibiting LSD1 activity, the compound has obvious inhibiting and killing effects on kinds of cancer cells and can be applied to preparation of the anti-cancer medicine as a further developed lead compound.

The invention belongs to the technical field of food and provides a fresh-keeping technology of cleaning, crispy-keeping, alkaline solution and microwave enzyme inactivation, and vacuum packing of leafy vegetables. The technology has the characteristics that the microwave technology is adopted; the enzyme inactivation effect is good; the inactivation rate of peroxydase can reach 96.8%; the physical appearances of vegetables are better preserved; and the loss of nutrient substances like vitamin c is less. The technology has the advantages that the detect is overcome that when the leafy vegetables are blanched by conventional hot water for a short time, the enzyme inhibition rate is low; the defect is overcome that when the leafy vegetables are blanched by hot water for a long time, the vegetables soften and turn yellow, and the loss of the nutrient elements of vegetables is great; and the alkaline solution and microwave blanching is adopted, so that the thorough inactivation of chlorophyllase is realized, green preserving process can be simplified, and the problem that heavy mental is left over in green preserving liquid is solved.

The invention provides a novel herbal composition containing the extracts of the leaves and / or stem of <italic>Argemone mexicana < / highlight>plant, optionally containing the extracts of the fruits of <italic>Cuminum cyminum< / highlight>, which exhibits useful in vitro, in vivo and interesting immunological and pharmacological activities; a process for preparation thereof; and a method of treatment of psoriasis and related immunological and biological disorders by administration of the said novel herbal composition. The useful in vitro, in vivo and interesting immunological and pharmacological activities exhibited by the extracts and fractions of the leaves and / or stem of <italic>Argemone mexicana < / highlight>plant include immunosuppression, lymphoproliferation inhibition, cytokine modulation such as IL-2 inhibition, IFNgamma inhibition, IL-10 induction, keratinocyte proliferation inhibition, keratolytic activity, endothelial cell proliferation inhibition, inhibition of cell adhesion molecule expression such as ICAM-1, MEST inhibition, and enzymes inhibition such as p60src Tyrosine kinase, which are known to be involved in anti-psoriatic activity. The novel herbal composition(s) is useful in the treatment of various disorders, such as psoriasis including plaque psoriasis, gutatte psoriasis, pustular psoriasis and psoriasis of the nails; dermatitis and scleroderma; eczema; inflammatory disorders and other autoimmune diseases like psoriatic arthritis, rheumatoid arthritis, Crohn's disease, multiple sclerosis, irritable bowel disease, ankylosing spondilitis, systemic lupus erythremetosus and Sjogren's syndrome; allergies like asthma and chronic obstructive pulmonary disease and is safe, well-tolerated, non-toxic, with minimal and reversible adverse reactions or side effects, and most importantly, with minimal relapse or recurrence of the disease following completion of a treatment regimen. The invention also describes the presence of phosphodiesterase (III, IV and V) inhibition and 5-Lipoxygenase inhibition in the aqueous, ethanolic or aqueous-ethanolic extracts of fruits of <italic>Cuminum cyminum < / highlight>plant.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.