222 results about "Endopeptidase" patented technology

A compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and / or heart failure. ARB includes S—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate.

The invention concerns a recombinant nucleic acid molecule encoding an antimicrobial fusion peptidoglycan endopeptidase. The recombinant nucleic acid molecule according to the invention is formed from a nucleic acid encoding a bacterial endopeptidase (lysostaphin) from Staphylococcus simulans and a nucleic acid encoding a second endopeptidase (endolysin) module from Group B streptococcal bacteriophage B30. The encoded fusion endopeptidase has antimicrobial activity and kills both Staphylococcus bacteria and Streptococcus bacteria.

Botulinum neurotoxins, the most potent of all toxins, induce lethal neuromuscular paralysis by inhibiting exocytosis at the neuromuscular junction. The light chains (LC) of these dichain neurotoxins are a new class of zinc-endopeptidases that specifically cleave the synaptosomal proteins, SNAP-25, VAMP, or syntaxin at discrete sites. The present invention relates to the construction, expression, purification, and use of synthetic or recombinant botulinum neutoroxin genes. For example, a synthetic gene for the LC of the botulinum neurotoxin serotype A (BoNT / A) was constructed and overexpressed in Escherichia coli. The gene product was purified from inclusion bodies. The methods of the invention can provide 1.1 g of the LC per liter of culture. The LC product was stable in solution at 4° C. for at least 6 months. This rBoNT / A LC was proteolytically active, specifically cleaving the Glu-Arg bond in a 17-residue synthetic peptide of SNAP-25, the reported cleavage site of BoNT / A. Its calculated catalytic efficiency kcat / Km was higher than that reported for the native BoNT / A dichain. Treating the rBoNT / A LC with mercuric compounds completely abolished its activity, most probably by modifying the cysteine-164 residue located in the vicinity of the active site. About 70% activity of the LC was restored by adding Zn2+ to a Zn2+-free, apo-LC preparation. The LC was nontoxic to mice and failed to elicit neutralizing epitope(s) when the animals were vaccinated with this protein. In addition, injecting rBoNT / A LC into sea urchin eggs inhibited exocytosis-dependent plasma membrane resealing.

The present invention discloses a crystalline ARB-NEPi dicationic compound and a preparation method and application thereof. In particular, the present invention relates to the crystalline ARB-NEPi dicationic compound having the formula of NEPi.Nax.Ky.ARB.ZH2O. The present invention also relates to a pharmaceutical composition containing an effective amount of the crystalline dicationic compound and application of the pharmaceutical composition in the preparation of drugs for treatment or prevention of neutral-endopeptidase-related diseases, cardiovascular diseases, hypertension, acute and chronic heart failures, congestive heart failure, left ventricular dysfunction, hypertrophic cardiomyopathy, diabetic cardiomyopathy, supraventricular arrhythmia and ventricular arrhythmia, atrial fibrillation, atrial flutter or detrimental vascular remodeling, and the like, and the pharmaceutical composition has broad application prospects.

The invention relates to glutamine endopeptidase enzymes from Rothia spp. bacteria that are naturally associated with the oral cavity, formulations comprising the glutamine endopeptidase enzymes and the use thereof for the treatment, prevention of allergic reaction and diagnosis of gluten allergy related diseases such as Celiac Sprue, gluten allergy and / or dermatitis herpetiformis.

The invention relates to an improved preparation method of an important intermediate (2R, 4S)-5-(biphenyl-4-yl)-4-tert-butoxycarbonylamino-2-methyl pentanoic acid (that is a compound shown in the formula III) for preparing sacubitril which is a neutral endopeptidase (NEP) inhibitor and of an analog or salt of the intermediate. The method mainly comprises that in the presence of a palladium catalyst, hydrogenation is carried out to make the compound shown in the formula III and having high optical purity and the analog or salt of the compound. The improved method is available in raw materials, mild in reaction condition, and simple and convenient to operate. The product quality is excellent and the cost is low, so that the method is suitable for industrial mass production.