43 results about "Peptide Synthesis technique" patented technology

The invention relates to the technical field of polypeptide synthesis, and particularly relates to a solid synthetic method of semaglutide. The solid synthetic method includes coupling Gly and a resin to obtain a Gly-resin; coupling step by step for the first time an ammonia acid or an amino acid derivative to obtain a first peptide resin the sequence of which is shown as SEQ ID No.1; removing a side chain protective group of Lys; coupling step by step for a second time 2-(2-(2-aminoethoxy)ethoxy) acetic acid, 2-(2-(2-aminoethoxy)ethoxy) acetic acid, Glu and octadecanedioic acid to obtain a second peptide resin; performing pyrolysis; and purifying. The solid synthetic method is simplified in operation step, short in synthetic period, low in cost, reduced in production of waste liquid, low in side products and high in product yield, and is suitable for large-scale production of the semaglutide.

The invention belongs to the technical field of polypeptide synthesis, and especially relates to a synthesis method of semaglutide. The synthesis method comprises following steps; 1, prior coupling oflys26 side chain is carried out; and 2, O-iso-acylated dipeptide is adopted to break the secondary structure of beta-sheet in semaglutide synthesis process effectively so as to avoid polycondensationin polypeptide synthesis process, and then O to N transfer reaction is adopted to convert esterified semaglutide into semaglutide. The method is capable of reducing product synthesis difficulty, avoiding generation of a plurality of impurities, ensuring the product quality of semaglutide bulk drugs, increasing product yield, increasing the scale of single batch semaglutide production, and realizing mass production of semaglutide.

The invention relates to the technical field of polypeptide synthesis, and discloses a method for preparing ularitide. The method includes the following steps that (1) full-protection linear peptide resin is synthesized; (2) splitting is performed to obtain linear peptide; (3) oxidation is conducted to obtain the ularitide; and (4) purification, salt rotation and freeze-drying are carried out to obtain the ularitide competitive product. By the adoption of the method, the process is simple, synthesis difficulty of the ularitide can be lowered, the yield of the synthesized ularitide is high, cost is low, the purity is 98% or above, and popularization is facilitated.

The invention provides high-purity bivalirudin and an industrial preparation method thereof. The preparation method employs solid phase peptide synthesis technology and uses the solvent--ethyl acetate which is convenient to use and recover and has a low price as a washing agent, so reaction yield and product quality are improved, production cost is effectively reduced, and discharge of waste is reduced.

The invention provides a method for preparing thymosin alpha 1 by liquid phase fragment condensation, belonging to the technical field of biochemistry. According to the method, high capacity value (not less than 0.8mmol/g) resin is used as a starting material, firstly, a standard solid phase polypeptide synthesis (SPPS) technology is adopted for synthesizing a high-purity peptide fragments with selected structures, then, a liquid phase condensation technology is adopted for connecting the peptide fragments, and thus, a high-purity (more than 99%) target peptide is obtained. Compared with the solid phase thymosin alpha 1 synthesis technology, the method provided by the invention avoids the problem of low coupling ratio of amino acids behind the 12th position, and greatly improves yield (up to 25-30%) of the thymosin alpha 1; meanwhile, the peptide fragment formed by solid phase synthesis is free from purification, post-treatment technology is simplified, finally, the thymosin alpha 1 is purified by means of high performance liquid chromatography, preparation difficulty is reduced, preparation times is decreased, synthesis cost of the thymosin alpha 1 is lowered, and implementation of large-scale and industrialized production is facilitated.

The invention relates to a method for preparing terlipressin, and belongs to the technical field of polypeptide synthesis. The method comprises the steps that terlipressin peptide resin is synthesized through a fragment condensation method, 3-12 fragments are synthesized through a solid phase method, 1-2 fragments are connected to 3-12 solid phase amino-acid resin, full-peptide resin is obtained, and the terlipressin is obtained after cracking and cyclizing. Due to the fact that Boc-Gly-Cly-OH is adopted as a raw material, lack of glycine impurities is reduced, the operation step of removing glycine protection groups at an N terminal is omitted, product purity is improved, and the total cost is obviously reduced.

A method for synthesizing phenylalanyl-lysine dipeptide belongs to the technical field of peptide synthesis. The method comprises the following steps: preparing an aqueous solution of phenylalanine and lysine from commercially available phenylalanine and lysine, preparing a non-aqueous reaction medium of ethylene glycol, preparing a phenylalanine-lysine dipeptide reaction solution, preparing a resin column for purifying loaded phenylalanine-lysine dipeptide, preparing a phenylalanyl-lysine dipeptide eluent, preparing phenylalanyl-lysine dipeptide freeze-dried powder, preparing an aqueous solution of recovered phenylalanine and lysine, and preparing a regenerated resin column in order to prepare the phenylalanyl-lysine dipeptide with the content being 95-98%. The method using chymotrypsin as a catalyst in the non-aqueous medium of ethylene glycol to synthesize the phenylalanyl-lysine dipeptide has the advantages of mild conditions, high specificity and high synthesis efficiency, and isa typical green production technology; and the phenylalanyl-lysine dipeptide can be widely applied to the fields of medicines, textiles, foods and the like, and has considerable social values.

The invention provides a preparation method of plecanatide, and relates to the technical field of polypeptide synthesis. AM resin or MBHA resin is modified through FMPB, H-Leu-OtBu serves as first amino acid to be coupled to the modified resin, amino acid at sites difficult to connect is modified and then is gradually coupled to the modified resin according to the sequence of plecanatide main chain peptide, so that the synthesis difficulty of plecanatide linear peptide is greatly reduced, and the problems of many impurities, low purity, low yield, amino acid racemization and the like in the existing synthesis are solved. The Cys at sites of 4 and 12 in the sequence are subjected to first oxidation bonding and then subjected to column chromatography coarse purification, so that the purity of the obtained plecanatide is improved; the purification liquid is diluted, and the Cys at the 7-site and the 15-site are subjected to the second oxidation bonding, such that the concentration of thepre-oxidized plecanatide line peptide can be reduced so as to reduce the intermolecular disulfide bond during the second oxidation bonding process, and improve the yield of plecanatide; and further, the operation is simple and convenient, and the method is suitable for industrial production.

The invention belongs to the technical field of solid-phase peptide synthesis, particularly relates to magnetic nanoparticles for solid-phase peptide synthesis, and further discloses a synthesis method of the magnetic nanoparticles and application of the magnetic nanoparticles in preparing magnetic solid-phase carriers. The magnetic nanoparticles are synthesized by subjecting superparamagnetic ferroferric oxide (Fe3O4) particles which are taken as a magnetic core to oleic acid modification and covering the surface of the magnetic core with polystyrene (PS) to form the magnetic nanoparticles which are of core-shell type PS@Fe3O4 structure; further, surface polymer modified magnetic nano-microspheres are obtained by introducing 1-(4-vinyl benzyloxybenzyl alcohol) in the process of covering Fe3O3 with PS. The magnetic nanoparticles have suitable size, have surface chemical adaptability capable of being functionalized, have excellent dispersibility and compatibility in media, and can be used as the magnetic solid-phase carriers in solid-phase peptide synthesis.

The invention provides a fluorescent probe for detecting the C-reactive protein and a preparation method thereof. With the phage display technology, the recombinant phage bound specifically is screened; and sequencing and sequence comparison are carried out by extracting the ssDNA of the recombinant to obtain a CRP-specific affinity ligand sequence. The ligand is synthesized based on the solid phase polypeptide synthesis technology and fluorescent labeling is carried out on the ligand to obtain a fluorescent probe that is specifically bound to the CRP. A fluorescent enzyme label plate is coated with a to-be-detected serum sample and a fluorescent probe with the certain concentration is added, wherein the probe can be bound to the CRP specifically; a fluorescent probe that is not bound is washed by using a proper buffer solution and a fluorescence microplate reader detects the fluorescence intensity, wherein the current fluorescence intensity is controlled by the CRP content in the to-be-detected sample strictly. According to the invention, a novel tool is provided for specific recognition and content detection of CRP. The fluorescent probe no only can qualitatively identify the CRPbut also can be used for quantitative detection.

The invention provides a preparation method of semaglutide and relates to the technical field of polypeptide synthesis. According to the preparation method provided by the invention, amino acid as shown in a formula I or a dipeptide fragment as shown in a formula II is adopted, and through steric hindrance of a raw material structure, polycondensation caused by beta folding in a semaglutide full-protection peptide resin coupling process can be improved, the difficulty of coupling of semaglutide resin is lowered, so that missing impurities, inserted impurities and racemization impurities are effectively avoided. Therefore, the preparation method provided by the invention has the advantages that the quality of a semaglutide crude product can be improved, the yield of the semaglutide is increased, and the preparation method is low in cost, simple to operate and suitable for industrial production.

The invention relates to the technical field of synthesis of polypeptides, in particular to a heating solid-phase synthetic method of polypeptides. In heating solid-phase synthesis of polypeptides, all reactions are performed after temperature is raised to a constant value. Compared with traditional solid-phase synthetic methods of polypeptides, the heating solid-phase synthetic method of polypeptides has greatly shortened reaction time and increased reaction speed; compared with microwave solid-phase synthetic methods of polypeptides, the heating solid-phase synthetic method of polypeptides can gain decreased chances for side effects and increased reaction yield of long-chain polypeptides.

The invention provides a hornet phallotoxin antitone analog WVD-II and a preparation method and application thereof, and belongs to and relates to the technical field of polypeptide synthesis. The amino acid sequence of the hornet phallotoxin antitone analog WVD-II is as shown in SEQID NO:1. The N end of the hornet phallotoxin antitone analog WVD-II disclosed by the invention has positive charges,so that the N end can be combined with a cell membrane having negative electricity; an alpha helical structure is formed from hydrophobic amino acids at a C end, and can bore a hole in the surface ofthe cell membrane, so that death of bacteria is caused. The in vitro antibacterial activity determination indicates that the hornet phallotoxin antitone analog WVD-II disclosed by the invention has significant sterilizing effects on gram-positive bacteria, gram-negative bacteria and fungi, has good stability, is low in hemolytic toxicity and has the characteristics of being broad-spectrum, efficient and safe. The hornet phallotoxin antitone analog WVD-II disclosed by the invention can be used as an active component clinically for replacing traditional antibiotics for treatment.

The invention provides a polypeptide reagent for activating human immune cells. The polypeptide reagent comprises 6-aminopurine, folic acid, glycyl-L-glutamine, L-glutathione, thymopentin, Pp25 and Pp21, wherein Pp25 and Pp21 are prepared by a solid-phase polypeptide synthesis technology.

The invention provides a semaglutide main peptide chain and a preparation method thereof, belongs to the technical field of polypeptide synthesis, and particularly relates to a method for performing condensation coupling on amino acid according to a polypeptide sequence of the semaglutide main peptide chain by taking a self-made polypeptide condensing agent and organic alkali as a condensation coupling system, which is beneficial to improving the coupling efficiency and reducing the generation of impurities. The purity and the yield of the crude peptide are improved, the synthesis cost is reduced, the purification difficulty is reduced, and the purification yield is improved; in the reversed-phase high performance liquid chromatography purification process of the main peptide chain of the semaglutide, a silica gel chromatographic filler modified by 1-pyridine-2-yl-1, 4-butanediamine and epoxy siloxane is used as a filler, so that the purification efficiency is favorably improved.

The invention relates to an inhibitor for regulating breast cancer proliferation and migration based on an SREBP-1/PI3K/AKT signal pathway and application of the inhibitor, the inhibitor is a short peptide, and the short peptide has an amino acid sequence as shown in SEQ ID NO.1. The inhibitor disclosed by the invention can be generated by adopting an existing short peptide synthesis technology, and is low in cost, good in effect, high in safety and high in selectivity.