24 results about "Peptide synthesis" patented technology

This invention relates to the field of peptide synthesis technology, specifically to a type of composition containing long-chain alkane for peptide synthesis and a method for preparing peptides. The composition includes peptide synthesis material A and material B; the general structural formula of peptide synthesis material A is Lca-K-L-AA or L... a -AA; where Lca contains long-chain alkyl and / or long-chain alkenyl groups, L is a polypeptide linker that does not contain long-chain alkyl or long-chain alkenyl groups, and K is an organic fragment or group used to link Lca and L; L a The material B is a polypeptide linker containing long-chain alkyl and / or long-chain alkenyl groups, where AA is an amino acid residue or a peptide containing fewer than 10 amino acid residues; the structure of material B contains long-chain alkyl and / or long-chain alkenyl groups. The compositions of this invention are applied to the synthesis of polypeptides, enabling the use of soluble carbon-based supports for solid-phase polypeptide synthesis.

The present invention relates to a Bsmoc protected lysine salt (1 X ) of formula 1 X , for example the hydrochloride salt (n = 1, HY = hydrochloric acid). The present invention also relates to a method for preparing a Bsmoc protected lysine derivative, which method employs a Bsmoc protected lysine salt of formula 1 X and comprises the step of reacting the epsilon-amino group of lysine with an activated carboxylic acid derivative. Some of the obtained Bsmoc protected lysine derivatives with side chain modifications are used as starting materials in solid phase peptide synthesis.

This utility model discloses an inert gas protective stirring system for solid-phase peptide synthesis to prevent aggregation, comprising: a main body and a sealing mechanism. The sealing mechanism includes a stirring tank, a stirring cover installed at the upper end of the stirring tank, a lower abutment block installed at the upper end of the stirring tank, and a sealing strip connected to the upper end of the lower abutment block; and a disassembly mechanism located inside the sealing mechanism. This utility model provides an inert gas protective stirring system for solid-phase peptide synthesis to prevent aggregation. By installing a sealing mechanism inside the main body of the device, it achieves the effect of sealing and isolation while facilitating disassembly and cleaning. By installing a disassembly mechanism inside the sealing mechanism, the threaded block at one end of the stirring rod can be quickly unscrewed and disassembled.

Convergent pathways for the preparation of a peptide by solid phase peptide synthesis or liquid phase peptide synthesis, as well as peptide fragments suitable for use in such pathways, are provided. The convergent pathways may be utilized for the synthesis of agonists of the glucagon-like peptide 1 receptor (GLP-1R) such as the peptide component of maridebart cafraglutide.

This document discloses methods for generating peptides, including liquid-phase peptide synthesis methods in which peptide elongation is carried out in one-pot cycles of one or more. Specifically, this disclosure provides liquid-phase peptide synthesis methods using a solvent system comprising 2-methyltetrahydrofuran for condensation reactions, and aggregation liquid-phase peptide assembly methods in which benzyl alcohol anchor groups are selectively removed from N-protected C-protected peptides via base-catalyzed ester hydrolysis.

The utility model relates to the technical field of polypeptide processing, in particular to a multi-stage circulating filtering device for polypeptide synthesis reaction liquid, and aims to solve the problem that foreign matters easily enter filtering equipment when a filter element is replaced. The multi-stage circulating filtering device comprises a barrel, a through hole is formed in the upper surface of the barrel, and a lifting assembly is arranged above the barrel. Through cooperation of a hydraulic rod, a sealing cover and a first magnetic ring, the first magnetic ring applies pressure to a second magnetic ring, a filter cloth performs preliminary filtration on a reaction liquid, a filter membrane performs secondary filtration on the reaction liquid, and under the cooperation action of the hydraulic rod, the sealing cover and the first magnetic ring, the first magnetic ring drives the second magnetic ring to move out of the cylinder; after the second magnetic ring is detached, the through opening is sealed again, flowing of air inside and outside the cylinder is reduced, the filter membrane and the filter cloth which are replaced are installed and positioned through magnetic adsorption of the first magnetic ring and the second magnetic ring, the installation efficiency is improved, the contact time with the outside is shortened, and the safety of reaction liquid is improved.

The application discloses an internal circulation device for production type polypeptide synthesis, which comprises a reaction kettle and a water jacket covering the reaction kettle, a cavity for filling circulating water is formed between the reaction kettle and the water jacket, a water storage tank for storing the circulating water is further arranged, a heating pipe is arranged in the water storage tank, a water pumping assembly is connected to the water storage tank, a three-way electromagnetic valve is connected to the water pumping assembly, a first water pipe and a bypass pipe are connected to the three-way electromagnetic valve, a water cooler is connected to the first water pipe, a second water pipe extending into the cavity is connected to the water cooler, the bypass pipe is communicated with the side wall of the second water pipe, and a water returning assembly is further connected to the bottom of the cavity, which is used for returning the circulating water in the cavity to the water storage tank, and the device has the advantages that a set of water storage tank can be shared for temperature rising and temperature dropping, and the cost of equipment is reduced.

This invention provides a method for preparing and applying a class of Motixafortide-nitrogen mustard conjugates and their fluorescent probes, belonging to the fields of peptide preparation and biomedicine. This invention utilizes a solid-phase peptide synthesis method to covalently link the DNA alkylating agent nitrogen mustard with the CXCR4 targeting peptide Motixafortide, and further couple it with a fluorescent dye, successfully preparing a series of novel conjugates and their fluorescent probes. Experimental verification shows that the Motixafortide-nitrogen mustard conjugates and their fluorescent probes prepared in this invention can significantly enhance the antitumor activity and targeting of nitrogen mustard to tumor cells. Simultaneously, the rhodamine B-labeled dinitrogen mustard conjugate BCCR exhibits specific targeting of the CXCR4 receptor and dual targeting of the tumor cell nucleus. These conjugates enable real-time tracking of the entire process of tumor targeting, cell delivery, and nuclear localization, providing a powerful tool for efficacy evaluation and mechanism research, thus possessing promising clinical translational prospects and application value.

The invention relates to methods and compositions useful for routing and tracking multiple mobile units within a microfluidic device. Mobile units may be routed through a plurality of chemical environments, and the mobile units may be tracked to determine the path and / or environments that the mobile units have routed through. Mobile units may be routed in accordance with a predetermined algorithm. Mobile units may be routed through microfluidic devices in ordered flow. Mobile units routed through the microfluidic device can be used to perform various chemical reactions uniquely associated to the units, including without limitation peptide synthesis, enzymatic gene synthesis and gene assembly.

Provided is a method for obtaining a polypeptide or protein containing one or more non-proteinogenic amino acids. The method mainly comprises the following steps: 1) activating a dipeptide of the following formula I under acidic or neutral conditions; 2) reacting the activated dipeptide with a polypeptide or protein; and 3) removing a protective group in situ; thereby obtaining a final polypeptide or protein. In the process of synthesizing the polypeptide, by means of activating the dipeptide under acidic or neutral conditions, the DeFmoc phenomenon in a long activation process can be avoided, thereby effectively controlling N-terminal His-Aib insertion peptide impurities, and reducing product loss. The activation of the dipeptide under acidic or neutral conditions provides an activated ester with good stability, resulting in a stable process with sufficient operating time during production, which is conducive to scaled-up industrial production. Moreover, fewer organic solvents such as DMF and acetonitrile are used, and water is used for dilution, thereby lowering costs.

The application provides an amino acid tag, a preparation method thereof and a polypeptide synthesis method. The amino acid tag comprises hydrophobic amino acids; the hydrophobic amino acids comprise phenylalanine and / or proline. The amino acid tag can solve the problem of poor polypeptide synthesis effect in the prior art and is suitable for the field of polypeptide synthesis.

This invention discloses a 96-channel peptide synthesizer and its synthesis method, comprising a reaction system, a solvent management system, and a control system. The reaction system includes a housing, a reaction rack, reactors, a dispensing tower, and amino acid bottles. The housing is equipped with partitions to achieve functional zoning. The reaction rack houses 96 detachable reactors with oscillating stirring capabilities. The amino acid bottles feature quick-release pull-rings and cylinder-operated metering structures. The dispensing tower employs staggered operation for synchronous liquid supply. The solvent management system uses positive nitrogen pressure as its power source and achieves precise solvent delivery through a dispensing pump, transfer bottle, and solvent valve. The control system is fully automated via computer control, capable of monitoring channel status, editing process parameters, and supporting mode switching. This invention achieves high-throughput, automated peptide synthesis with 96 channels, offering advantages such as convenient operation and high synthesis efficiency.

This invention discloses a class of lipid vitamins based on amino acid structures and their synthesis method. The head of the lipid vitamin consists of one or more amino acids, and the tail consists of a hydrophobic vitamin and a fatty acid chain. The molecular weight of the amino acid lipid vitamin is 1000-2000 Da. The synthesis method is a solid-phase synthesis method based on peptide synthesis. First, the carbon terminus of the amino acid is linked to a 2-chlorotriphenylmethyl chloride resin. Then, a condensation-washing-deprotection-washing cycle is performed. Finally, the vitamin and fatty acid chain are coupled at the nitrogen terminus to obtain a class of lipid vitamins based on amino acid structures. The synthesized lipid vitamin is removed from the resin using a lysis buffer, and soluble byproducts in the organic solvent are removed using a non-polar solvent. This method is simple to operate, produces high-purity products, requires fewer complex control factors, and has strong reproducibility.

This invention discloses an enzyme-catalyzed method for the synthesis of nicotinic tripeptide-1 and its derivatives, belonging to the field of biocatalysis and peptide synthesis technology. The method uses nicotinic acid or its active ester and tripeptide-1 (GHK) or its salt as substrates, and carries out an amidation reaction in a non-aqueous phase or an organic solvent system containing a small amount of water, catalyzed by a protease or lipase, to efficiently and selectively synthesize nicotinic tripeptide-1. This method features mild reaction conditions (20-60°C), requires no protection or deprotection of amino acid side chains, has few side reactions, produces high-purity products, is environmentally friendly, and the enzyme can be recycled, significantly reducing production costs and waste emissions, making it suitable for industrial production. The obtained product has broad application prospects in the fields of cosmetics, health products, and pharmaceuticals.

The application discloses a synthetic method of eticaptide, belongs to the technical field of polypeptide synthesis, and particularly relates to a synthetic method of eticaptide. The synthetic method comprises the following steps: taking a polypeptide synthesis carrier as a starting material, sequentially reacting with amino acids to perform coupling, performing cleavage treatment through a trifluoroacetic acid cutting liquid, and then reacting with H-Cys-OH.HCl to obtain eticaptide. The polypeptide synthesis carrier is obtained by the following steps: first, reacting 4,4'-dihydroxybenzophenone with a halogen compound, then performing reduction treatment, then reacting with ethyl carbamate, and finally performing sodium hydroxide treatment. The halogen compound is selected from C10-30 straight-chain or branched-chain alkanes containing halogen substituents, wherein the halogen is bromine, chlorine, fluorine or iodine. The eticaptide prepared by the synthetic process has high yield and high purity, the synthesis efficiency and the purification efficiency of the eticaptide are significantly improved, and the eticaptide has a good application prospect.

The application belongs to the technical field of polypeptide synthesis equipment, and discloses a multi-channel synthesizer and a synthesis method thereof. The synthesizer comprises a body, a synthesis operation cavity and a reagent storage and transportation cavity are independently arranged in the body through physical isolation, a reaction system comprising a plurality of independent swing reactors, a common metering and transferring unit, and a corresponding number of activation bottles corresponding to the reactors are arranged in the synthesis operation cavity, and an amino acid solution supply unit is arranged at the upper portion; reagent storage and transportation cavities are centrally arranged with DMF, DCM, piperidine, condensation reagent, methanol and other storage bottles, two independent nitrogen positive pressure conveying paths are adopted: the first path is connected with amino acids, condensation reagents, a metering activation system and a reaction system, and is specially used for precise metering, mixing and adding of the condensation reaction; the second path is connected with various types of washing and deprotection reagent storage bottles and the reaction system, and is used for direct and rapid adding. The synthesis process is optimized, the cross contamination and reagent evaporation risk are significantly reduced, and the efficiency and reliability of multi-channel parallel synthesis are improved.

Provided are crystalline forms of peptide fragments, method of preparation thereof, and use thereof for preparing peptides. The present crystalline compounds may be employed as intermediates with improved purity and physical properties for peptide syntheses.

The application discloses a method for continuously and enzymatically synthesizing a fragment of retaspimautide, a micro-reaction system and a method for preparing immobilized enzymes, and belongs to the technical field of polypeptide synthesis. The method comprises fragment splitting, substrate preparation, continuous flow enzymatic coupling, online monitoring and purification. The micro-reaction system comprises raw material conveying, modular micro-reaction, online monitoring and other modules, and realizes continuous and automatic synthesis. The immobilized enzyme adopts macroporous silica gel as a carrier and is prepared through pretreatment, covalent binding and post-treatment. The application combines the advantages of continuous flow and enzymatic synthesis, improves the purity of the product to more than 95%, shortens the synthesis time, reduces the production cost, reduces environmental pollution, is easy to scale up, and solves the problems of low efficiency and poor purity in the prior art.

This application relates to a peptide synthesizer using tandem resin reactors. This document teaches a solid-phase peptide synthesis (SPPS) apparatus and a method for manufacturing peptides using it. The system comprises at least two reactors, each containing a specific amount of SPPS resin. These reactors are arranged in series. A deprotecting agent is added to the first reactor and then sequentially transferred to the second and third reactors, thereby deprotecting the protected N-group. A washing solvent is added to the first reactor and then transferred to the second reactor, and this operation is repeated several times. Similarly, an amino acid-activated ester solution is sequentially added to the first, second, and third reactors, thereby coupling the amino acid to the deprotected N-group. A washing solvent is added to the first reactor and then transferred to the second reactor, and this operation is repeated several times before the next cycle. The use of tandem reactors reduces the total solvent required. Online LCMS is also used to monitor the progress and properties of the reactions occurring within the solid-phase resin particles.

This invention provides a supramolecular polypeptide hydrogel with ferroptosis reversal function and its application. The supramolecular polypeptide hydrogel is formed by the self-assembly of polypeptide FRC through intermolecular non-covalent interactions. The amino acid sequence of polypeptide FRC is shown in SEQ ID NO.1. This invention uses a solid-phase peptide synthesis method to obtain a novel polypeptide FRC with highly efficient ferroptosis reversal activity. It can significantly reduce ROS levels, upregulate GPX4 expression, and enhance the antioxidant capacity of cardiomyocytes, thereby effectively inhibiting cardiomyocyte ferroptosis under oxidative stress. Simultaneously, polypeptide FRC can self-assemble into a supramolecular polypeptide hydrogel through intermolecular non-covalent interactions, allowing direct injection into the myocardial injury site. Utilizing the sustained-release properties of the hydrogel, the drug can be released for a long time, requiring only a single injection to continuously reverse the ferroptosis process, significantly reducing tissue damage and improving cardiac function, providing a new strategy for the development of related drugs and formulations.

Lipid modifications can be used to improve the pharmacokinetic profile of therapeutic peptides. Provided herein are compounds and methods useful in the preparation of peptides comprising one or more lipidated lysine resides. The compounds provided herein can be used in the preparation of lipidated peptides via peptide synthesis (e.g., solid phase peptide synthesis (SPPS) or liquid phase peptide synthesis (LPPS)).

This invention relates to the field of peptide synthesis technology, and in particular to a method for preparing atosiban acetate, comprising: swelling an amide resin and then removing Fmoc protection to obtain an amide resin with deprotected Fmoc; activating Fmoc-Gly-OH and coupling it with the deprotected amide resin, followed by deprotection; then, sequentially activating, coupling, and deprotecting the remaining amino acid monomers according to the atosiban amino acid sequence from C-terminus to N-terminus to obtain a linear atosiban resin; pyrolyzing and post-processing the linear atosiban resin to obtain crude linear atosiban; and subjecting the crude product to a cyclization reaction and post-processing to obtain atosiban acetate. The method provided by this invention is simple to operate, leaves no harmful residues, and can stably prepare high-purity products, making it suitable for industrial production.

This application discloses a peptide synthesizer with an automatic lid-opening function, including a tank and an opening / closing module. One end of the opening / closing module is hinged to the tank, and the other end is hinged to a sealing lid for closing the tank. A sealing ring is also provided on the sealing lid. A rotating module is also provided on the tank, and a rotating locking module, powered by the rotating module, is provided between the tank and the sealing lid. The rotating module controls the rotating locking module to rotate around the tank to push the sealing lid to close and compress the sealing ring. Compared with the prior art, this application achieves automatic closing and opening of the sealing lid, minimizing the labor intensity and improving disassembly and assembly efficiency. Furthermore, there are no connecting bolts between the tank and the sealing ring in this application; therefore, the installation and opening of the sealing lid can be achieved through the movement controlled by the opening / closing module and the rotating module, eliminating the need for frequent installation and removal of bolts and other structural components, thus improving disassembly and assembly efficiency.