5 results about "Wang resin" patented technology

This invention belongs to the field of biomedical technology and relates to the application of YMRFamide short peptide in anti-inflammation. The amino acid sequence of the YMRFamide short peptide is Tyr-Met-Arg-Phe. This invention provides a complete solid-phase synthesis and purification method for this peptide, including using Fmoc-Phe-Wang resin as a starting material, sequentially linking arginine, methionine, and tyrosine, followed by deprotection, resin cleavage, and activated carbon-ethanol crystallization purification steps to finally obtain a high-purity YMRFamide short peptide. The preparation process of this invention is simple, efficient, and reproducible, with significantly improved product stability and solubility. The YMRFamide short peptide exhibits multi-pathway anti-inflammatory potential, is expected to effectively regulate the expression of inflammatory factors, and has high biocompatibility and good safety, providing an important candidate molecule for the development of novel anti-inflammatory drugs.

The application discloses a synthesis method of phosphorodiamidate morpholino oligonucleotide, belongs to the technical field of solid-phase synthesis of phosphorodiamidate morpholino oligonucleotide, and specifically relates to the following steps: adding 9-fluorenylmethyloxycarbonyl-piperazine-succinic acid into Wang resin to mix and react to synthesize 9-fluorenylmethyloxycarbonyl-piperazine-succinic acid-Wang resin, then adding phosphoramidite monomers to perform coupling reaction after deprotection treatment, performing cap treatment after the coupling is completed, then repeatedly performing deprotection treatment, coupling reaction and cap treatment until the coupling of all phosphoramidite monomers is completed, then removing the protecting group of the last phosphoramidite monomer, and then performing cleavage treatment and deprotection treatment of a base protecting group to obtain a phosphorodiamidate morpholino oligonucleotide (PMO) reaction solution. The application provides a synthesis method of phosphorodiamidate morpholino oligonucleotide with high coupling efficiency, low impurity level, high yield and high purity.

Provided is a method for preparing lutetium[177Lu]dotatate and a precursor compound thereof, comprising performing coupling reactions on Fmoc-Thr(tBu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Thr(tBu)-OH, Fmoc-Lys(Boc)-OH, Fmoc-D-Trp(Boc)-OH, Fmoc-Tyr(tBu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-D-Phe-OH, and DOTA-(tBu)3-CO2H successively on a Wang resin by means of a solid-phase synthesis method to obtain DOTA-(tBu)3-D-Phe-Cys(Trt)-Tyr(tBu)-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(tBu)-Wang resin, performing an oxidation reaction to remove Trt protecting groups from two Cys residues and form a disulfide bond therebetween, thus achieving cyclization, and then performing a cleavage reaction to remove the Wang resin and protecting groups to obtain a lutetium[177Lu]dotatate precursor compound represented by formula I. The preparation method can significantly improve the purity of the prepared lutetium[177Lu]dotatate precursor compound, reduce the impurity content, improve the product yield, and simplify the subsequent purification process.

The invention provides an AOD-9604 polypeptide synthesis method, which comprises: (1) dispersing Fmoc-Phe-OH and Wang resin in a solvent, adding pyridine and 2, 6-dichlorobenzoyl chloride, carrying out a reaction, carrying out suction filtration, washing, and terminating with acetic anhydride to prepare Fmoc-Phe-Wang resin; (2) sequentially coupling amino acids by adopting a solid-phase synthesis method to obtain peptide resin; (3) adding the peptide resin into a lysis solution, reacting, and carrying out solid-liquid separation to obtain a filtrate; adding the filtrate into methyl tert-butyl ether, centrifuging to remove supernate, adding the obtained solid into methyl tert-butyl ether, pulping to suspend, centrifuging, repeating the operation twice, removing supernate, and drying the obtained solid to obtain a linear peptide crude product; and (4) dissolving the linear peptide crude product with a mixed solvent of water, acetic acid and dimethyl sulfoxide, adding water for dilution, adding an oxidizing agent to oxidize and bridge the disulfide bond, reducing with VC to obtain an AOD-9604 polypeptide crude product, and performing reverse preparation and freeze-drying to obtain the AOD-9604 polypeptide. The purity of the solid-phase synthesized simple linear peptide is 86% or above, the cost is low, and side reactions can be controlled.

The present application relates to the technical field of biological medicine, and particularly discloses a novel polypeptide drug targeting specific PPI sites and a preparation and treatment application method thereof.The novel polypeptide drug is prepared by a solid-phase synthesis method, and the specific steps are as follows: resin activation: Fmoc-Gly-Wang resin (degree of substitution: 0.3-0.8 mmol / g) is placed in a solid-phase synthesis reaction column, soaked in N,N-dimethylformamide (DMF) for 20-30 minutes, the resin is fully swelled, then the resin is washed with DMF for 3 times, each time for 5 minutes, and the resin activation is completed; deprotection: 20% piperidine / DMF solution is added to the reaction column, reacted at room temperature for 15-20 minutes, the Fmoc protective group is removed, then the reaction column is washed with DMF for 6 times, each time for 5 minutes, and the residual piperidine is removed.The novel polypeptide drug has high specificity and high affinity, can accurately recognize and combine target proteins, and has the beneficial effects that: high specificity and high affinity: the novel polypeptide drug of the present application is combined with specific PPI sites through various chemical bonds (hydrogen bond, hydrophobic interaction, electrostatic interaction), has extremely high specificity and affinity, and can accurately recognize and combine target proteins.