65 results about "Peptide drug" patented technology

The invention belongs to the technical field of biological medicine, and relates to an oral peptide drug delivery system based on a soybean trypsin inhibitor and core-shell hydrogel, the oral peptide drug delivery system comprises therapeutic polypeptide, KTI and a core-shell structure gel matrix, and the problems that an existing oral peptide delivery system is passively protected and drug burst release is remarkable are solved. A chitosan / sodium tripolyphosphate ionic cross-linked network forms an inner core, a sodium alginate / calcium ion'egg box 'structure cross-linked network forms a shell, and therapeutic polypeptides such as liraglutide and KTI are jointly embedded. Through the pH response characteristic and sequential release design of the core-shell structure, KTI is preferentially and rapidly released in the intestinal environment to inhibit local protease activity, then therapeutic polypeptide is slowly released, and active protection and synergistic interaction are achieved. The invention further provides a specific preparation method and parameters. The polypeptide has the advantages of stable structure in a gastric acid environment, targeted release in intestinal tracts, high encapsulation efficiency, capability of avoiding burst release and the like, and provides a new strategy for efficient delivery of oral polypeptide drugs.

This invention provides an application of the peptide Nod-T3 in the preparation of drugs for treating lung diseases. The Nod-T3 peptide is derived from human protein and has a significant inhibitory effect on chronic lung inflammation and fibrosis caused by smoking. It can be used to treat COPD and other smoking-related lung diseases. It also has high biocompatibility and low toxicity, and has the potential and development value to become a new type of peptide drug.

A peptide sequence mimicking endogenous cofilin-1 incorporates transmembrane amino acid sequences to enhance cellular uptake of the peptide drug. When cofilin peptide drugs are introduced into cancer cells, they affect cancer cell migration and invasion abilities. Furthermore, the peptide sequence can be conjugated with a chelator for cancer diagnosis.

This invention discloses a GLP-1 peptide drug microneedle and its preparation method. The microneedle is composed of PVP, NVP, a photoinitiator, and a GLP-1 receptor agonist. The preparation method includes two steps: material preparation and peptide microneedle patch preparation. First, a certain amount of PVP is dissolved in NVP to prepare a solution with appropriate specific gravity and viscosity. Then, the photoinitiator and GLP-1 receptor agonist are added to the solution to form a liquid system that is as uniformly suspended as possible. Second, the suspension is filled into a microneedle mold, and NVP is polymerized into solid PVP by ultraviolet light irradiation. Under the constraint of the mold, the solid PVP forms the geometric shape of the microneedle. Subsequently, a small amount of NVP is spread evenly on the backing layer of the microneedle and covered with a plastic film. Ultraviolet light irradiation is applied again to crosslink the plastic film with the PVP microneedle, and the microneedle is then peeled out of the mold. The advantage of this application is that it uses PVP to prepare an NVP solution with suitable specific gravity and viscosity, so that the subsequently added drug is uniformly suspended in the solution, thereby improving the uniformity of drug loading on microneedles and increasing the drug loading capacity, which is beneficial to improving the efficacy and consistency of drug efficacy.

This invention discloses a selenylamide-based hydrogenation reaction of acetylacetamide compounds and its application in the modification of selenium-containing peptides and proteins, belonging to the fields of organic chemistry and chemical biology. The reaction involves the reaction of a selenium-containing compound with an acetylacetamide compound in a solvent with the addition of an additive. The applications of this reaction include: 1) selective modification and labeling of selenocysteine ​​in peptides and proteins; 2) cyclization reactions of selenium-containing peptides and selenoproteins; and 3) sequential modification of selenium-containing peptides in the presence of cysteine ​​by precise pH control combined with the hydrogen sulfide reaction of acetylacetamide. This reaction has advantages such as mild conditions, simple operation, fast reaction rate, high yield, good stability, and good selectivity. It provides a new and robust approach for the selective modification and labeling of selenium groups in bioconjugations, peptides, and / or proteins, and also provides a new method for the construction of cyclic peptides, offering a powerful tool for the development of selenium-containing peptide drugs.

The application discloses a polypeptide for targeted recognition of a neuroendocrine tumor marker INSM1 and products and applications thereof, and belongs to the fields of molecular imaging and protein polypeptide drug engineering. Specifically, the application relates to development of a polypeptide with high affinity and specificity to a neuroendocrine tumor marker insulinoma-associated protein 1 (INSM1). The application discloses an amino acid sequence of the polypeptide and related applications. The polypeptide is used for labeling and preparation of a polypeptide probe, can be specifically combined with the INSM1 protein, and can be used for in-vivo and in-vitro imaging of neuroendocrine tumors, so as to overcome a diagnosis difficulty caused by a hidden onset of the neuroendocrine tumor and realize early positioning and qualitative diagnosis.

Provided, as an anti-SARS-CoV-2 peptide drug, is an optimal salt form of a peptide that binds to a receptor-binding domain (RBD) in SARS-CoV-2.　A sodium or potassium salt of a peptide according to the present invention has, in a direction from an N-terminus to a C-terminus, a first region including a first helix and a second region including a second helix. The first region and the second region each include a site that binds to a receptor-binding domain (RBD) in SARS-CoV-2. A bond is formed between amino acid residues within five residues on the N-terminus side in the sequence of the site that binds to the receptor-binding domain (RBD) in SARS-CoV-2 in the first region and amino acid residues within five residues on the C-terminus side in the sequence of the site that binds to the receptor-binding domain (RBD) in SARS-CoV-2 in the second region, and the peptide binds to the receptor-binding domains (RBD) in SARS-CoV-2.

The application relates to the technical field of biological medicine, and particularly provides a pharmaceutical composition containing a peptide drug active molecule and an application thereof. The pharmaceutical composition comprises a peptide drug active molecule and a drug delivery molecule, and the weight ratio of the peptide drug active molecule to the drug delivery molecule is 1:(1-500); the drug delivery molecule is selected from a structure as shown in formula (I) or a pharmaceutically acceptable salt thereof. The application provides an application of the pharmaceutical composition in preparing an oral dosage form drug. The peptide drug active molecule is significantly improved in stability and permeability in a gastrointestinal fluid by being compounded with the drug delivery molecule, so that gastrointestinal absorption of the peptide drug active molecule is increased and oral bioavailability of the peptide drug active molecule is improved.

This invention relates to a non-natural methionine and its synthesis method, using inexpensive and readily available transition metals as catalysts. N Using arylglycine, styrene compounds, and disulfides as raw materials, a series of non-natural methionine compounds were obtained with high selectivity and high yield through a three-component reaction under mild conditions. The compounds prepared in this invention are multifunctional non-natural methionine derivatives, representing a novel class of natural methionine derivatives. They can be used in drug modification, biosensor fabrication, and other fields, possessing significant research and application value and providing new synthetic strategies for the preparation of novel peptide drugs.

The invention belongs to the technical field of polypeptide drugs, and particularly relates to an anti-tumor polypeptide and application thereof. According to the preparation method, Rink amide MBHA amino resin is taken as a solid phase carrier, modification and transformation are carried out according to an amino acid sequence of a template polypeptide H-0 (hymenochirin-1Pa): Ac-LKLSPKTKDTLKKVLKGAIKGAIAIASAMA-NH2, and on the basis that key amino acid residues are reserved, original amino acids are replaced by S5 at the positions of i and i + 4 amino acids, so that the target stapling peptide is obtained. Pharmacological experiments show that the synthesized stapled peptide can significantly inhibit growth and proliferation of tumor cells of liver cancer, lung cancer, glioma and colon cancer, and has an application prospect of being developed into a novel anti-cancer drug.

A peptide sequence mimicking endogenous cofilin-1 incorporates transmembrane amino acid sequences to enhance cellular uptake of the peptide drug. When cofilin peptide drugs are introduced into cancer cells, they affect cancer cell migration and invasion abilities. Furthermore, the peptide sequence can be conjugated with a chelator for cancer diagnosis.

The embodiment of the application discloses an AI+physical hybrid evaluation method based on combination modeling and consistency scoring for short peptide screening. The method firstly constructs a target database based on a large language model, and prepares a short peptide candidate library from natural sources; then a variety of advanced structure prediction models are used to model the short peptide-target protein complex, generating multiple candidate structures; the prediction results are preliminarily screened through an inter-model consistency scoring mechanism; the high-confidence complexes are verified for binding stability through molecular dynamics simulation; finally, multiple indexes such as structure confidence, consistency score and simulation stability are fused, and the weight is optimized through a machine learning model to realize comprehensive evaluation. Experiments show that the method can significantly improve the success rate of screening of potential active short peptides, and the accuracy on an independent test set is improved by about 5% compared with a single model, and has the advantages of multi-model complementation, high prediction reliability and reliable physical verification, and can be widely applied in the fields of modernization of traditional Chinese medicine, development of functional food and research and development of short peptide drugs.

This invention belongs to the field of peptide drugs, specifically relating to an anti-drug-resistant bacterial peptide and its application in pharmaceutical manufacturing. Using Rink amide MBHA amino resin as a solid-phase support, the amino acid sequence of the template peptide raniseptin PL:Ac-GVFDTVKKIGKAVGKFALGVAKNYLNS-NH2 was modified, with amino acid residues 9I and 16F replaced by R8 and S5, respectively, to obtain the target stapling peptide PL-11. Compared to the template peptide PL-0, the stapling peptide PL-11 significantly enhances the antibacterial activity against Staphylococcus aureus, Enterococcus faecalis, and Staphylococcus epidermidis.

The disclosure provides, inter alia, formulations for drug delivery, such as extended release of peptide therapeutics.

This invention belongs to the field of peptide drugs, specifically relating to an anti-drug-resistant bacterial peptide and its application in pharmaceutical manufacturing. Using Rink amide MBHA amino resin as a solid-phase support, the amino acid sequence of the template peptide raniseptin PL:Ac-GVFDTVKKIGKAVGKFALGVAKNYLNS-NH2 was modified, with amino acid residues 6V and 13V replaced by R8 and S5, respectively, to obtain the target stapling peptide PL-10. Compared to the template peptide PL-0, the stapling peptide PL-10 significantly enhances the antibacterial activity against Staphylococcus aureus, Enterococcus faecalis, and Staphylococcus epidermidis.

Problem The purpose of the present invention is to provide a novel method for prevention and / or treatment of opioid tolerance or opioid dependence. Specifically, the purpose of the present invention is to develop peptide-based blockers to block MOR-DOR and KOR-DOR heterodimerization. In addition, the purpose of the present invention is to develop homodimer blockers for MOR, DOR, and KOR which modulate their downstream signaling without affecting their internalization. Solution The present invention is a prophylactic and / or therapeutic agent for the prevention and / or treatment of opioid tolerance or opioid dependence comprising the peptide which inhibits the dimer formation of the opioid receptor, wherein the above opioid receptor dimer is a heterodimer or a homodimer formed from one or two opioid receptors selected from the group consisting of the μ type (MOR), the κ type (KOR), and the δ type (DOR).

The invention generally refers to a compound as shown in a formula (I): formula (I); wherein L1, L2, LD1, LD2, R5 and R6 are defined in the specification. The invention provides pharmaceutical compositions encompassing such compounds and methods of treating cancer using complexes of the compounds.

Methods of treating ocular diseases such as age-related macular degeneration may include the administration of peptides comprising complement factor H and factor H-like protein domains to reduce an amount of geographic atrophy in a subject in need thereof. These methods may be administered by intraocular, intervascular or subcutaneous injection.

This invention belongs to the field of peptide drugs, specifically relating to an antibacterial peptide and its application in pharmaceutical manufacturing. Using Rink amide MBHA amino resin as a solid-phase support, the amino acid sequence of the template peptide raniseptin PL:Ac-GVFDTVKKIGKAVGKFALGVAKNYLNS-NH2 was modified, with amino acid residues 13V and 20V replaced by R8 and S5, respectively, to obtain the target stapling peptide PL-13. Compared to the template peptide PL-0, the stapling peptide PL-13 significantly enhances the antibacterial activity against Staphylococcus aureus, Enterococcus faecalis, and Staphylococcus epidermidis.

GLP-1 and glucagon dual agonists disclosed herein have improved biological stability, including proteolytic stability, and duration of action. The peptides can be administered about once a week.

Disclosed herein are compositions comprising a population of silk fibroin nanoparticles having a polydispersity index (PDI) of 0.5 or less, including but not limited to, a PDI of 0.450 or less, 0.40 or less, 0.35 or less, 0.325 or less, 0.30 or less, 0.275 or less, 0.250 or less, 0.225 or less, or 0.200 or less, wherein a glucagon-like peptide-1 (GLP-1) compound or other protein drug or peptide drug including but not limited to insulin, monoclonal antibodies, and related structures is embedded within the population of silk fibroin nanoparticles, wherein the population of silk fibroin nanoparticles is optionally surface treated with at least one of polyethylene glycol, human transferrin protein, the Fc receptor of IgG, or other novel surface modifiers including but not limited to peptides, proteins, or nanobodies. Methods of making and administering the compositions are described herein.

The invention belongs to the field of drug sustained release preparations, and provides an ovulation inducing preparation for improving fertility and a preparation method thereof. The core-shell structure microsphere design is adopted, leuprorelin acetate is entrapped in the core of the polylactic acid microsphere, and covalently anchored amido bond connection is formed through an end group activated polylactic acid NHS ester intermediate and a chitosan-sodium tripolyphosphate ion network shell layer, so that the high stability of the shell layer is realized; by optimizing the compounding use of the internal phase stabilizer and the freeze-drying protective agent, the particle size distribution D50 of the microspheres is controlled to be 10-60 microns, the thickness of the shell layer is controlled to be 0.05-5 microns, and high encapsulation efficiency, good drug slow release performance and excellent storage stability are realized. The technical problems that in an existing peptide medicine core-shell microsphere system, a shell layer is prone to falling off, the medicine is suddenly released, and the stability is poor after freeze-drying are solved, and the peptide medicine core-shell microsphere has the advantages of being high in encapsulation efficiency, controllable in release and good in biocompatibility and has wide application value in the technical field of assisted reproduction.

The present disclosure provides peptide products, including peptides covalently attached to surfactant moieties, that have improved properties, including increased duration of action and bioavailability, and are useful for treating insulin resistance, diabetes, obesity, metabolic syndrome, and cardiovascular disease and their associated conditions, such as NASH and PCOS. [Selected figure] Figure 18A

This invention provides the preparation and application of a class of artificial peptide transporters for promoting transmembrane delivery of peptide drugs. The general structural formula is as follows: The compound involved in this invention consists of three parts: (1) a diamide structure as an anion-binding unit, which binds to the carboxyl anion of the peptide molecule; (2) a crown ether as a cation-binding unit, which binds to the amino cation of the peptide molecule; and (3) a hydrophobic side chain: connecting the anion-binding unit and the cation-binding unit, so that the whole molecule can act as molecular tweezers to form a stable complex with the peptide drug and encapsulate it in a hydrophobic environment to promote its transmembrane transport. The compound obtained in this application has inexpensive raw materials, is easy to synthesize, and significantly improves the bioavailability of peptide drugs. It has shown significant synergistic anticancer activity in both in vitro and in vivo experiments, and therefore has great potential as a pharmaceutical excipient.

Peptide agents are disclosed herein that increase blood glucose clearance independent of insulin action. Also described herein are methods of treating metabolic disorders such as diabetes or obesity by administering the disclosed peptide agents.

This application belongs to the field of genetic engineering technology and discloses human enterokinase light chain mutants and their applications. This application involves single-point mutations or multiple rounds of combined mutations based on the wild-type human enterokinase light chain -C112S mutant sequence. The obtained variants have higher specific activity compared to the parent, which is expected to increase unit yield, reduce the residual amount of protease in the final product, and lower product costs. Furthermore, these mutants exhibit high stability in the enzymatic digestion of peptides / proteases, such as liraglutide and smegglutide, GLP-1 analogs, reducing enzyme usage, increasing digestion efficiency, and decreasing the proportion of non-specific products, thereby lowering the production cost of peptide drugs and promoting the rapid development of related industries.

The present invention relates to the field of peptide drugs, and particularly to a triple-target peptide and a derivative thereof. The triple-target peptide provided by the present invention exerts effects of lowering blood glucose, reducing blood lipids, and weight loss. Based on the above studies, the triple-target peptide provided by the present invention is further long-acting modified, and while retaining excellent effects for the specific indications described above, also has long-acting advantages, which can reduce dosing frequency, improve medication convenience, and enhance patient compliance. Experimental results show that the peptide and the long-acting derivative thereof provided by the present invention can significantly lower blood glucose, reduce blood lipids and / or induce weight loss, and can effectively prevent, treat, or ameliorate diabetes, obesity, obesity-related diseases, or metabolic disorders.

The application discloses a double-drug one-peptide drug delivery system, a preparation method and application thereof, and belongs to the technical field of biological medicines. The drug delivery system comprises Ce@MPBMPs, DAP, RosA, MM and E7 homing peptides. The drug delivery system can be in situ attached to the corresponding intervertebral disc segment of waist pain, and oxygen vortex generated by CeO2 is triggered in an inflammatory acidic environment by means of microneedle transdermal drug delivery technology, so as to realize the response release of double drugs and the synergistic inhibition of pathological microenvironment deterioration. Meanwhile, the homing peptide E7 modified on the outer layer can specifically recruit endogenous mesenchymal stem cells, and activate the anti-inflammatory outer vesicle secreted by the mesenchymal stem cells in a time and space specific manner, so as to play an anti-inflammatory role. Therefore, the drug delivery system can effectively inhibit the deterioration of the inflammatory microenvironment, a key pathological factor of intervertebral disc degeneration, and realize the delay treatment of intervertebral disc degeneration.

The invention relates to a fluorine-containing ionizable lipid compound, a preparation method and application thereof, and an LNP composition, and relates to the technical field of medical biologication.The fluorine-containing ionizable lipid compound is synthesized by taking an aldehyde compound, an amine compound, a carboxylic acid compound and an isonitrile compound as raw materials through a Ugi reaction; the obtained fluorine-containing ionizable lipid compound, sterol, auxiliary lipid and a polyethylene glycol lipid derivative form a lipid nanoparticle-like composition, and the composition can be used for drug delivery, including nucleic acid drugs such as small molecule drugs, mRNA, DNA and the like, protein / polypeptide drugs, and gene editing complexes such as mRNA / sgRNA, Cas9 / sgRNA and the like; the mRNA expression of different organs in an animal body is realized through different administration modes, and the application requirements of mRNA nucleic acid therapy, nucleic acid vaccines, gene editing and the like can be met.