33 results about "Peptide drug" patented technology

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.

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 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 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.

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.

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 invention relates to formulation for oral delivery of peptides and / or drug molecules and a method of manufacturing the same. The oral formulation is useful for delivering peptides to the gastrointestinal tract, preferably at the ileo-caecal junction of colon.

This invention relates to an enzyme-responsive brain-targeting sustained-release formulation based on dialkylimidazolium biomimetic lipids, its preparation method, and its application, belonging to the field of drug delivery. First, dialkylimidazolium biomimetic lipids are covalently coupled with natural phospholipids to form a dialkylimidazolium conjugate. Then, this dialkylimidazolium conjugate is self-assembled with dialkylimidazolium biomimetic lipids, natural phospholipids, cholesterol, and a therapeutic drug to form a drug-loaded lipid nanoparticle delivery system. This drug delivery system can effectively cross the blood-brain barrier to achieve brain-targeted delivery of the loaded drug. In the glioma microenvironment, this drug delivery system can gradually hydrolyze the dialkylimidazolium conjugate through an enzyme-responsive mechanism to achieve sustained release of the loaded drug, providing a new strategy for improving the brain targeting and efficacy of different types of anti-glioma drugs, such as small nucleic acid drugs, peptide drugs, and small molecule drugs.

This invention belongs to the field of peptide drug synthesis, specifically relating to a method for synthesizing high-purity retatrutide. This invention utilizes fragments such as Fmoc-Ile-Glu(OtBu)-OH for synthesis, effectively avoiding the generation of Ile-deficient impurities and reducing the use of expensive materials. By optimizing the synthesis process, this invention reduces the synthesis difficulty and shortens the product production cycle. The resulting crude retatrutide has high purity, facilitating subsequent preparation and purification, and significantly improving product purity and yield.

The application discloses a kind of target specificity peptide sequence design deep learning algorithm based on condition generation and affinity joint optimization, comprising: constructing target protein-protein fragment data for model pre-training;Construct target protein-peptide PDB data set and target protein-peptide data and experimental affinity data for model fine-tuning, wherein affinity data is also used as training affinity classifier;Based on protein large language model, target protein sequence and peptide sequence are encoded;Candidate peptide sequences are generated in continuous latent space by condition diffusion model;And the combination ability is evaluated by combining affinity classification model, through joint optimization and noise consistency training, in unified latent space, alignment generation and discrimination process is generated, realize the directional generation and efficient screening of peptide sequence.The application can generate peptide with high sequence diversity and superior binding potential without target protein three-dimensional structure information, and provides an efficient calculation method for peptide drug design of structure missing or highly dynamic target.

The invention describes peptides with anticancer activity and exhibiting antagonistic activity against CD133 protein, which were obtained and designed by means of computer tools, evaluating physicochemical parameters of flexibility, hydrophilicity, hydrophobicity, antigenicity and total charge as described herein, in addition to the modeling of the protein, which allowed selecting 4 regions with the appropriate characteristics. After modeling the selected peptides, CD133 peptide-protein molecular docking was performed, where stable interactions were observed, even showing hydrogen bonds. Finally, the peptides of the invention showed anticancer effects against several cancer cell lines, including cancer cells resistant to conventional treatments such as triple negative breast cancer cells.

This invention relates to the field of peptide drug preparation techniques, specifically disclosing a method for the hydrophobic tag-assisted liquid-phase synthesis of retatrutide. The retatrutide preparation method includes the following steps: synthesizing two hydrophobic tags, TAG1 and TAG2; dividing retatrutide into six fragments and linking each fragment to a TAG; wherein the C-terminal amino group of TAG2 can be directly retained after deprotection; the peptide fragments obtained during synthesis can be purified by acetonitrile slurrying; the main chain of retatrutide is obtained by end-to-end ligation, followed by the ligation of side chains to obtain fully protected retatrutide; finally, deprotection and removal of the hydrophobic tag are performed to obtain retatrutide. The preparation method of this invention uses readily available starting materials, and the reaction operations and separation / extraction processes in each step of the synthesis route are simple, the conditions are mild, the overall yield is high, and material costs are significantly reduced.

Disclosed herein are patches, methods, devices, and systems for delivering a non-aggregating peptide, such as alcadein and its fragments, into a subject. In some aspects, the patch includes a backing, a matrix comprising a non-aggregating peptides disposed within the matrix, and a release liner. In other aspects, the method includes opening at least one channel in the subject's skin, applying the patch described herein, thereby treating a disease or disorder associated with the brain, such as Alzheimer's disease.

The present invention relates to a method for administration of peptide drugs via a reusable pen comprising a replaceable drug cartridge. In particular, the present invention relates to a liraglutide solution administered via a reusable pen. Further, the present invention relates to a semaglutide solution administered via a reusable pen. Further, the present invention also relates to a tirzepatide solution administered via a reusable pen. Further, the present invention also relates to a setmelanotide solution administered via a reusable pen. Further, the present invention also relates to a teduglutide solution administered via a reusable pen.

The present invention relates to the field of biomedicine, and specifically relates to an ionizable lipid and the use thereof. The ionizable lipid has the structure as represented by formula (I). Lipid nanoparticles constructed by using the ionizable lipid of the present invention can realize the safe and efficient delivery of nucleic acid drugs, small molecule drugs, peptide drugs and protein drugs.

This invention provides the application of ARF6 as a scaffold protein in the preparation of engineered extracellular vesicles, belonging to the field of biomedical technology. The application of ARF6 (SEQ ID NO.1) as a scaffold protein in the preparation of engineered extracellular vesicles (EVs) provided by this invention. This invention uses natural full-length ARF6 as a scaffold protein to prepare engineered EVs, fully leveraging its comprehensive advantages of short gene sequence, high editing and synthesis efficiency, strong loading capacity, and good versatility. It effectively overcomes the technical bottlenecks of existing EV drug delivery systems, such as low loading efficiency and complex construction processes, successfully constructing a highly efficient, universal, and safe protein and peptide drug delivery platform. The technical solution of this invention showed good anti-inflammatory effects in both cellular inflammation models and sepsis mouse models, indicating that this invention has significant clinical application value and industrialization prospects in the fields of drug delivery and disease treatment.

This application discloses a method, system, and application for predicting antimicrobial peptide activity, relating to the fields of bioinformatics and peptide drug design. The method includes: training multiple classifiers using a sample dataset; dividing the activity dataset into several data subgroups; employing a K-fold cross-validation strategy, using each data subgroup as the validation set and the remaining data subgroups as the training set to train a classification model and a regression model corresponding to each data subgroup; preprocessing the target amino acid sequence to generate candidate peptides; inputting the ESM feature vector of each candidate peptide into the trained multiple classifiers, the trained classification model corresponding to the data subgroup to which the candidate peptide belongs, and the regression model, respectively, to obtain the predicted probability that the candidate peptide is an antimicrobial peptide, the probability of having inhibitory activity against the target pathogen, and the predicted value of the inhibitory activity intensity against the target pathogen; and selecting the final list of candidate antimicrobial peptides, thereby improving prediction accuracy and data quality in the case of small samples.

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 invention belongs to the field of biomedical technology, specifically disclosing a CD300LF affinity peptide and its applications. The CD300LF affinity peptide provided by this invention can specifically bind to the CD300LF protein and can be used to prepare peptide drugs or detection reagents targeting CD300LF, expanding the forms of drug / formulation development targeting CD300LF. Experiments have shown that the CD300LF affinity peptide can effectively reprogram tumor-associated macrophages, reverse the polarization of TAMs from M2 to M1, and promote the production of M1-related cytokines, thereby enhancing the phagocytic capacity of macrophages against tumor cells. The CD300LF affinity peptide provided by this invention exhibits significant tumor-suppressing effects and immune-activating effects in in vivo tumor models. Its modified peptide has excellent in vivo stability and anti-enzymatic degradation ability, and has no obvious toxic side effects, showing good prospects for translation and industrialization.

This invention belongs to the field of peptide drug synthesis, specifically relating to a method for synthesizing smegglutinin. This method uses a modified amino resin as the solid-phase resin, which can significantly improve the yield and purity of the peptide, and the raw materials are inexpensive and the method is simple.

The application provides a sleep-aiding active peptide intelligent screening method and system based on a multi-modal fusion network, and belongs to the technical field of bioengineering and artificial intelligence. The multi-modal fusion network model of the application is obviously better than the traditional QSAR model in the performance of accuracy, precision, recall rate, F1 score, AUC-ROC, AUC-PR and other indexes, and has good generalization ability and the accuracy of active peptide prediction, and can be widely applied to the discovery and optimization of sleep-aiding active peptides in the research and development of functional foods, health foods and peptide drugs.

This invention discloses a microneedle for long-term administration of peptide drugs, its preparation method, and its application. The microneedle comprises a substrate and needle bodies arranged in an array on the substrate. Each needle body includes a base attached to the substrate and a needle tip located on the base. The needle tip contains a plurality of drug-loaded sustained-release microspheres with a particle size of less than 10 μm. In this microneedle, the drug-loaded sustained-release microspheres are located only in the needle tip portion. This microneedle exhibits high drug delivery efficiency, good puncture resistance, and good drug loading rate, effectively solving the problems of high frequency of administration, short half-life, and poor patient compliance associated with water-soluble peptide drugs.

A method for improving blood kinetics of a peptide is provided. The method for improving blood kinetics of a peptide includes a step of preparing a peptide having a modified amino acid sequence.