26 results about "Peptidomimetic" patented technology

The invention belongs to the technical field of biology, and particularly relates to a receptor peptidomimetic capable of improving the breeding efficiency of butter crabs and application of the receptor peptidomimetic. The optimal binding conformation is screened according to the sequence prediction binding conformation of the vitellogen and the receptor of the vitellogen, the hotspot residues are screened according to the optimal binding conformation, and the binding energy change before and after mutation of the hotspot residues is calculated to determine the receptor peptidomimetic sequence. The receptor peptidomimetic can obviously slow down the development speed of the ovary of the blue crab and effectively induce the formation of the butter crab by utilizing the specificity of specific recognition of the vitellogenin of the blue crab and the receptor, so that the butter crab product can be produced in a planned manner.

The present invention relates to a composition for preventing, ameliorating or treating central nervous system diseases, comprising a peptidomimetic compound (NIP001) containing hydrophilic arginine and a hydrophobic histidine derivative. In the present invention, the peptidomimetic compound comprising hydrophilic arginine and a hydrophobic histidine derivative was confirmed to effectively inhibit inflammatory responses in microglia and to have the effect of improving the cognitive function of mice with scopolamine-induced cognitive impairment, and thus can be used as a targeted therapeutic agent for central nervous system diseases.

The present invention is directed to peptidomimetics having antibacterial activity, especially against Gram-negative bacteria. The peptidomimetics of the invention are compounds of the general formula (I), P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-P15-P16 (I) and salts thereof, in particular pharmaceutically acceptable salts thereof, as described in the description and in the claims. The invention is also directed to therapeutic uses of the peptidomimetics for the treatment or prevention of bacterial infections and diseases related to bacterial infections and to non-therapeutic uses of the peptidomimetics for preserving or disinfecting foodstuffs, cosmetics, medicaments or other nutrient-containing materials.

The invention relates to β-catenin-binding peptides and peptidomimetics comprising an amino acid sequence ESILDEHXQRVW or EYPESILDEHXQRVWR, wherein X is L, M, I, F, Y, W or C, or a variant of said amino acid sequences, and to uses thereof.

Provided are cyclic peptidomimetics that can, e.g., antagonize the extracellular domain of EGFR, and methods of use thereof.

Compositions containing self-assembling peptides and / or self-assembling peptidomimetics (“self-assembling peptides”) can be used to create a long-lasting “lift” or means of elevating tissue to be resected, dissected, manipulated or repaired, as a bulking agent, or as a tissue forming matrix by injection of a solution that forms a solid gel in situ, which is stable for a prolonged period of time from days to a month, is hemostatic, and may prevent adhesions. These self-assembling peptides and methods of use thereof enable better separation of tissues and visualization of margins, more durable and robust lifts, less need for frequent injections that carry risk of undesired perforation, and simultaneous management of adverse effects, such as bleeding, leaking, inflammation and iatrogenic injury during endoscopic, laparoscopic or other minimally invasive, or open surgical procedures in and / or on the body.

The invention discloses a peptidomimetic compound, a preparation method, a related product and application, and belongs to the technical field of peptidomimetic compounds. The technical problem to be solved is to provide a compound which has an average value of inhibiting 3CL protease IC50 of 6.3-25.9 [mu] M and can effectively reduce the virus load. The key point of the technical scheme is that the structure of the peptidomimetic compound is shown as (I).

Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

The present invention provides methods of generating diverse chemical structures on DNA through Wittig olefination of novel on-DNA phosphorane ylides and Homer-Wadsworth-Emmons reaction of on-DNA β-keto phosphonates. The methods of this invention provide access to DNA-encode libraries (DELs) of diverse peptides, peptidomimetics, chalcone-based molecules, and the like.

The invention provides a brand new D-configuration diphenylalanine-based peptidomimetic mediated A beta / p62 co-coagulation autophagy degradation strategy. The D-configuration diphenylalanine peptidomimetic can be used as a scaffold molecule, can be combined with extracellular A beta and then enters cells to be combined with p62 to form a multi-component compound, a co-aggregate is formed along with increase of intermolecular acting force, efficient autophagy degradation can be driven on the premise that A beta aggregate is effectively isolated in cells, and the autophagy degradation efficiency is improved. Further, an autophagy degradation strategy of extracellular target protein co-coagulation is established. Peptidomimetic mediated A beta / p62 co-coagulation autophagy degradation of D-configuration diphenylalanine can reduce accumulation of A beta in neuronal cells, alleviate pathological characteristics of amyloid protein, alleviate synaptic injury, neuroinflammation and A beta burden in AD mouse brains, and significantly save learning and memory defects of mice.

The invention belongs to the field of biological medicine, and discloses a broad-spectrum anti-enterovirus peptidomimetic 2CA-1 targeting enterovirus 2C protein and application of the broad-spectrum anti-enterovirus peptidomimetic 2CA-1. The 2CA-1 can be accurately butted to 2C protein binding pockets of EV71 and CVB3, the helicase activity of the 2CA-1 is effectively inhibited, and the 2CA-1 shows a strong and broad-spectrum antiviral effect on various pathogens such as coxsackie virus, EV-D68 and rhinovirus on the cellular level. More importantly, the 2CA-1 realizes a druggability breakthrough of excellent oral bioavailability in an animal model, and the in-vivo virus load can be remarkably reduced after oral administration. The invention provides an antiviral candidate drug with high-efficiency broad-spectrum activity and ideal oral administration characteristics, and has a wide application prospect.

The present invention relates to a peptidomimetic and a composition containing the same that exhibits excellent inhibitory effects on itch-inducing cytokines (TNF-α, IL-4, IL-6, and IL-8), and more specifically, to a peptidomimetic and a composition containing the same that include a histidine derivative capable of effective control of itch-inducing cytokines. The tetrapeptide containing the histidine derivative of the present invention exhibits excellent inhibitory effects on the inflammatory cytokines TNF-α, IL-4, IL-6, and IL-8, and also exhibits excellent stability in the human body when applied, making it extremely useful in industrial fields such as cosmetics and pharmaceuticals.

Lipid nanoparticles (LNP) having an immune regulation function, presenting at least one immune ligand on the surface thereof, promoting activation of non-variant natural killer T cells (iNKT cells) and inducing an immune response, or mediating recognition, binding or internalization between the lipid nanoparticles and the immune cells, and regulating the functional state of the immune cells; the formulation of the lipid nanoparticles comprises at least one of a ceramide-based glycolipid family, a peptidomimetic, and fucosterol, and the formulation forms nanoparticles of 1-1000 nm by a mixing process. The invention provides a lipid nanoparticle formula for enhancing organ targeting, cell targeting or cell activity, a pharmaceutical composition prepared by using the formula and application of the pharmaceutical composition. The formulation can encapsulate and deliver active ingredients such as nucleic acids, gene editing system components and natural small molecules.

The application discloses a kind of based on D configuration diphenylalanine peptidomimetic or its pharmaceutically acceptable salt, with the following structure: Wherein X represents C, O, S, n represents the integer of 1~6.The peptidomimetic described in the application has endoplasmic reticulum targeting, and can specifically induce endoplasmic reticulum autophagy.The peptidomimetic described in the application can be used as endoplasmic reticulum inducer for cell homeostasis and disease mechanism and treatment target research, promote the research and application of drug.

Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

The present invention is directed to peptidomimetics having antibacterial activity, especially against Gram-negative bacteria. The peptidomimetics of the invention are compounds of the general formula (I),P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-P15-P16                      (I)and salts thereof, in particular pharmaceutically acceptable salts thereof, as described in the description and in the claims. The invention is also directed to therapeutic uses of the peptidomimetics for the treatment or prevention of bacterial infections and diseases related to bacterial infections and to non-therapeutic uses of the peptidomimetics for preserving or disinfecting foodstuffs, cosmetics, medicaments or other nutrient-containing materials.

The invention relates to a peptidomimetic of an NPC-1 epitope on the MUC5AC protein which is differentially expressed in pancreatic and colorectal cancer, and diagnostic and therapeutic usages. Further, antibodies that selectively bind the NPC-1 epitope peptidomimetics and may be used in diagnostic and therapeutic methods.

The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.

The present invention relates to compounds of Formula I: (I) and their pharmaceutically acceptable salts that activate the melanocortin-5 receptor (MC5R) and uses thereof in the treatment or prevention of a disease or condition related to MC5R activity.

The present specification provides a pharmaceutical composition for preventing or treating gastric cancer, comprising, as an active ingredient, a protein activity inhibitor or gene expression inhibitor for at least one of SHMT1, TYMS, MTHFD1, and DHFR, wherein the protein activity inhibitor is at least one of a compound, a peptide, a peptidomimetic, a substrate analog, an aptamer, and an antibody that specifically bind to a protein, and the gene expression inhibitor is at least one of an antisense nucleotide, RNAi, siRNA, miRNA, shRNA, and a ribozyme that complementarily bind to mRNA of a gene.

Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

The present invention relates to an agent that inhibits the expression or activity of the G Protein-Coupled Receptor 182 (GPR182) protein for use in the treatment or prevention of a pathological condition selected from myocardial infarction, myocardial ischemia, myocardial necrosis, cardiac hypertrophy, cardiac fibrosis, limb ischemia, ischemia-related tissue degeneration, stroke and a cancer, wherein (a) the agent that inhibits the expression of the GPR182 protein is selected from an siRNA, miRNA, shRNA, a ribozyme and an antisense nucleic acid molecule; and / or (b) the agent that inhibits the activity of the GPR182 protein specifically binds to the GPR182 protein and inhibits binding of one or more endogenous ligands to the GPR182 protein, and wherein the agent is selected from an antibody, an Fc fusion polypeptide, an adnectin, an affibody, an affilin, an anticalin, an atrimer, an avimer, an evibody, a Kunitz-type domain, a designed ankyrin repeat protein (DARPin), a fynomer, a peptide or peptidomimetic, an aptamer, and a small molecule; or any combination and / or hetero-or homo-oligomeric, covalent or non-covalent complex thereof.

The present disclosure provides novel methods for treating or preventing amyotrophic lateral sclerosis (ALS), methods for delaying the onset of neurological symptoms associated with ALS, increasing survival in subjects afflicted with ALS, and attenuating the decline of muscle strength associated with ALS in a subject in need thereof. The present disclosure also provides methods for treating or preventing α-synucleinopathy or TDP-43 proteinopathy. The methods comprise administering to the subject an effective amount of a mitochondriatargeting peptidomimetic compound, such as (R)-2-amino-N-((S)-1-(((S)-5-amino-1-(3-benzyl-1,2,4-oxadiazol-5-yl)pentyl)amino)-3-(4-hydroxy-2,6-dimethylphenyl)-1-oxopropan-2-yl)-5-guanidinopentanamide, or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, and / or solvate thereof.

This invention particularly provides compounds, pharmaceutical compositions, and methods related to the treatment of viral infections caused by coronaviruses or enteroviruses. The invention provides compounds of formulas (I), (II), and (III) and methods for using said compounds in a therapeutic manner. These compounds are peptide mimics of the coronavirus protease 3CL and are suitable for treating conditions caused by viral infections, including COVID-19.