41 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.

Described herein are bacteriocin peptides and peptidomimetics as well as compositions comprising same. Aspects and embodiments described herein may be used in medical treatment and disinfection of surfaces.

The invention discloses a fatty cation amphiphilic peptide simulant as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly, developing an amphipathic cationic peptide simulant system based on cysteine, then introducing ethylenediamine as a cationic group by forming a peptide bond at the terminal of carboxyl, and introducing a hydrophobic group containing an aromatic ring to a sulfydryl side chain; wherein the cationic group provides positive charges and hydrophilicity and is beneficial to electrostatic interaction with a bacterial membrane with negative charges, and the hydrophobic group is beneficial to insertion of the membrane into a phospholipid bilayer; in addition, the N terminal is modified by fatty acids with different chain lengths, the amphiphilic balance of the cysteine-based cationic peptide simulant is finely adjusted, and finally the fatty cationic amphiphilic peptide simulant is synthesized. The peptidomimetic has good antibacterial activity, is not easy to induce bacteria to generate drug resistance, and can be used for preparing drugs for treating, improving and / or preventing infection of drug-resistant bacteria and / or drug-resistant fungi.

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.

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

Disclosed are inhibitors for the β-catenin / T-cell factor interaction. The inhibitors are selective for β-catenin / T-cell factor over β-catenin / phosphocadherin, and β-catenin / phosphoAPC interactions. Methods of using the disclosed compounds to treat cancer are also disclosed.

Disclosed herein is a series of helical sulfono-γ-AApeptides that mimic the binding mode of the α-helical HD2 domain of B-Cell Lymphoma 9 (BCL9). As disclosed herein, sulfono-γ-AApeptides can structurally and functionally mimic the α-helical domain of BCL9, and selectively disrupt β-catenin / BCL9 PPIs with even higher potency. More intriguingly, these sulfono-γ-AApeptides can enter cancer cells, bind with β-catenin and disrupt β-catenin / BCL PPI, and exhibit excellent cellular activity, which is much more potent than the BCL9 peptide. Furthermore, enzymatic stability studies demonstrated the remarkable stability of the helical sulfono-γ-AApeptides, with no degradation in the presence of pronase for 24 h, augmenting their biological potential.

The application discloses an adamantane-modified antibacterial peptide mimetic and application thereof. The application obtains a carboxyl end fatty amine-modified compound protected by adamantane amine or Boc through Fmoc amino acid amide condensation, then removes the Fmoc group through piperidine to obtain a series of crude products containing adamantane amine modification and intermediate compounds of Boc-protected fatty amine modification; the intermediate compounds are further modified by adamantane acid through amide condensation to obtain a compound with an amino end, and then other protecting groups are cleaved through trifluoroacetic acid to obtain a series of crude products of adamantane acid modification; after the crude products are purified, the adamantane-modified peptidomimetic is obtained. The adamantane-modified peptidomimetic is used for preparing drugs for infectious diseases caused by sensitive bacteria and drug-resistant bacteria, has high efficient antibacterial activity, low toxicity and is not affected by traditional drug resistance mechanisms.

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 present invention discloses cationic guanidine based peptides, oligomers, and oligomer-peptide hybrid compounds, and also envisages within its scope monomers for obtaining peptides, oligomers and oligomer-peptide hybrid compounds, and the processes thereof. The present invention additionally relates to the composition for administration of the compounds and their utility as antimicrobial, antifungal agent and as a carrier therapeutic molecules for drug delivery applications.

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.

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 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.

Disclosed are peptides and peptidomimetics that in some embodiments include the amino acid sequence KRGARST or (SEQ ID NO: 1), AKRGARSTA or (SEQ ID NO: 2), or CKRGARSTC (SEQ ID NO: 3). Also disclosed are conjugates and compositions that include the peptides and / or peptidomimetics, methods for directing a moiety to tumor lymphatic vasculature, methods for imaging tumor lymphatic vasculature, methods for reducing or inhibiting tumor metastasis, methods for reducing the number of tumor lymphatic vessels, methods for treating cancer, methods for treating a disease or disorder associated with a gC1q / p32 receptor biological activity, methods for detecting the presence of a gC1q / p32 receptor, methods for detecting interactions between gC1q / p32 receptors and the presently disclosed conjugates and compositions, methods for delivering the presently disclosed conjugates and compositions to gC1q / p32 receptors, methods for assessing gC1q / p32 receptor levels in cells, methods for identifying subjects having diseases associated with gC1q / p32 receptor biological activities, and methods for screening for compounds that interact with gC1q / p32 receptors.

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.

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 discloses a photocurable hydrogel that can bind cytokines and is used for culturing tumor organoids, and its application, and belongs to the technical field of organoid culture. The present invention develops a hydrogel that can fix cells, bind cytokines, and achieve organoid recovery by using norbornene-modified heparin, norbornene-modified gelatin, thiol four-arm polyethylene glycol, dextran, matrix metalloprotein peptidomimetic MMP, and photoinitiator. Organoids can be directly prepared using this hydrogel, and a variety of structural heparins can be used, which reduces costs. Modified heparin can bind factors or matrix proteins and controllably release factors. Modified gelatin provides amino acid energy for collagen hydrolysate. The hydrogel is formed by photocuring in a step-by-step polymerization manner, and has a controllable structure and adjustable biomimetic modulus and adjustable biomimetic stress relaxation. The hydrogel of the present invention can be used for the cultivation of a variety of organoids, overcoming the problems of low repeatability and instability of current technologies, and is suitable for fields such as tumor drug evaluation.

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 disclosure provides a design and synthesis of a useful carbon skeleton, a design and synthesis of a peptidomimetic molecule and applications and uses based thereon. More particularly, provided is a method for designing a compound skeleton with a desired structure, said method comprising, with the use of a computer: (1) a step for generating a molecular formula of a carbon-containing compound; (2) a step for randomly synthesizing molecules using the adjacency matrix and extracting compounds that correspond to the molecular formula among the randomly synthesized molecules; and (3) a step for selecting a compound that satisfies preset conditions.

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.