647 results about "Cyclic peptide" patented technology

This disclosure provides cyclic peptide compounds of formula (A) or formula (II) as inhibitors of Ras kinase, and compositions and use of the same in treating diseases associated with Ras kinase.

Disclosed are a pentapeptide compound and a composition and use thereof, relating to the technical field of polypeptides, the peptide or a salt thereof having a structure as shown in formula (I): R1-Lys-Lys-Leu-Ala-R2 (I). The invention also relates to a cyclic peptide, and the structure of the cyclic peptide is Cyclo-[Lys-Lys-Lys-Leu-Ala]. The compound disclosed by the invention has the effects of controlling oil, repairing, resisting oxidation and the like, and can be used for nursing skin or mucosa.

The present invention relates to compounds of the formulae (I) or (XX) that are panRAS inhibitors for use in a method of treating cancer.

The invention relates to the field of computer-aided drug design (CADD) and molecular informatics, in particular to a multi-modal representation learning method based on cyclopeptide molecules, which is used for predicting cell membrane permeability of cyclopeptide. The method mainly comprises the following steps: (1) data collection: integrating cyclic peptide permeability data from a ChEMBL database, a CycPeptMPDB database and a CyclicPepeda database and patent literatures; (2) multi-modal learning: for different modal data, a deep learning model is adopted to extract feature representations of the data; the method comprises the following steps of: encoding an SMILES sequence by using ChemBERTa (ChemBERTa); using Vision Transform to extract molecular image features, and learning a molecular image structure and 3D coordinate information based on GNN; (3) multi-modal feature fusion: adopting a self-adaptive extensible fusion mechanism, integrating SMILES feature information into image, graph and 3D coordinate features through a cross-modal feature fusion mechanism, and splicing all modal features to obtain multi-modal molecular representation; and (4) permeability prediction: sending the multi-modal molecular representation into a full connection layer for regression prediction so as to evaluate the permeability of the cyclopeptide.

The invention discloses a cyclic peptide compound as well as a preparation method and application thereof, belongs to the field of polypeptide synthesis and application, and particularly relates to full-protection peptide resin prepared by solid-phase synthesis. Carrying out cutting and monocyclization on the full-protection peptide resin to obtain monocyclic peptide; the monocyclic peptide is subjected to binary cyclization treatment to obtain a cyclic peptide compound Cyclo (His-Lys-Cys-Gly-His-Lys-Cys-Gly-, and a disulfide bond is in bridge connection with Cysamp; and the binary cyclization is cyclized under the action of iodine methanol and ascorbic acid. The cyclopeptide compound prepared by the invention has the advantages of low toxicity, good stability, good antioxidant effect and good anti-inflammatory effect, and the expression of type I collagen can be improved. Therefore, the invention has the advantages of low toxicity, good stability, good antioxidant effect and good anti-inflammatory effect, and can improve the expression of the type I collagen.

The invention discloses an antibacterial cyclic peptide screening system and method based on a multi-modal cross attention mechanism, and belongs to the field of antibacterial cyclic peptide screening, the antibacterial cyclic peptide screening system comprises the antibacterial cyclic peptide screening system of the multi-modal cross attention mechanism, the antibacterial cyclic peptide screening system of the multi-modal cross attention mechanism comprises a multi-modal cross attention screening model and a multi-modal cross attention screening model, the method is used for screening antibacterial cyclic peptides; data of the data input module comprises a one-dimensional sequence, a two-dimensional structure and a three-dimensional structure, data sources in the data input module comprise but are not limited to APD3, DRAMP and a Un i Prot public database, and the data input module is used for conveying data of the antibacterial cyclic peptide; through cooperative use of the devices, the cross attention fusion module is arranged, and weights of different modals are dynamically allocated, so that a key active region of the antibacterial cyclic peptide is more obvious, and a multi-modal cross attention screening model can more accurately identify related characteristics of the antibacterial activity of the antibacterial cyclic peptide; the screening of the antibacterial cyclic peptide is more accurate.

The invention provides a cyclic peptide as well as a preparation method and application thereof. The cyclic peptide has an amino acid sequence # imgabs0 # represented by formula (1) (wherein X is a Lys residue modified with a fatty acid molecule, and a line connecting Arg and Lys represents an amide bond. The cyclic peptide prepared by the invention has wide antifungal activity and antibacterial activity on drug-resistant bacteria; meanwhile, the biotoxicity and the protease degradation resistance are high, and the in-vivo antibacterial effect of the cyclopeptide can be prolonged. The cyclic peptide can be applied to preparation of anti-bacterial and anti-fungal infection drugs, and can be used as an excellent substitute drug or an auxiliary drug of existing antibiotics. The method for preparing the cyclic peptide is simple, raw materials are easy to obtain, and industrial production can be achieved.

The invention discloses a bidirectional reversible conversion method and system between a peptide molecule SMILES and a sequence expression. The core innovation lies in that a new sequence description syntax is defined to retain information of a polypeptide special bond and specific modification of amino acid; a main chain atom index and adjacency traversal topology identification algorithm is adopted, and end group and topology integrated detection and coding are carried out; a residue recognition algorithm for main chain cutting and template library matching is compatible with any standard or non-standard amino acid residues, an extensible end group library / monomer template library and an automatic increment mechanism, and automatic recognition and sequence annotation of S-S disulfide bonds; the invention relates to a high-fidelity assembly algorithm of HELM anchor points and topology aware cyclic peptide processing. The method solves the problems of incapability of supporting a complex polypeptide topological structure, poor reversibility, insufficient expansibility of a monomer library and the like in the prior art, can be widely applied to scenes of quantitative structure-activity relationship model construction, large-scale polypeptide data cleaning and the like, and has remarkable practicability and innovativeness.

The invention provides a coordination nano assembly of chiral cyclopeptide and manganese ions as well as a preparation method and application of the coordination nano assembly. According to the method, a manganese superoxide dismutase protein structural domain and a unique tumor microenvironment of melanoma high tyrosinase are combined, and polypeptide sequences L-YD-hL-DD-h, L-YL-HL-DL-H and D-yD-hD-dD-h with different chirality are designed for the first time; the chirality of the polypeptide is regulated and controlled, the in-vivo circulation stability and the cell entry efficiency of the nano assembly are improved, the coordination self-assembly of manganese and different chiral cyclopeptides is realized, and the in-situ oxidation of an in-vivo tumor microenvironment is simulated for photo-thermal therapy and cell membrane coating. The method disclosed by the invention is simple, mild in experimental condition and easy to operate, the prepared cell membrane coated nano assembly not only has long circulation stability and high cell entry efficiency, but also can realize mild photo-thermal therapy through in-situ oxidation, releases manganese ions to activate a CGAS-STING pathway for immunotherapy of tumors, and has a wide application prospect. The potential application value is realized in the field of combined treatment of tumors.

The invention belongs to the technical field of nuclear medicine molecular diagnosis and treatment, and discloses a modified CAIX targeting cyclic peptide, a nuclide marker and application of the modified CAIX targeting cyclic peptide in tumor diagnosis and treatment. According to the CAIX targeted cyclic peptide, a rigid bifunctional chelating agent RESCA is introduced to replace a traditional chelating agent, and a sulfonated or alkylated amino acid connector is combined, so that the enzymolysis resistance and in-vivo stability of the probe are remarkably improved. By optimizing the structure of the connector, the lipophilicity is reduced, liver and gall metabolism and non-specific uptake are reduced, and the high uptake rate of tumor target tissues is maintained. The therapeutic nuclide marker of the cyclopeptide can be used for intratumoral irradiation therapy using DOTA or NOTA in combination with an alkylated amino acid linker or an albumin ligand. Experiments show that the marker has high radiochemical purity, excellent pharmacokinetic characteristics and low kidney retention, and is suitable for precise diagnosis and targeted therapy of CAIX high expression tumors such as kidney cancer, colorectal cancer and brain glioma.

The invention relates to a turtle-derived cyclic peptide compound with an anti-tumor effect and a preparation method thereof. The preparation method comprises the following steps: crushing tortoise plastron, adding water for reflux extraction, filtering, concentrating and drying to obtain tortoise-shell glue; dissolving the obtained tortoise-shell gelatin in water, adding protease for enzymolysis, and centrifuging after enzyme deactivation to take supernate; carrying out graded filtration on the obtained supernate and collecting components; and separating and purifying the collected components to obtain the cyclic peptide. The obtained compound has remarkable anti-tumor activity and has a good application prospect in preparation of anti-tumor drugs.

The invention discloses a radix pseudostellariae extract with high content of radix pseudostellariae cyclic peptide B and a preparation method and cosmetic application of the radix pseudostellariae extract, and belongs to the technical field of cosmetics. The preparation method comprises the following steps: (1) crushing radix pseudostellariae, adding alcohol and performing ultrasonic treatment to obtain feed liquid; (2) adding a compound enzyme into the feed liquid to carry out enzymolysis, enzyme deactivation, solid-liquid separation, concentration and impurity removal to obtain an enzymatic hydrolysate; and (3) eluting the enzymatic hydrolysate with macroporous resin to obtain an eluent, and drying to obtain the product, the compound enzyme is prepared from pectinase, papain, beta-glucosidase, cellulase and xylanase according to the mass ratio of (5 to 10) to (0.5 to 1) to (3 to 7) to (0.3 to 1). The radix pseudostellariae extract disclosed by the invention is prepared by adopting an enzymolysis process, more active ingredients can be reserved, the content of radix pseudostellariae cyclic peptide B in the obtained extract is high, and the radix pseudostellariae extract has relatively good anti-inflammatory, soothing, repairing and anti-aging effects.

The invention belongs to the technical field of polypeptides and biological medicines, and particularly relates to a WK7 series antibacterial peptide and application thereof in the aspects of resisting bacteria and preventing and treating diabetic foot, pneumonia and septicemia. According to the invention, a linear peptide WK7-line with an amino acid sequence of WKRWKRW is used as a minimum active unit, and modification is carried out to form a plurality of linear modified peptides; meanwhile, a cyclic peptide WK7-cyl is formed on the basis of the linear peptide WK7-line through cyclization, and the cyclic peptide WK7-cyl is further modified to form an annular modified peptide. The linear peptide WK7-line, the linear modified peptide, the cyclic peptide WK7-cyl and the cyclic modified peptide jointly form the WK7-series antibacterial peptide, and the WK7-series antibacterial peptide is artificially synthesized polypeptide, is small in molecular weight, easy to synthesize, free of cytotoxicity, almost free of hemolysis risk, high in sterilization speed and broad-spectrum antibacterial property and can be used for preparing the antibacterial peptide. The traditional Chinese medicine composition has a certain effect on prevention and treatment of diabetic foot ulcer, pneumonia and septicemia.

The invention relates to a cyclopeptide inhibitor aiming at human STING (stimulating interferon gene) and application of the cyclopeptide inhibitor. The cyclic peptide can specifically bind to and inhibit activation of human STING. The invention also provides a nanoparticle delivery system for loading the cyclopeptide on a cationic polymer PBAE and an amphiphilic polymer pDMA-pEPEMA, and a preparation method of the nanoparticle delivery system. The cyclic peptide and the nanoparticles thereof can be used for preparing medicines for treating autoimmune diseases (such as systemic lupus erythematosus and the like) caused by excessive activation of the cGAS-STING signal pathway. Compared with the existing small molecule STING inhibitor, the cyclopeptide inhibitor provided by the invention has higher specificity, stability and inhibition effect.

The present invention discloses a class of bicyclic peptide compounds and their applications, belonging to the technical field of bicyclic peptide compounds. Specifically, the invention relates to the preparation of a fully protected peptide resin using solid-phase synthesis; cleavage and monocyclic cyclization of the fully protected peptide resin to obtain a monocyclic polypeptide; and dicyclic cyclization of the monocyclic polypeptide to obtain a bicyclic peptide compound, wherein the dicyclic cyclization is carried out under the action of iodine methanol and ascorbic acid. The bicyclic peptide compound prepared by the present invention has the following beneficial effects: good safety, low cytotoxicity, good stability, slow degradation rate, good effect on enhancing collagen expression, good effect on enhancing elastin expression, and good effect on inhibiting neurotransmitter release.

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and / or functional groups which have utility in imaging and targeted cancer therapy.

The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to Nectin-4, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.

Provided herein are novel cyclic peptides, their synthetic process, compositions, properties including stability and pharmacokinetic profiles, and applications for treating solid tumor cancers.

The invention provides a cyclic peptide used for treating, improving or preventing nervous system injury of mammals or diseases or pains caused by the injury, neurodegenerative diseases, anxiety or epilepsy or used as a neuronal protective agent, a conjugate containing the cyclic peptide, a pharmaceutical composition containing the cyclic peptide or the conjugate and application of the cyclic peptide and the conjugate.

The invention belongs to the technical field of active polypeptides and preparation, and particularly relates to an antioxidant and anti-inflammatory cyclopeptide capable of inhibiting matrix metalloproteinase as well as a preparation method and application of the antioxidant and anti-inflammatory cyclopeptide. The cyclic peptide is formed by end-to-end covalent coupling of linear peptide with the amino acid sequence of DEETGEF, has the activity of resisting oxidation, resisting inflammation and inhibiting matrix metalloproteinase, is free of cytotoxicity and skin irritation, and is suitable for being used as cosmetics for resisting skin aging, wrinkles and the like.

The invention provides a bicyclic peptide as well as a preparation method and application thereof in cosmetics. Specifically provided is a bicyclic peptide or a salt thereof, which has a structure as shown in formula I. The bicyclic peptide or the salt thereof provided by the invention can be applied to skin care products, has one or more effects of moisturizing, repairing, anti-aging and the like, and has a good application prospect;

The present disclosure relates to the synthesis of cyclic peptides that are able to effectively deliver cargo, e.g., a therapeutic moiety (TM), inside a cell to treat a variety of conditions and diseases.

Disclosed are cell-penetrating cyclic peptides. The peptides can be used to deliver peptides and other biologically active moieties into cells. Formulations containing the cell-penetrating cyclic peptides are also described.

The invention belongs to the technical field of nuclear medicine, and relates to a CAIX-targeted cyclic peptide and a preparation method and application thereof, the CAIX-targeted cyclic peptide structure is shown as a formula 1, Linker is a cyclization connexon, and Chenator is a nuclide chelating group. The CAIX-targeted cyclic peptide provided by the invention has high affinity with CAIX, and has low affinity with isoenzyme CAII of CAIX, so that the CAIX-targeted cyclic peptide has high selective affinity with CAIX; the nuclide-labeled radioactive probe has high labeling rate and excellent in-vitro stability, has excellent pharmacokinetic characteristics in tumor-bearing model mice of human renal clear cell carcinoma, and has extremely high tumor uptake, tumor-muscle ratio and tumor-kidney ratio which can meet diagnosis requirements; due to the long-time retention characteristic in tumors, the polymer has a relatively high tumor treatment application value.

To provide peptide ligands, and peptide complexes comprising the peptide ligands conjugated to a second peptide.SOLUTION: The present invention provides a peptide ligand that binds to Nectin-4 present on a cancer cell, or a pharmaceutically acceptable salt thereof, the peptide ligand comprising a polypeptide comprising at least three reactive groups separated by at least two loop sequences, and a molecular scaffold that forms covalent bonds with the reactive groups of the polypeptide, such that at least two polypeptide loops are formed on the molecular scaffold, wherein the polypeptide is a modified derivative of a specific sequence.SELECTED DRAWING: None

The present disclosure relates to the technical field of polypeptides. Disclosed are a cyclic peptide, and a composition and the use thereof. The cyclic peptide of the present disclosure has a structure as shown in formula (I): Cyclo-[Gly-His-Lys-Lys] (I). The present disclosure specifically relates to the cyclic peptide or a salt thereof, or a composition thereof, and the use thereof in the preparation of a composition for caring or treating skin or mucosa.

A preparation method, intermediates, and use of a cyclic peptide toxin α-Amanitin and / or Amaninamide are provided, belonging to the technical field of organic synthesis. A total synthesis method of the cyclic peptide toxin compounds α-Amanitin and Amaninamide is provided, where raw materials and reagents used are easily purchased through commercial channels, the intermediates are stable, and the preparation method shows mild reaction conditions, simple operation process, desirable operability of separation and purification, and high yield. The preparation method also shows important reference and practical value, can achieve gram-scale preparation of the α-Amanitin and Amaninamide, and has excellent industrial prospects. Therefore, the preparation method is of significant application value in the field of cyclic peptide toxin synthesis.

SorCS2 related lipidated cyclic peptides, cyclic peptides, lipidated linear peptides, linear peptides which may be of use in medicine, and related aspects.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to N-methylation modified cyclopeptide and application thereof. On the basis of a GluA2-3Y polypeptide sequence, chemical modification and transformation of amido bond N-methylation and head-tail cyclization are carried out, the N-methylation modified cyclopeptide with stable metabolism and good permeability is obtained, and the endocytosis of a GluA2AMPA receptor is blocked to protect nerve cells, so that the GluA2AMPA receptor can be effectively inhibited, and the GluA2AMPA receptor can be effectively inhibited. The invention also provides application of the cyclic peptide in preparation of drugs for treating cerebral arterial thrombosis.

The invention discloses an anti-aging composition and application thereof. According to the anti-aging composition disclosed by the invention, the anti-aging composition is prepared by compounding dimethyl silanol hyaluronate, radix pseudostellariae cyclic peptide B and a medicago sativa extract. The medicago sativa extract disclosed by the invention is obtained by adopting a pulsed ultrasound-assisted subcritical extraction technology, and can play a better anti-aging effect. Experiments verify that the composition can significantly increase the content of retinoic acid binding receptor RAR alpha and RXR gamma proteins and type I collagen, inhibit cell aging and achieve an anti-aging effect similar to that of retinol, but compared with retinol, the composition is mild and non-irritant, can significantly improve the preservative efficacy of a product when being used in skin care products, and can reduce the dosage of preservatives.