653results about "Peptides with abnormal peptide link" patented technology

The present invention relates to four specific macrocyclic compounds for use as inhibitors of KRAS mutant for the treatment of cancer. Example (1): 1-[4-(dimethylamino)-4-methyl-pent-2-ynoyl]-N-[(1S)-1-[[(6S,8S,14S)-22-ethyl-25-fluoro-(21M)-21-[2-[(1S)-1-methoxyethyl]-3-pyridyl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetrazapentacyclo[18.5.2.12,6.110,14.023,27]nonacosa-1(26),20,23(27),24-tetraen-8-yl]carbamoyl]-2-methyl-propyl]-4-fluoro-N-methyl-piperidine-4-carboxamide.

The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and / or presenter proteins are intracellular proteins. In some embodiments, the target and / or presenter proteins are mammalian proteins.

The present disclosure provides for polypeptide conjugates. The polypeptide conjugates disclosed herein comprise a polyarginine peptide and a cyclic cell-penetrating peptide (cCPP) conjugated, directly or indirectly, to the polyarginine peptide. The present disclosure demonstrates that cCPPs conjugated to polyarginine peptides can be used to deliver nucleic acids to the cytosol of cells.

The invention relates to an acinetobacter baumannii resistant cyclic peptide and application thereof, in particular to a compound shown in a formula (I), a tautomer, a stereoisomer, a hydrate, a solvate, pharmaceutically acceptable salt or prodrug of the compound and a preparation method of the tautomer, the stereoisomer, the hydrate, the solvate and the pharmaceutically acceptable salt or prodrug of the compound. The invention further discloses application of the acinetobacter baumannii in preparation of drugs for treating or preventing infection and diseases caused by the acinetobacter baumannii. # imgabs0 #

The invention discloses a VEGF / TIE-2 dual-targeting polypeptide and application thereof in preparation of antitumor drugs, and relates to the technical field of biological medicines. The VEGF / TIE-2 dual-targeting polypeptide (named as RTP) provided by the invention is formed by combining an amino acid sequence capable of identifying VEGF and TIE-2 in a targeting manner, an amino acid sequence capable of forming beta-sheet nanofibers through self-assembly, an amino acid sequence capable of identifying carbonic anhydrase IX in a targeting manner and an enzyme reactive amino acid sequence capable of realizing MMP-2 specific shearing. The RTP can be subjected to allosteric and self-assembly in tumor cells to form stable water-insoluble nanofibers, the formation and metastasis of tumor neovascularization are strongly inhibited through VEGF and TIE-2 double signal channels, and the tumor progress is inhibited.

A hydrophilic linker, an intermediate of the hydrophilic linker, a linker-drug conjugate prepared from the linker and a preparation method therefor, and an antibody-drug conjugate and use thereof.

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 invention provides a Nectin-4 targeting bicyclic peptide compound as shown in a formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof as a nuclide ligand, and belongs to the field of medicines. The invention also provides a complex containing the bicyclic peptide compound, the bicyclic peptide compound is further connected with radionuclide, a pharmaceutical composition containing the complex, and application of the complex and the pharmaceutical composition in preparation of drugs for preventing, treating, treating and / or alleviating cancers. # imgabs0 #

An antibody-drug conjugate as shown in formula I, a preparation method therefor, and a use thereof in prevention and / or treatment of diseases related to abnormal cell activity, including but not limited to a use in prevention and / or treatment of tumor diseases.

To provide camptothecin compounds and their conjugates with novel structures, improved efficacy and improved safety.SOLUTION: The present invention provides a compound having the structure of the upper formula in the figure, or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, nitrogen oxide, isotope-labeled product, metabolite or prodrug thereof. In the formula, R1 and R2 are each hydrogen, halogen, C1-6 alkyl, C1-6 alkoxyl, or the like, or are connected with adjacent carbon atoms to form a 5- to 6-membered oxygen-containing heterocyclic ring; R3 is hydrogen or is connected with an ortho-carbon atom of R1 to form a 6-membered carbocyclic ring; and A is selected from one of the lower two formulas in the figure.SELECTED DRAWING: None

The present disclosure provides a compound comprising a radiolabeling moiety, a targeting moiety, and a DNA intercalating agent and complexes thereof For example, the present disclosure provides a compound of Formula I or a pharmaceutically acceptable salt and / or solvate thereof. Methods of making and uses thereof, such as cancer theranostic applications, are also included. (I)

Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with liver X receptors, comprising bis-octahydrophenanthrenecarboxamides and protein (e.g., antibody) drug conjugates thereof. [Selected figure] Figure 11

The present invention relates to a compound binding to an endogenous receptor, said compound comprising (i) an oligopeptide comprising a dipeptide with Trp being the C-terminal amino acid of said dipeptide, wherein said Trp is replaced with an α-amino acid Xaa2, whereby the stability in serum or plasma of the peptide bond connecting Xaa2 to the N-terminally adjacent amino acid is increased as compared to the peptide bond connecting Trp to the N-terminally adjacent amino acid in an otherwise identical compound; and (ii) a moiety capable of generating therapeutically effective radiation, said moiety being covalently bound to said oligopeptide.

Among the various aspects of the present disclosure are compounds that are useful for inhibiting one or more proteases including various serine proteases such as Hepatocyte Growth Factor Activator (HGFA), and the type II transmembrane serine proteases (TTSPs) including matriptase, hepsin, and TMPRSS2. The present invention also relates to various methods of using the inhibitor compounds to treat and / or prevent infections and their symptoms / complications, including those caused by coronaviruses and influenza viruses, conditions associated with inflammation, various other malignancies, pre-malignant conditions, and / or cancer.

The invention belongs to the technical field of biological medicines, and discloses a small molecule ligand for targeted administration, a ligand medicine conjugate, a rheumatoid arthritis treatment medicine and application. The small molecule ligand for targeted administration provided by the invention takes a structure as shown in a formula (1) as a linker, and meanwhile, a group M1 derived from a fibroblast activating protein inhibitor is introduced, so that the small molecule ligand can be well applied as a drug delivery platform for RA treatment; the molecular biological activity of the anti-rheumatism medicine is kept, and meanwhile, the anti-rheumatism medicine is fully released in an inflammation joint area, so that a better rheumatoid arthritis treatment effect is achieved, and the anti-rheumatism medicine has a good application prospect. # imgabs0 #

Methods and devices for the administration of compositions comprising glutathione trisulfide (GSSSG), pantethine trisulfide (PTN-SSS), or lipoic acid trisulfide (LA-SSS) to treat peripheral neuropathy, e.g., chemotherapy-induced peripheral neuropathy (CIPN), e.g., by oral or nasal administration. The methods can be used, e.g., to reduce pain associated with CIPN, or reduce the risk of development of CIPN.

The present application provides stable peptide-based Akt capture agents and the use thereof as detection, diagnosis, and treatment agents. The application further provides novel methods of developing stable peptide-based capture agents, including Akt capture agents, using iterative on-bead in situ click chemistry.

The invention relates to a method for semi-solid-phase synthesis of a polycyclic compound and an intermediate, a long chain is synthesized through solid phase, then two-step ring closing is performed to form a key intermediate, and simple derivation is performed on the basis of the key intermediate to obtain a PCSK9 antagonist compound. According to the invention, starting materials for solid-phase synthesis are selected, steric hindrance is effectively avoided, and solid-phase reaction and subsequent liquid-phase correlation cyclization can be smoothly carried out, so that the yield is improved, and the cost is reduced.

To provide camptothecin compounds and their conjugates with novel structures, improved efficacy and improved safety.SOLUTION: The present invention provides a compound having the structure of the upper formula in the figure, or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, nitrogen oxide, isotope-labeled product, metabolite or prodrug thereof. In the formula, R1 and R2 are each hydrogen, halogen, C1-6 alkyl, C1-6 alkoxyl, or the like, or are connected with adjacent carbon atoms to form a 5- to 6-membered oxygen-containing heterocyclic ring; R3 is hydrogen or is connected with an ortho-carbon atom of R1 to form a 6-membered carbocyclic ring; and A is selected from one of the lower two formulas in the figure.SELECTED DRAWING: None

To provide STAT degraders and uses thereof.SOLUTION: The present invention provides compounds, compositions thereof, and methods of using the compositions. In some embodiments, the present invention provides a method of treating a hematologic malignancy selected from LGL leukemia (T cell and NK cell), cutaneous T cell lymphoma (CTCL), peripheral T cell lymphomas (PTCL, all subtypes including ALCL), diffuse large B cell lymphoma (DLBCL), acute myelogenous leukemia, multiple myeloma, and myelofibrosis.SELECTED DRAWING: None

The invention discloses a cell adhesion protein Nectin-4 targeted bicyclic peptide fluorescent probe and a preparation method thereof, the probe provided by the invention can be used for accurate detection of recurrent tumors and metastatic lymph nodes, and the probe is applied to rapid pathology and fluorescent surgical navigation in an operation. The method has the advantages of high signal-to-background ratio, high specificity and long imaging time window.

According to an embodiment of the present invention, there is provided a magnetic resonance image processing method, the magnetic resonance image processing method being performed by a magnetic resonance image processing apparatus, the magnetic resonance image processing method including: inputting an input image having a slice resolution higher than 0 and lower than 1 to an artificial neural network model; and outputting an output image having a slice resolution of 1 from the artificial neural network model.

The invention belongs to the field of medicines, and discloses an SERPINE1 protein degradation agent and application thereof. The general formula of the SERPINE1 protein degradation agent is # imgabs0 # or # imgabs1 #. The research finds that a structural fragment for inhibiting SERPINE1 protein and a structural sheet or a hydrophobic label of an E3 protein ligand are coupled together through a linker, the length of the linker is adjusted, the obtained SERPINE1 protein degradation agent has an unexpected anti-tumor effect, the anti-tumor effect of the SERPINE1 protein degradation agent is superior to that of a single SERPINE1 inhibitor, and the SERPINE1 protein degradation agent has a good application prospect. The drug resistance of tumor cells can be overcome, and the drug-forming target property is good.

The invention relates to application of a topoisomerase inhibitor and a conjugate thereof. Specifically, the inventor provides a class of camptothecin derivatives, linker conjugates and antibody-drug conjugates with novel structures, and the camptothecin derivatives, linker conjugates and antibody-drug conjugates have excellent anti-tumor activity and good lipophilicity. In-vitro and in-vivo experiments show that the drug conjugate containing the camptothecin derivative disclosed by the invention has an improved anti-tumor curative effect and high safety, and has an application prospect in the field of cancer treatment.

A compound comprising a prostate specific membrane antigen (PSMA)-targeting moiety of the following formula (I) or of a salt or a solvate thereof. R1 is —R1aR1b— wherein R1a is absent, —CH2—, —O—, or —S—, and R1b is —CH2— or —CHF—. R2 is —(CH2)3—O—, —(CH2)3—, —(CH2)4—, —CH2—O—(CH2)2—, or —CH2—S—(CH2)2. R3 is ethylene fused to a tricyclic fused ring. L1, L2, L3, L4, L5b L5c, L6 and L7 are linkages (e.g. peptide bonds). Xbr is a branching atom. Rrad is a radiometal chelator. Ralb is an albumin binder. n1, n2, n3, n4, and n5 are integers. When the PSMA-targeting moiety is linked to a radiolabeling group, the compound may be used as an imaging agent or therapeutic agent for PSMA-expressing diseases / conditions.

The invention described herein pertains to the diagnosis, imaging, and / or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and / or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

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 invention relates to an azobenzene-containing connexon as shown in a formula I, a protein coupling medicine containing the connexon and application of the connexon, further relates to a pharmaceutical composition containing the protein coupling medicine, and further relates to application of the protein coupling medicine for treating and / or preventing diseases. # imgabs0 #

To provide non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides.SOLUTION: The dolastatin analogs may have a wide range of possible functional groups, but typically have at least one oxime, carbonyl, dicarbonyl, and / or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and / or hydroxylamine group.SELECTED DRAWING: Figure 4