20 results about "Selective degradation" patented technology

The present disclosure relates to a novel class of bifunctional molecules that are useful in a targeted or selective degradation of a protein.

The invention relates to an application of a PROTAC compound targeting M2-1 protein in preparation of an anti-RSV (Respiratory Syndrome Virus) drug, and belongs to the technical field of biological medicines. According to the invention, by constructing bifunctional micromolecules capable of simultaneously combining the M2-1 protein and CRBN E3 ubiquitin ligase, selective degradation of the M2-1 protein is realized, the limitation that the protein cannot be effectively targeted in the prior art is broken through, and a new technical approach is provided for solving the problems of single target spot, high drug resistance risk, lack of specific drugs and the like in RSV infection treatment; the method has obvious novelty and substantial progress.

The present application relates to a controllable degradation of siliconized DNA hydrogel and its preparation method and application, the hydrogel is assembled into a three-dimensional network through the DNA structure with single-stranded region in the center and linear DNA structure, and the mechanical properties and thermal stability thereof are improved through in-situ siliconization. The precisely designed single-stranded region can still be recognized and degraded by specific nucleic acid enzyme after siliconization, realizing the accurate control of selective degradation. Taking human umbilical vein endothelial cells as an example, the present application verifies the good biocompatibility of the material, and the present application can be used for cell embedding and release, and is suitable for advanced biological materials, medical, pharmaceutical and other research and application fields such as organoid culture, tissue engineering and controllable drug release.

This invention relates to binding molecules comprising a TRIM21 binding portion and a protein binding portion for the selective degradation of target proteins. The invention also relates to compositions comprising these molecules and their use in therapies. Furthermore, the invention relates to TRIM21 binding molecules and their use.

The invention belongs to the technical field of biological medicines, and particularly relates to an mTORC1 selective degradation agent containing a hydrophobic label as well as a synthesis method and application of the mTORC1 selective degradation agent. The structural formula of the degradation agent is as shown in formula I. Representative compounds have the effect of inhibiting proliferation of various tumor cells, and can provide new research and development thoughts and directions for anti-tumor drugs. .

Compounds and compositions that have a Mannose 6-Phosphate Receptor Ligand bound to an Extracellular Protein Binding Ligand are provided for the selective degradation of a target extracellular protein in vivo to treat disorders mediated by the extracellular protein.

The invention discloses an iron-based nano-enzyme targeting chimera as well as a preparation method and application thereof. According to the chimera, lipidosome is used as a carrier, a coordination active center is constructed by Plerixabor with CXCR4 high affinity and iron ions, selective adsorption of transferrin is achieved through surface chemical design, and double-target tumor targeted enrichment is achieved by means of TfR1-mediated rapid endocytosis. And meanwhile, selective degradation of CXCR4 through a lysosome way is accelerated, so that synergistic treatment of'blocking transfer signals-chemical kinetics killing 'is realized. The preparation provided by the invention has good biocompatibility and expandability. The platform has the advantages of molecular recognition, protein crown regulation and control, microenvironment response and the like, is suitable for precise treatment of various tumors with high CXCR4 expression, and can be used as a universal membrane protein degradation and chemical kinetics treatment integrated carrier to be expanded and applied.

The invention provides a heterocyclic compound as well as a composition and application thereof. Specifically provided is a compound represented by formula II or a pharmaceutically acceptable salt thereof. The compound has one or more of the following advantages: the structure is novel, IKZF2 can be efficiently and highly selectively degraded, the functions of T cells are inhibited and regulated, the compound is applied to treatment of tumors or diseases, and the compound has huge clinical development value.

The invention discloses a PROTAC compound for degrading PAK5 as well as a preparation method and application of the PROTAC compound, and belongs to the technical field of biological medicines. The PROTAC molecule provided by the invention has obvious enzymatic activity for inhibiting PAK5 kinase and has good protein degradation activity on PAK5, so that the PROTAC molecule can be used for preparing a targeted PAK5 inhibitor or a targeted PAK5 degradation agent, and the PROTAC molecule provided by the invention also has a good selective degradation effect on PAK5 and can be used for preparing a targeted PAK5 inhibitor or a targeted PAK5 degradation agent. Particularly, the compound PL15 shows high selectivity for PAK5 protein degradation activity of more than 1000 times, so that the PROTAC molecule provided by the invention has relatively good application potential in treatment of tumors such as breast cancer and liver cancer mediated by PAK5.

A composition and method for the selective degradation of integrins, for example, used in the treatment of fibrosis, is provided. The compound of interest is a bifunctional integrin degradation molecule comprising a TG2 binding moiety linked to an integrin binding moiety.

The invention discloses a novel chemical upgrading and recycling method for polysulfone special engineering plastics, and belongs to the technical field of solid waste treatment. According to the method disclosed by the invention, high-yield metal is adopted as a photocatalyst, and various commercialized polysulfone plastic resins and (waste) polysulfone special engineering plastics can be degraded into diaryl ether high-added-value fine chemicals in a high-selectivity manner under room-temperature visible light illumination. The method disclosed by the invention has the advantages of low energy consumption, low cost, less pollution, single selectivity and the like, and has a wide application prospect in the field of high-added-value recovery treatment of the waste polysulfone special engineering plastics.

Disclosed in the present invention are a class of selective mTORC1 degraders based on an autophagy-lysosome pathway, a preparation method therefor, and the use thereof. The prepared rapamycin derivative exhibits an in vitro anti-MCF7 tumor cell activity comparable to that of rapamycin, and can achieve the selective degradation of mTORC1, while the protein level in mTORC2 is not affected.

This invention provides a highly efficient continuous cleaning system for waste PET bottle flakes used for recycling polyester staple fibers, relating to the field of resource recycling technology. It includes a three-stage linkage cleaning module, an integrated continuous conveying system, a wastewater recycling system, a precision sorting module, and an AI visual recognition + multi-sensor fusion control system. The three-stage linkage cleaning module employs a physical-chemical-biological synergistic approach to simultaneously remove three types of impurities from the bottle flake surface: label adhesive, grease, and stains. This invention constructs a three-stage linkage cleaning module that combines low-temperature embrittlement, enzymatic pre-degradation, and high-frequency ultrasound to achieve synergistic physical-chemical-biological decontamination, enabling the simultaneous and efficient removal of label adhesive, grease, and stains. Low-temperature embrittlement rapidly cracks the adhesive layer; enzymatic pre-degradation selectively degrades grease and protein-based stains under alkaline-free conditions, avoiding thermal degradation of the PET molecular chains.

Compositions and methods for selective degradation of integrin are provided, which are useful, for example, in the treatment of fibrosis. A compound of interest as a bifunctional integrin degrading molecule comprises a TG2 binding moiety linked to an integrin binding moiety.

The application relates to a method for degrading antibiotics by friction-activated peroxymonosulfate of a transition bimetallic catalyst and application. 1 Compared with the prior art, the application has better degradation effect on antibiotics, has the advantages of promoting multi-path O2 generation, realizing non-radical dominant selective degradation of electron-rich antibiotics, etc., and has great potential in practical application of antibiotic wastewater treatment.

The application belongs to the technical field of chemical medicine synthesis, and particularly relates to a proteolysis targeting chimera, a preparation method, a pharmaceutical composition and purposes thereof. The structural formula of the proteolysis targeting chimera is shown in formula Ia or formula Ib; the preparation process is simple and easy to operate; the proteolysis targeting chimera or pharmaceutically acceptable salt thereof prepared has the effect of efficiently degrading CDK2 / 4 / 6 / 9 and has high selectivity; and experimental results show that the compound can induce the targeted degradation of CDK2 / 4 / 6 / 9 protein by using the ubiquitin-proteasome system, inhibit the downstream signal pathway, realize the selective degradation of CDK2 / 4 / 6 / 9 at the protein level, cell level and animal level, and has a good effect of resisting the proliferation of prostate cancer cells.

The invention discloses a modularized protein-targeted autophagy degradation platform based on a bispecific nano antibody. The platform is formed by fusing a target protein recognition module, a spatial conformation regulation and control module and an autophagy receptor capture module through covalent peptide bonds. According to the invention, through molecular dynamics simulation and free energy screening, a topological configuration with Target-Linker-p62 as a core is accurately locked, and G8 (octa-polyglycine) is preferably selected as a connecting arm to eliminate steric hindrance. Experiments prove that the platform has extremely high affinity to target proteins (HSP90 and GRP78) and a receptor p62 and can efficiently induce selective degradation of specific proteins in tumor cells. The method has the advantages of being stable in structure, high in degradation efficiency, high in universality and the like, and a new means is provided for research and development of anti-tumor drugs.

This invention uses waste tires as a carbon source and Ni(NO3)2·6H2O and Fe(NO3)3·9H2O metal precursors to prepare NiFe2O4@C x (x=0.5, 1, 2, 4) porous and fluffy carbon materials were synthesized using a simple and ultrafast microwave-mediated solid-state synthesis of biochar materials derived from waste tires. Rapid microwave treatment not only facilitates the construction of porous and fluffy structures and the formation and exposure of more active sites, but also accelerates mass transfer during the catalytic process. The NiFe2O4 in NiFe2O4@C1 and its large specific surface area can promote the activation of non-free radicals by peroxymonosulfate (PMS). 1 NiFe2O4@C1 system exhibited excellent catalytic performance in the selective degradation of antibiotics with low vertical ionization potential (VIP) using O2. It completely removed oxytetracycline hydrochloride (OTC) within 10 minutes during the catalytic activation of PMS. Furthermore, the NiFe2O4@C1 / PMS system demonstrated highly efficient selective degradation in degradation tests of other antibiotics with low vertical ionization potentials.

The application discloses a kind of selective mTORC1 degradation agent based on autophagy-lysosome pathway and its preparation method and application, belong to the field of biological medicine technology.The application based on autophagy degradation proposes the concept of selective mTORC1 degradation, designs and synthesizes three kinds of rapamycin derivatives, and the in-vitro anti-MCF7 tumor cell activity of representative compound can be comparable with positive drug rapamycin;The rapamycin derivative obtained by the application can realize the selective degradation of mTORC1, and the degradation process is related to autophagy, while the protein level in mTORC2 is not affected.The selective mTORC1 degradation agent obtained by the application can bring new ideas and potential drug research and development direction for the treatment of related diseases, and also provides a powerful tool for in-depth study of the function and regulation mechanism of mTORC1.

The invention discloses a chimera (Protac) compound for targeted degradation of GSK-3beta protein. X1 is selected from one of alkyl chains of C1-C6, alkyl chains of C3-C8 and containing thioether, and alkyl chains of C3-C8 and containing ether; the gene has the activity of selectively degrading GSK-3beta protein and promoting the repair activity of non-homologous end-linked DNA in cells. The invention also provides a preparation method of the compound. The invention relates to pharmaceutically acceptable salts and carriers of the compounds. The invention also relates to an application in preparation of drugs for inhibiting GSK-3beta activity or drugs for DNA damage repair and radiation damage protection. The invention develops the GSK-3beta inhibitor with low toxicity, high efficiency and strong specificity, so that the GSK-3beta inhibitor reaches substoichiometry, the administration frequency is reduced, the GSK-3beta inhibitor is friendly to targeted GSK-3beta diseases, and a new way is opened up for the application of targeted GSK-3beta treatment drugs.