15 results about "Chemical ligation" patented technology

The invention belongs to the technical field of medical chemistry, and particularly relates to a targeted protein degradation compound containing an SYVN1 binding compound and application of the targeted protein degradation compound. According to the invention, a series of compounds interacting with SYVN1 are found, and the compounds can be used as'warheads' to participate in ERAD and effectively degrade transmembrane protein targets. Based on the SYVN1 binding compound, a new TPD technology for hijacking ERAD is established, and a brand new platform is provided for processing TMSPs and other proteins which are difficult to target by the current TPD technology. A SYVN1 interaction compound is further connected with a known ligand interacting with a protein target through a chemical linker, a series of ERADEC molecules are generated, the molecules can significantly degrade target protein, and a new possibility is provided for targeted degradation of drugs.

The application discloses a bifunctional compound and use thereof, the bifunctional compound is a bifunctional compound with K-L-S structure, wherein: K is a targeting group of cyclin 7CDK7;S is a covalent group targeting cysteine or lysine on CDK7 protein;L is a divalent linking group chemically connecting the targeting group K and the covalent group S;The bifunctional compound or does not contain divalent linking group L, and the targeting group K is directly connected with the covalent group S.The bifunctional compound or its pharmaceutically acceptable salt, ester, hydrate, solvate or stereoisomer and the pharmaceutical composition containing the same show pharmacological activity related to degradation, inhibition of target protein CDK7, and can be used for preventing and treating CDK7 related diseases or disorders.

The invention discloses a charge-assisted targeting cyclodextrin carrier molecule as well as a preparation method and application thereof, the cyclodextrin carrier molecule integrates cyclodextrin, an M2pep ligand and a pH response group through chemical connection to obtain a biologically safe carrier with a clear structure and simple components. The carrier molecule is used for loading a drug and constructing nanoparticles, and cyclodextrin is responsible for loading a fluorescent dye or a nuclear drug; the M2pep ligand provides an active targeting function for the tumor; on one hand, the pH response group adjusts the surface charge of the nano-particles to enable the nano-particles to be negatively charged and prolong the blood circulation time of the medicine, and on the other hand, the nano-particles respond to an acidic tumor microenvironment and are switched into positive charges to enhance the tumor targeting of the nano-particles. In addition, the nano-particles also have the characteristics of quickly developing tumors, retaining in the tumors for a long time and quickly removing in normal organs, so that the technical problems of low tumor drug delivery efficiency and more non-target organ accumulation in the prior art are solved.

The present invention provides a composition and a method for treating a disease associated with amyloid deposits of Aβ in a patient's brain, such as Alzheimer's disease. Such a method involves administering a pharmaceutical composition comprising an immunogenic fragment of Aβ capable of inducing a beneficial immune response in the form of an antibody against Aβ. The immunogenic fragment comprises a linear or polyvalent peptide of Aβ. The pharmaceutical composition comprises an immunogenic fragment chemically linked to a carrier molecule that can be administered together with an ajuvant.

This invention provides a polyfunctional chemical conjugation molecule that has been found to be useful as a modifier for target substrates. [Solution] A polyfunctional chemical conjugation molecule is provided, comprising a localization portion, a chemical linker portion, an activator portion, a first orientation adapter that interconnects the chemical linker portion to the activator portion at one end, and optionally a second orientation adapter that interconnects the chemical linker molecule to the localization portion at a different end. The molecule provides a use for post-translational modification of a polymer that is not a natural substrate of the activator portion. Diseases or disorders may be treated or prevented by this molecule.

Disclosed herein, in part, are novel calicheamicin derivatives with novel chemical linkers that include cleavable moieties and conjugated to targeting antibodies.

The present invention belongs to the technical field of medicinal chemistry, and specifically relates to a targeted protein degradation complex containing an SYVN1 binding compound and the use thereof. The present invention identifies a series of compounds that interact with SYVN1. The compounds can be used as "warheads" to participate in ERAD and effectively degrade transmembrane protein targets. On the basis of the SYVN1 binding compound, a new TPD technology for hijacking ERAD is established, providing a brand-new platform for treating TMSPs and other proteins that are difficult to target by means of current TPD technologies. Further, the compounds that interact with SYVN1 are linked, via a chemical linker, to a known ligand that interacts with a protein target, thereby generating a series of ERADEC molecules. The molecules can significantly degrade the target protein, providing a new possibility for a targeted degradation drug.

The invention provides a preparation method of a [mu]-conotoxin disulfide bond substitute, which comprises the following steps: on the basis of Fmoc solid-phase synthesis and DADA module embedding technology, coupling amino acid residues under the assistance of automatic microwaves to prepare a linear precursor peptide of [mu]-conotoxin, and carrying out in-situ oxidation and thiolysis activation on the linear precursor peptide to obtain the [mu]-conotoxin disulfide bond substitute. And carrying out folding oxidation on the obtained cyclized peptide by using natural chemical connection to assist cyclization so as to form the mu-conotoxin disulfide bond substitute. According to the method, the three-dimensional conformation and biological activity of the natural peptide are kept, meanwhile, efficient and rapid synthesis of the large-span disulfide bond substituted bridging peptide is achieved, the structural stability of the peptide product is remarkably improved, the reaction condition is mild and easy to control, the process is simple, the separation yield of the target product is stable, and the method can be used for rapidly preparing various variants and has wide application prospects. Different production and research requirements are met, and good market application prospects are achieved.

This invention relates to the field of advanced petrochemical new materials technology, and discloses a luminescent composite material, its preparation method, and its application. The composite material comprises the following components: homopolymer polypropylene, polybutylene succinate, a compatibility modification system, double-modified rare-earth strontium aluminate luminescent powder, dispersant, antioxidant, weathering agent, toughening agent, nucleating agent, and silane coupling agent. This invention employs a compatibility modification system composed of maleic anhydride-grafted PP-g-PBS copolymer and double-modified nano-montmorillonite. The maleic anhydride-grafted PP-g-PBS copolymer constructs a chemical link between the polypropylene and polybutylene succinate molecular chains through a grafting reaction, reducing the interfacial tension between the two resins. The double-modified nano-montmorillonite, after ionic liquid intercalation and silane grafting treatment, exhibits increased interlayer spacing and improved surface activity, uniformly dispersed in the matrix, and acts as a physical crosslinking point, improving the compatibility of the matrix resin and preventing phase separation.

Conventional cancer treatments are often ineffective, and therefore, there remains a need to develop more targeted and potent therapies to treat HCC. Antibody-drug conjugates (ADCs), which include antibodies that target GPC3 and are conjugated to cytotoxic drugs via a chemical linker, provide targeted therapies for treating patients with HCC tumors that express GPC3. [Solution] This disclosure provides GPC3 antibody-drug conjugates (ADCs), and includes compositions and methods for using such ADCs.

The invention relates to engineered lactobacillus plantarum outer vesicles targeting a cerebral infarction area and a preparation method thereof. The engineered lactobacillus plantarum outer vesicle targeting the cerebral infarction area is obtained by modifying the lactobacillus plantarum outer vesicle with E-selectin binding oligopeptide Esbp, and the engineered lactobacillus plantarum outer vesicle can well target a new target E-selectin of the cerebral infarction area, so that the outer vesicle is delivered to the cerebral infarction area to treat cerebral infarction. The engineered lactobacillus plantarum outer vesicle has the advantages of high acquisition speed, high yield, low cost and the like, and the chemical connection method is simple in synthesis step and lower in cost, so that the engineered lactobacillus plantarum outer vesicle targeting the cerebral infarction area has the characteristics of low cost and simplicity in preparation, and is suitable for industrial popularization and application.

This invention belongs to the fields of medicinal chemistry, glycochemistry, and biomedicine, and provides a fucoidan-based heparin pentasaccharide, its preparation method, and its applications. The preparation method involves the chemical linkage and purification of sulfated azidoethyl-α-L-pyranoside with alkyne-based heparin pentasaccharide to obtain the target product. This compound exerts anticoagulant and antithrombotic effects by potently inhibiting the intrinsic coagulation factor X enzyme complex (FXase). Its APTT prolongation and FXase inhibitory activity are significantly superior to heparin pentasaccharide, and it significantly reduces the risk of bleeding at equivalent antithrombotic doses. It can be used in the development of drugs or functional foods for thrombotic cardiovascular and cerebrovascular diseases.

The disclosure relates to the synthesis of amide containing compounds in flow. In particular, the disclosure relates to the synthesis of polypeptides via native chemical ligation in flow. The disclosure also relates to selective desulfurization or deselenization of amide containing compounds comprising a thiol, disulfide, selenol or diselenide functional group respectively, particularly polypeptides.

Disclosed are bifunctional degraders comprising electrophilic PRO-TACs that engage DCAF1 and pharmaceutical compositions comprising the same. The bifunctional degraders are of Formula A-B-C wherein, A is a ligand to a protein of interest, B is a linker that is a bond or a chemical linker that is chemically linked to A and C, and C is a ligand to the E3 ligase substrate receptor DCAF1, wherein the protein of interest is any protein having a ligand that can form a covalent bond with the linker B; and C comprises an azetidinyl acrylamide that forms a covalent bond with C1113 of DCAF1 through a Michael addition reaction.

Disclosed herein, in part, are novel calicheamicin derivatives with novel chemical linkers that include cleavable moieties and conjugated to targeting antibodies.