http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110548151-B
Outgoing Links
Predicate | Object |
---|---|
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-54 |
filingDate | 2018-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2020-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2020-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-110548151-B |
titleOfInvention | Design method of covalent drug |
abstract | The invention relates to a design method of a covalent drug, belonging to the technical field of targeted drugs. The invention solves the technical problem of providing a design method of covalent drugs. The approach is primarily to design covalent inhibitors by targeting specific residues at the periphery of the binding pocket. The main body part of the drug molecule is combined with the binding site, the covalent reaction target head and the specific amino acid residue on the periphery of the pocket form covalent binding, and the linker part is connected with the reaction target head and the main body part. The main structure of the drug molecule is not changed, the combination of the main part and the combination site is not influenced, and meanwhile, the covalent bond formed by the drug molecule and specific amino acid residues on the periphery of the pocket can greatly increase the combination capacity of the compound molecule and the target protein, thereby obtaining lasting and strong biological activity. By using the method, even if no covalent reactive residue exists in the binding pocket, the covalent inhibitor can be developed according to specific amino acid around the pocket, thereby greatly widening the design thought and application range of the covalent drug. |
priorityDate | 2018-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 64.