http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2010535202-A
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02A50-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-20 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07H19-167 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7076 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H19-167 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-00 |
| filingDate | 2008-08-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2010-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | JP-2010535202-A |
| titleOfInvention | 5'-substituted adenosine, its preparation and use as an inhibitor of S-adenosylmethionine decarboxylase |
| abstract | The present invention provides a 5'-substituted adenosine, its production and use as an inhibitor of S-adenosylmethionine decarboxylase. The crystal structure of a complex of S-adenosylmethionine methyl ester and mutant hAdoMetDC F223A is considered to have eliminated the stacking of aromatic rings of F7, adenine and F223 in the crystal structure. . In the structure of this mutant with an ester added, the π-π interaction with F7, hydrogen bonding with the backbone of Glu67, and electrostatic interaction contribute to maintain the syn conformation of the ligand unchanged. The Several AdoMet substrate analogs in which the 8 position of adenine was substituted with various groups were synthesized and analyzed for their hAdoMetDC inhibitory ability. In understanding this result, virtual modeling of the enzyme inhibitor complex was performed and 5′-deoxy-5 ′-[N-methyl-N- [2- (aminooxy) ethyl] amino-8-methyl] adenosine. The crystal structure of human AdoMetDC with (MAOEMA) and 5'-deoxy-5 '-[N-methyl-N- [4- (aminooxy) butyl] amino-8-ethyl] adenosine (MAOBEA) bound to the active site. Determined experimentally. [Selection] Figure 4 |
| priorityDate | 2007-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 430.