| Predicate |
Object |
| assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_68c213ba9952360f439567152e047b18 |
| classificationCPCAdditional |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2500-10
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K2319-20
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K2319-95 |
| classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-5008
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K1-13
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12N9-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-52
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-573
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 |
| classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K17-02
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-708
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7076
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-66
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-00 |
| filingDate |
2011-12-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_52afe5a6ff4f61029b1f8c967e44aafe
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9c9b7c2e0b9747f21c771ba3966f0687
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_651c3c5254eeb64fea9cdacbb63e37db
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b2db3a2f9054344ca9e2965c0f823212
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3a0f463cd234fbb4cd5f17eedfb3ebd8 |
| publicationDate |
2014-01-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber |
CN-103502275-A |
| titleOfInvention |
Small-molecule hydrophobic labeling of fusion proteins and their resulting degradation |
| abstract |
The present invention relates to the ability to modulate any protein of interest with small molecules in living systems. In particular, the present invention relates to the discovery that attachment of hydrophobic moieties to the surface of a protein mimics the partially denatured state of the protein, allowing cellular quality control machinery to induce its proteasomal degradation. Aspects of the invention relate to bifunctional small molecules that bind proteins including, for example, self-labeling tags such as bacterial dehalogenases (HaloTag proteins) and present hydrophobic groups on their surface. Hydrophobic labeling of HaloTag proteins with hydrophobic moieties (eg, adamantyl moieties) is achieved, and the labeling causes degradation of cytosolic, prenylated and transmembrane fusion proteins in cell culture. The present invention also demonstrates the in vivo usefulness of hydrophobic markers by degrading proteins expressed in zebrafish embryos and by inhibiting RasG12V-driven tumor development in mice. Thus, the hydrophobically tagged HaloTag fusion protein provides small molecule control over any protein of interest, making it an ideal system for identifying potential drug targets in disease models. |
| isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-107828876-A
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-107922927-A |
| priorityDate |
2010-12-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type |
http://data.epo.org/linked-data/def/patent/Publication |