PROTACs (Proteolysis Targeting Chimeras)
GPTKB entity
Statements (51)
| Predicate | Object |
|---|---|
| gptkbp:instanceOf |
gptkb:biotechnology
protein degradation technology drug discovery technology |
| gptkbp:abbreviation |
PROTACs
|
| gptkbp:advantage |
can degrade rather than inhibit proteins
potential to overcome drug resistance |
| gptkbp:application |
gptkb:cancer
drug development neurodegenerative disease research |
| gptkbp:category |
small molecules
heterobifunctional molecules targeted therapeutics |
| gptkbp:companyResearching |
gptkb:Pfizer
gptkb:Arvinas gptkb:Genentech gptkb:Novartis gptkb:Bristol_Myers_Squibb gptkb:Kymera_Therapeutics gptkb:C4_Therapeutics gptkb:Nurix_Therapeutics |
| gptkbp:component |
chemical linker
ligand for target protein ligand for E3 ubiquitin ligase |
| gptkbp:example |
gptkb:KT-474
gptkb:ARV-110 gptkb:ARV-471 CFT7455 CC-90009 DT2216 NX-2127 PROTAC-BCL-xL |
| gptkbp:firstDescribed |
2001
|
| gptkbp:fullName |
Proteolysis Targeting Chimeras
|
| gptkbp:function |
induce targeted protein degradation
|
| https://www.w3.org/2000/01/rdf-schema#label |
PROTACs (Proteolysis Targeting Chimeras)
|
| gptkbp:inventedBy |
gptkb:Raymond_Deshaies
gptkb:Craig_Crews |
| gptkbp:limitation |
cell permeability challenges
pharmacokinetic limitations potential off-target effects |
| gptkbp:mechanismOfAction |
hijack ubiquitin-proteasome system
|
| gptkbp:relatedTo |
gptkb:proteasome
gptkb:ubiquitin_ligase targeted protein degradation molecular glues |
| gptkbp:target |
disease-causing proteins
undruggable proteins |
| gptkbp:usedIn |
clinical trials
preclinical studies |
| gptkbp:bfsParent |
gptkb:Oerth_Bio
|
| gptkbp:bfsLayer |
7
|