proteolysis-targeting chimera (PROTAC)
GPTKB entity
Statements (34)
| Predicate | Object |
|---|---|
| gptkbp:instanceOf |
small molecule
drug discovery technology |
| gptkbp:advantage |
can degrade rather than inhibit proteins
potential for lower drug resistance |
| gptkbp:application |
cancer therapy research
neurodegenerative disease research targeted protein degradation in drug discovery |
| gptkbp:component |
chemical linker
ligand for E3 ligase ligand for target protein |
| gptkbp:developedBy |
gptkb:Raymond_Deshaies
gptkb:Craig_Crews |
| gptkbp:example |
gptkb:ARV-110
gptkb:ARV-471 |
| gptkbp:firstDescribed |
2001
|
| gptkbp:function |
induces targeted protein degradation
|
| gptkbp:hasCompany |
gptkb:Arvinas
gptkb:Kymera_Therapeutics gptkb:C4_Therapeutics |
| https://www.w3.org/2000/01/rdf-schema#label |
proteolysis-targeting chimera (PROTAC)
|
| gptkbp:limitation |
cell permeability challenges
pharmacokinetic challenges |
| gptkbp:mechanismOfAction |
induces ubiquitination of target protein
leads to proteasomal degradation recruits E3 ubiquitin ligase to target protein |
| gptkbp:relatedTo |
targeted protein degradation
ubiquitin-proteasome system molecular glues |
| gptkbp:target |
disease-causing proteins
undruggable proteins |
| gptkbp:used_in |
clinical trials
preclinical studies |
| gptkbp:bfsParent |
gptkb:Obsidian_Therapeutics
|
| gptkbp:bfsLayer |
7
|