Targeted Protein Degradation

URI: https://gptkb.org/entity/Targeted_Protein_Degradation
GPTKB entity
Statements (44)
Predicate Object
gptkbp:instanceOf gptkb:biological_pathway
gptkb:drug_discovery_strategy
gptkbp:advantage broader target space
catalytic mode of action
overcomes limitations of traditional inhibitors
potential for lower dosing
gptkbp:clinicalTrialPhase gptkb:NCT03888612
gptkb:NCT04072952
gptkbp:enables removal of disease-causing proteins
targeting undruggable proteins
gptkbp:example gptkb:ARV-110
gptkb:ARV-471
gptkb:dBET1
CC-90009
gptkbp:fieldOfStudy gptkb:pharmacy
chemical biology
molecular biology
gptkbp:firstDescribed early 2000s
gptkbp:hasApplication gptkb:cancer
therapeutics
neurodegenerative disease treatment
gptkbp:hasPatent US patents on PROTACs
gptkbp:limitation drug resistance
delivery challenges
off-target effects
gptkbp:mechanismOfAction ubiquitin-proteasome system
lysosomal degradation
gptkbp:publishedIn gptkb:Nature_Reviews_Drug_Discovery
gptkb:Annual_Review_of_Pharmacology_and_Toxicology
gptkb:Cell_Chemical_Biology
gptkbp:relatedTo gptkb:targeted_therapy
gptkb:E3_ubiquitin_ligase
small molecule drugs
protein homeostasis
gptkbp:studiedBy academic institutions
pharmaceutical companies
gptkbp:technology gptkb:AUTACs
gptkb:LYTACs
Degronimids
PROTACs
molecular glues
gptkbp:bfsParent gptkb:Kymera_Therapeutics
gptkbp:bfsLayer 7
https://www.w3.org/2000/01/rdf-schema#label Targeted Protein Degradation