Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Cell Chemical Biology

Volumn 25, Issue 1, 2018, Pages 78-87.e5

  Bondeson, Daniel P ^a   Smith, Blake E ^a   Burslem, George M ^a   Buhimschi, Alexandru D ^a   Hines, John ^a   Jaime Figueroa, Saul ^a   Wang, Jing ^b   Hamman, Brian D ^b   Ishchenko, Alexey ^b   Crews, Craig M ^a  

^a YALE UNIVERSITY   (United States)

^b Arvinas Inc   (United States)

Author keywords

chemical biology; CRBN; MAPK p38; PROTACs; protein degradation; protein protein interactions; proteomics; selective degradation; ternary complex; VHL

Indexed keywords

FORETINIB; LIGASE; MESSENGER RNA; MITOGEN ACTIVATED PROTEIN KINASE 14; PHOSPHOTRANSFERASE; PROTEASOME; UBIQUITIN PROTEIN LIGASE E3; PROTEIN KINASE INHIBITOR; UBIQUITIN PROTEIN LIGASE;

ARTICLE; BINDING AFFINITY; CHIMERA; COMPLEX FORMATION; CONTROLLED STUDY; DRUG POTENCY; DRUG PROTEIN BINDING; MDA-MB-231 CELL LINE; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN PROTEIN INTERACTION; PROTEIN STABILITY; PROTEIN TARGETING; PROTEOMICS; UBIQUITINATION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DESIGN; DRUG EFFECT; HUMAN; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; SYNTHESIS;

DRUG DESIGN; HUMANS; PROTEASOME ENDOPEPTIDASE COMPLEX; PROTEIN KINASE INHIBITORS; PROTEOLYSIS; SMALL MOLECULE LIBRARIES; UBIQUITIN-PROTEIN LIGASES; UBIQUITINATION;

EID: 85033403065     PISSN: 24519456     EISSN: 24519448     Source Type: Journal    
DOI: 10.1016/j.chembiol.2017.09.010     Document Type: Article

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