Phthalimide conjugation as a strategy for in vivo target protein degradation

Science

Volumn 348, Issue 6241, 2015, Pages 1376-1381

  Winter, Georg E ^a   Buckley, Dennis L ^a   Paulk, Joshiawa ^a   Roberts, Justin M ^a   Souza, Amanda ^a   Dhe Paganon, Sirano ^a   Bradner, James E ^a,b  

^a DANA FARBER CANCER INSTITUTE   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 CHLOROPHENYL) 2,3,9 TRIMETHYL 6H THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE 6 ACETIC ACID TERT BUTYL ESTER; ANTINEOPLASTIC AGENT; BRD4 PROTEIN; DBET1; FKBP12 PROTEIN; PHTHALIMIDE; PROMYELOCYTIC LEUKEMIA PROTEIN; SCAFFOLD PROTEIN; TRANSCRIPTION FACTOR; TUMOR PROTEIN; UBIQUITIN CONJUGATING ENZYME E2; UBIQUITIN PROTEIN LIGASE E3; UNCLASSIFIED DRUG; AZEPINE DERIVATIVE; BRD4 PROTEIN, HUMAN; CRBN PROTEIN, HUMAN; DBET1 COMPOUND; FK 506 BINDING PROTEIN; LIGAND; NUCLEAR PROTEIN; PEPTIDE HYDROLASE; PHTHALIMIDE DERIVATIVE; THALIDOMIDE; UBIQUITIN PROTEIN LIGASE;

CYTOLOGY; DEGRADATION; ENZYME ACTIVITY; INHIBITOR; LIGAND; MOLECULAR ANALYSIS; PROBE; PROTEIN; RODENT;

ACUTE MYELOBLASTIC LEUKEMIA; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CANCER GROWTH; CANCER SURVIVAL; CONCENTRATION RESPONSE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOWN REGULATION; DRUG CONJUGATION; DRUG EFFICACY; DRUG TOLERABILITY; FLUORESCENCE ACTIVATED CELL SORTING; HUMAN; HUMAN CELL; IMMUNOBLOTTING; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROMYELOCYTIC LEUKEMIA; PROTEIN DEGRADATION; PROTEIN EXPRESSION; PROTEIN STABILITY; PROTEIN TARGETING; SIGNAL TRANSDUCTION; TUMOR GROWTH; TUMOR VOLUME; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DISEASE MODEL; DRUG DESIGN; DRUG EFFECTS; LEUKEMIA, PROMYELOCYTIC, ACUTE; METABOLISM; MOLECULARLY TARGETED THERAPY; PROTEIN TERTIARY STRUCTURE; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

MUS;

ANIMALS; AZEPINES; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DRUG DESIGN; LEUKEMIA, PROMYELOCYTIC, ACUTE; LIGANDS; MICE; MOLECULAR TARGETED THERAPY; NUCLEAR PROTEINS; PEPTIDE HYDROLASES; PHTHALIMIDES; PROTEIN STABILITY; PROTEIN STRUCTURE, TERTIARY; PROTEOLYSIS; TACROLIMUS BINDING PROTEIN 1A; THALIDOMIDE; TRANSCRIPTION FACTORS; UBIQUITIN-PROTEIN LIGASES;

EID: 84932634729     PISSN: 00368075     EISSN: 10959203     Source Type: Journal    
DOI: 10.1126/science.aab1433     Document Type: Article

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