Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity - Pillow, Thomas H.; Adhikari, Pragya; Blake, Robert A.; Chen, Jinhua; Del Rosario, Geoffrey; Deshmukh, Gauri; Figueroa, Isabel; Gascoigne, Karen E.; Kamath, Amrita V.; Kaufman, Susan; Kleinheinz, Tracy; Kozak, Katherine R.; et al. (ChemMedChem, 2020)
Keywords: Animals; Antibodies; Antibodies, Monoclonal - chemistry; Antibodies, Monoclonal - immunology; antibody-drug conjugate; Antigens; Biodegradation; BRD4; Cell Cycle Proteins - antagonists & inhibitors; Cell Cycle Proteins - metabolism; Cell Line, Tumor; Cell Survival - drug effects; Chemical properties; Chemistry, Medicinal; chimeric protein degrader; Conjugates; Conjugation; Degradation; Drug Carriers - chemistry; drug delivery; Female; Half-Life; Heterocyclic Compounds, 4 or More Rings - chemistry; Humans; Immunoconjugates - chemistry; Immunoconjugates - pharmacology; Immunoconjugates - therapeutic use; Lectins, C-Type - immunology; Leukemia, Myeloid, Acute - drug therapy; Leukemia, Myeloid, Acute - pathology; Life Sciences & Biomedicine; Mice; Mice, SCID; Organic chemistry; Pharmacokinetics; Pharmacology; Pharmacology & Pharmacy; Protein Binding; Proteins; Proteolysis - drug effects; Proto-Oncogene Proteins c-myc - genetics; Proto-Oncogene Proteins c-myc - metabolism; Receptors, Mitogen - immunology; Science & Technology; Surface Plasmon Resonance; Transcription Factors - antagonists & inhibitors; Transcription Factors - metabolism; Von Hippel-Lindau Tumor Suppressor Protein - metabolism; Xenograft Model Antitumor Assays; DRUG; STRATEGY; LETHAL ACTIVITY; drug delivery; DOSE-ESCALATION; antibody-drug conjugate; THERAPY; chimeric protein degrader; BROMODOMAIN INHIBITOR OTX015; PROTEIN-DEGRADATION; LYMPHOMA; antibodies; LEUKEMIA; KNOCKDOWN; BRD4