Design, synthesis, and evaluation of linker-duocarmycin payloads: Toward selection of HER2-targeting antibody-drug conjugate SYD985

Molecular Pharmaceutics

Volumn 12, Issue 6, 2015, Pages 1813-1835

  Elgersma, Ronald C ^a   Coumans, Ruud G E ^a   Huijbregts, Tijl ^a   Menge, Wiro M P B ^a   Joosten, John A F ^a   Spijker, Henri J ^a   De Groot, Franciscus M H ^a   Van Der Lee, Miranda M C ^a   Ubink, Ruud ^a   Van Den Dobbelsteen, Diels J ^a   Egging, David F ^a   Dokter, Wim H A ^a   Verheijden, Gijs F M ^a   Lemmens, Jacques M ^a   Timmers, C Marco ^a   Beusker, Patrick H ^a  

^a SYNTHON BV   (Netherlands)

Author keywords

ADC; antibody drug conjugate; design; drug targeting; DUBA; duocarmycin; HER2; linker duocarmycin; seco DUBA; structure activity relationship; SYD983; SYD985

Indexed keywords

ANTIBODY CONJUGATE; ANTINEOPLASTIC AGENT; DUOCARMYCIN DERIVATIVE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; SECODUOCARMYCIN; SYD 981; SYD 982; SYD 983; SYD 984; SYD 985; TRASTUZUMAB; UNCLASSIFIED DRUG; 2 PYRROLIDONE DERIVATIVE; DUOCARMYCIN A; INDOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL LINE; CONTROLLED STUDY; CYCLIZATION; CYTOTOXICITY; DNA ALKYLATION; DNA BINDING; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; HYDROPHOBIC INTERACTION CHROMATOGRAPHY; MACACA FASCICULARIS; MOUSE; NONHUMAN; PLASMA; PRIORITY JOURNAL; RAT; TUMOR XENOGRAFT; CHEMISTRY; METABOLISM; TUMOR CELL LINE;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; HUMANS; IMMUNOCONJUGATES; INDOLES; PYRROLIDINONES; RECEPTOR, ERBB-2;

EID: 84930626816     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp500781a     Document Type: Article

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