Molecular basis of valine-citrulline-PABC linker instability in site-specific ADCs and its mitigation by linker design

Molecular Cancer Therapeutics

Volumn 15, Issue 5, 2016, Pages 958-970

  Dorywalska, Magdalena ^a   Dushin, Russell ^a   Moine, Ludivine ^a   Farias, Santiago E ^a   Zhou, Dahui ^a   Navaratnam, Thayalan ^a,b   Lui, Victor ^a   Hasa Moreno, Adela ^a   Casas, Meritxell Galindo ^a   Tran, Thomas Toan ^a   Delaria, Kathy ^a   Liu, Shu Hui ^a   Foletti, Davide ^a,c   O'Donnell, Christopher J ^a   Pons, Jaume ^a,d   Shelton, David L ^a   Rajpal, Arvind ^a,e   Strop, Pavel ^a,e  

^a PFIZER INC   (United States)

^b Toronto Research Chemicals   (Canada)

^c 23andMe ^*  (United States)

^d Alexo Therapeutics   (United States)

^e Bristol Myers Squibb   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (2 AMINOETHYL)BENZENESULFONYL FLUORIDE; ALBUMIN; AMMONIUM SULFATE; ANTIBODY CONJUGATE; ANTIBODY DRUG CONJUGATE; CARBOXYLESTERASE; CARBOXYLESTERASE 1C; CATHEPSIN B; CITRULLINE; DIPEPTIDE; HYDROLASE; IMMUNOGLOBULIN; MALEIMIDE; PROTEINASE; RECOMBINANT PROTEIN; UNCLASSIFIED DRUG; VALINE; ANTINEOPLASTIC AGENT; BIOLOGICAL MARKER; CARBAMIC ACID DERIVATIVE; MONOCLONAL ANTIBODY; PROTEIN BINDING;

ANIMAL CELL; ANIMAL EXPERIMENT; ANION EXCHANGE CHROMATOGRAPHY; ARTICLE; BINDING SITE; CHEMICAL MODIFICATION; COMPARATIVE STUDY; CONTROLLED STUDY; CYTOTOXICITY ASSAY; DERIVATIZATION; DRUG CONJUGATION; ENZYMATIC ASSAY; ENZYME ACTIVITY; ENZYME ANALYSIS; ENZYME BLOOD LEVEL; ENZYME INHIBITION; ENZYME LINKED IMMUNOSORBENT ASSAY; FEMALE; HUMAN; HUMAN CELL; HYDROLYSIS; IN VITRO STUDY; IN VIVO STUDY; ION EXCHANGE CHROMATOGRAPHY; LIQUID CHROMATOGRAPHY; MOUSE; NONHUMAN; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRECIPITATION; PRIORITY JOURNAL; PROTEIN PURIFICATION; PROTEOMICS; SIZE EXCLUSION CHROMATOGRAPHY; STEREOSPECIFICITY; TANDEM MASS SPECTROMETRY; WESTERN BLOTTING; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG DESIGN; DRUG STABILITY; KNOCKOUT MOUSE; METABOLISM; MOLECULAR MODEL; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTIBODIES, MONOCLONAL; ANTINEOPLASTIC AGENTS; BIOMARKERS; CARBAMATES; CARBOXYLESTERASE; CITRULLINE; DRUG DESIGN; DRUG STABILITY; HUMANS; IMMUNOCONJUGATES; MICE; MICE, KNOCKOUT; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR STRUCTURE; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP; VALINE;

EID: 84969509943     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-15-1004     Document Type: Article

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