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Open AccessThe HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results
Approved antibody-drug conjugates (ADCs) for HER2-positive breast cancer include trastuzumab emtansine and trastuzumab deruxtecan. To develop a differentiated HER2 ADC, we chose an antibody that does not compe...
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Article
Open AccessSelective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is frequently mutated in cancer and inactivation results in a cellular dependence on its paralog, SMARCA2, thus making SMARCA2 an attract...
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Article
Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody–drug conjugates
The reversible attachment of a small-molecule drug to a carrier for targeted delivery can improve pharmacokinetics and the therapeutic index. Previous studies have reported the delivery of molecules that conta...
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Article
Mechanism-Based Pharmacokinetic/Pharmacodynamic Model for THIOMAB™ Drug Conjugates
THIOMAB™ drug conjugates (TDCs) with engineered cysteine residues allow site-specific drug conjugation and defined Drug-to-Antibody Ratios (DAR). In order to help elucidate the impact of drug-loading, conjugat...
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Article
Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates
Conjugating drugs to therapeutic antibodies is a promising strategy to increase their therapeutic efficacy. Shen et al. show that the local chemical environment of the conjugation site influences the in vivo stab...
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Article
In vivo monitoring of tumor relapse and metastasis using bioluminescent PC-3M-luc-C6 cells in murine models of human prostate cancer
We used the bioluminescent human prostate carcinoma cell line PC-3M-luc-C6 to non-invasively monitor in vivo growth and response of tumors and metastasis before, during and after treatments. Our goal was to deter...
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Article
Bioluminescent imaging (BLI) to improve and refine traditional murine models of tumor growth and metastasis
Bioluminescent imaging (BLI) permits sensitive in vivo detection and quantification of cells specifically engineered to emit visible light. Three stable human tumor cell lines engineered to express luciferase wer...