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  1. Article

    Open Access

    The 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...

    Gail D. Lewis, Guangmin Li, Jun Guo, Shang-Fan Yu in Nature Communications (2024)

  2. Article

    Open Access

    Selective 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...

    Jennifer Cantley, **aofen Ye, Emma Rousseau, Tom Januario in Nature Communications (2022)

  3. No Access

    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...

    Leanna R. Staben, Stefan G. Koenig, Sophie M. Lehar, Richard Vandlen in Nature Chemistry (2016)

  4. No Access

    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...

    Siddharth Sukumaran, Kapil Gadkar, Crystal Zhang, Sunil Bhakta in Pharmaceutical Research (2015)

  5. No Access

    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...

    Ben-Quan Shen, Keyang Xu, Luna Liu, Helga Raab, Sunil Bhakta in Nature Biotechnology (2012)

  6. No Access

    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...

    Darlene E. Jenkins, Shang-Fan Yu, Yvette S. Hornig in Clinical & Experimental Metastasis (2003)

  7. No Access

    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...

    Darlene E. Jenkins, Yoko Oei, Yvette S. Hornig in Clinical & Experimental Metastasis (2003)