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Showing 1–4 of 4 results
Advanced filters: Author: Shang-Fan Yu Clear advanced filters

  • Antibody drug conjugates (ADCs) with pyrrolobenzodiazepine (PBD) payloads are promising cancer therapeutics but are limited by toxicity. Here, the authors develop a HER2-targeted ADC (DHES0815A) with a reduced potency PBD payload that demonstrated promising preclinical efficacy and nonhuman primate tolerability, but culminated in a phase I clinical trial in patients with metastatic breast cancer which was terminated due to toxicity.

    • Gail D. Lewis
    • Guangmin Li
    • Eunpi Cho
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-15

  • Many drugs contain tertiary and heteroaryl amines; however, these functional groups are difficult to reversibly crosslink to a carrier protein. Now, a method for conjugating anticancer and antibiotic drugs to antibodies via a quaternary ammonium salt has been developed. Cleavage of the linker results in the traceless release of the free drug and subsequent therapeutic activity.

    • Leanna R. Staben
    • Stefan G. Koenig
    • Thomas H. Pillow
    Research
    Nature Chemistry
    Volume: 8, P: 1112-1119

  • SMARCA2 has been identified as a synthetic lethal target in SMARCA4 mutated tumors, however, homology between the two has hindered the development of selective SMARCA2 inhibitors. Here, the authors synthesize a proteolysis targeting chimera (PROTAC) capable of SMARCA2 specific degradation and demonstrate its utility in the treatment of SMARCA4 mutated tumors.

    • Jennifer Cantley
    • Xiaofen Ye
    • Robert L. Yauch
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-14