uncialamycin and Lung-Neoplasms

uncialamycin has been researched along with Lung-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for uncialamycin and Lung-Neoplasms

ArticleYear
Uncialamycin as a novel payload for antibody drug conjugate (ADC) based targeted cancer therapy.
    Bioorganic & medicinal chemistry letters, 2019, 02-01, Volume: 29, Issue:3

    Uncialamycin analogs were evaluated as potential cytotoxic agents in an antibody-drug conjugate (ADC) approach to treating human cancer. These analogs were synthesized using Hauser annulations of substituted phthalides as a key step. A highly potent uncialamycin analog 3c with a valine-citrulline dipeptide linker was conjugated to an anti-mesothelin monoclonal antibody (mAb) through lysines to generate a meso-13 conjugate. This conjugate demonstrated subnanomolar potency (IC50 = 0.88 nM, H226 cell line) in in vitro cytotoxicity experiments with good immunological specificity to mesothelin-positive lung cancer cell lines. The potency and mechanism of action of this uncialamycin class of enediyne antitumor antibiotics make them attractive payloads in ADC-based cancer therapy.

    Topics: Anthraquinones; Antibodies, Monoclonal; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Immunoconjugates; Lung Neoplasms; Models, Molecular; Molecular Structure; Structure-Activity Relationship

2019