Discovery of first-in-class DOT1L inhibitors against the R231Q gain-of-function mutation in the catalytic domain with therapeutic potential of lung cancer

• Main Authors: Zehui Tan (Author), Ning Guo (Author), Zhi Cao (Author), Shuyu Liu (Author), Jiayu Zhang (Author), Deyi Ma (Author), Jiahao Zhang (Author), Wencai Lv (Author), Nan Jiang (Author), Linghe Zang (Author), Lihui Wang (Author), Xin Zhai (Author)
• Format: Book
• Published: Elsevier, 2024-08-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Recent research certified that DOT1L and its mutations represented by R231Q were potential targets for the treatment of lung cancer. Herein, a series of adenosine-containing derivatives were identified with DOT1LR231Q inhibition through antiproliferation assay and Western blot analysis in the H460R2...