A unique binding pocket induced by a noncanonical SAH mimic to develop potent and selective PRMT inhibitors

• Main Authors: Youchao Deng (Author), Xiaosheng Song (Author), Iredia D. Iyamu (Author), Aiping Dong (Author), Jinrong Min (Author), Rong Huang (Author)
• Format: Book
• Published: Elsevier, 2023-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Protein arginine methyltransferases (PRMTs) are attractive targets for developing therapeutic agents, but selective PRMT inhibitors targeting the cofactor SAM binding site are limited. Herein, we report the discovery of a noncanonical but less polar SAH surrogate YD1113 by replacing the benzyl guani...