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Small Molecule Inhibitors Against Cancer-Associated Protein
University of Florida
Small molecule
Oncology
Hit To Lead or Lead Optimization
• Inhibitors against protein arginine methyltransferase 5 plays a role in tumor development and is overexpressed in several cancers, including lymphoma, glioblastoma, colorectal cancer, and prostate cancer.
• Inhibiting protein arginine methyltransferase 5 may be an effective treatment for inflammation and auto-immune disorders. Previously reported small molecule inhibitors of this protein have low potency or lack in vivo activity, limiting clinical applications.
• Researchers at the University of Florida have developed competitive compounds that inhibit protein arginine methyltransferase 5 activity in cellular processes.
• These small molecules have a 25-fold greater binding affinity and 40- fold greater efficacy than previous inhibitors of protein arginine methyltransferase 5.
• These small molecules are effective in vivo and have a high potency, making them strong therapeutic candidates for the treatments of cancer and autoimmune disorders.
US20220185792A1
Cryo-EM structure-based selection of computed ligand poses enables design of MTA-synergic PRMT5 inhibitors of better potency.
Communications Biology, (2022)
