Small Molecule Inhibitors Against Cancer-Associated Protein

Demonstrate a High Potency In Vivo, Making Them Strong Therapeutic Candidates for Cancer and Autoimmune Disorders

These small molecules are inhibitors against protein arginine methyltransferase 5, which plays a role in tumor development and is overexpressed in several cancers, including lymphoma, glioblastoma, colorectal cancer, and prostate cancer. The global treatment market for these specific cancers should reach $58 billion by 2024. Additionally, 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 are effective in vivo and have a high potency, making them strong therapeutic candidates for the treatments of cancer and autoimmune disorders.

Application(s)

Competitive inhibitor compounds that block the activity of a cancer-associated protein and may be effective therapeutics against certain cancers, inflammation, and autoimmune disorders

Advantages

• Can be incorporated in pharmaceutically acceptable salts, solvates, hydrates, or drugs, facilitating the development of new therapeutics
• Active in vivo, making clinical applications feasible
• Have high binding affinity and efficacy, resulting in a higher potency than other inhibitors

Technology

This family of indole-based small molecules prevents S-adensylmethionine from binding to protein arginine methyltransferase 5, inhibiting the protein from participating in cellular processes associated with various cancers and autoimmune diseases. These small molecules have a 25-fold greater binding affinity and 40-fold greater efficacy than previous inhibitors of protien arginine methyltransferase 5.