Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.

Abstract

Great successes have been achieved in developing small-molecule kinase inhibitors as anticancer therapeutic agents. However, kinase deregulation plays essential roles not only in cancer but also in almost all major disease areas. Accumulating evidence has revealed that kinases are promising drug targets for different diseases, including cancer, autoimmune diseases, inflammatory diseases, cardiovascular diseases, central nervous system disorders, viral infections, and malaria. Indeed, the first small-molecule kinase inhibitor for treatment of a nononcologic disease was approved in 2011 by the U.S. FDA. To date, 10 such inhibitors have been approved, and more are in clinical trials for applications other than cancer. This Perspective discusses a number of kinases and their small-molecule inhibitors for the treatment of diseases in nononcologic therapeutic fields. The opportunities and challenges in developing such inhibitors are also highlighted.

• Authors: Zhouling Xie, Xiaoxiao Yang, Yajun Duan, Jihong Han, Chenzhong Liao
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 64 Issue 3 Pg. 1283-1345 (02 11 2021) ISSN: 1520-4804 [Electronic] United States
• PMID: 33481605 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Protein Kinase Inhibitors
• Small Molecule Libraries

Topics

• Animals
• Autoimmune Diseases (drug therapy)
• Drug Discovery
• Humans
• Models, Molecular
• Protein Kinase Inhibitors (chemical synthesis, pharmacology)
• Small Molecule Libraries