Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.

Abstract

IRAK4, a serine/threonine kinase, plays a key role in both inflammation and oncology diseases. Herein, we summarize the compelling biology surrounding the IRAK4 signaling node in disease, review key structural features of IRAK4 including selectivity challenges, and describe efforts to discover clinically viable IRAK4 inhibitors. Finally, a view of knowledge gained and remaining challenges is provided.

• Authors: Divya Chaudhary, Shaughnessy Robinson, Donna L Romero
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 58 Issue 1 Pg. 96-110 (Jan 08 2015) ISSN: 1520-4804 [Electronic] United States
• PMID: 25479567 (Publication Type: Journal Article, Review)

Chemical References

• Protein Kinase Inhibitors
• Small Molecule Libraries
• IRAK4 protein, human
• Interleukin-1 Receptor-Associated Kinases

Topics

• Drug Discovery (methods, trends)
• Humans
• Inflammation (drug therapy)
• Interleukin-1 Receptor-Associated Kinases (antagonists & inhibitors, chemistry, metabolism)
• Molecular Structure
• Neoplasms (drug therapy)
• Protein Kinase Inhibitors (chemistry, metabolism, pharmacology)
• Protein Structure, Tertiary
• Signal Transduction (drug effects)
• Small Molecule Libraries (chemistry, metabolism, pharmacology)