title: 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.affiliation: Nimbus Discovery , 25 First Street, Suite 404, Cambridge, Massachusetts 02141, United States.
authors.forename: Divya
authors.initials: D
authors.lastname: Chaudhary
authors.forename: Shaughnessy
authors.initials: S
authors.lastname: Robinson
authors.forename: Donna L
authors.initials: DL
authors.lastname: Romero
mesh_terms: D055808:Drug Discovery / Q000379:methods / Q000639:trends; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D053592:Interleukin-1 Receptor-Associated Kinases / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D017434:Protein Structure, Tertiary; D015398:Signal Transduction / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D047428:Protein Kinase Inhibitors; D054852:Small Molecule Libraries; C507773:IRAK4 protein, human; D053592:Interleukin-1 Receptor-Associated Kinases