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J Med Chem. 2015 Jan 8;58(1):96-110. doi: 10.1021/jm5016044. Epub 2014 Dec 5.
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.
IRAK4 是一种丝氨酸/苏氨酸激酶,在炎症和肿瘤疾病中都起着关键作用。在此,我们总结了 IRAK4 信号节点在疾病中的强大生物学特性,回顾了 IRAK4 的关键结构特征,包括选择性挑战,并描述了发现临床可行的 IRAK4 抑制剂的努力。最后,提供了对已获得知识和尚存挑战的看法。