Only 15% of human kinases carry a bulky residue at the DFG-1 position, providing an opportunity for the design of selective ATP-site inhibitors without the typical hinge-binding interactions. The low sequence homology among unrelated kinases with bulky DFG-1 residues provides a new paradigm for selective kinase inhibitor development.

中文翻译：

---

DFG-1结合：开发选择性激酶抑制剂的新残基。

只有15％的人类激酶在DFG-1位置带有一个庞大的残基，这为设计具有典型的铰链结合作用的选择性ATP站点抑制剂提供了机会。具有大量DFG-1残基的无关激酶之间的低序列同源性为选择性激酶抑制剂的开发提供了新的范例。