LKB1 (AAK1 dual inhibitor)

LKB1是一种选择性的 Pim-1激酶抑制剂，Kd值为35 nM[1]。

PIM-1（原癌基因丝氨酸/苏氨酸-蛋白激酶）是由PIM1基因编码的酶，在多种人类癌症中具有重要作用。据报道，pim-1在脾脏、胸腺、骨髓、前列腺和口腔上皮细胞等部位表达。Pim-1在多个分离的人类肿瘤细胞中高表达，并参与细胞周期进程、细胞凋亡、转录激活和许多基本的信号转导途径。因此，抑制pim-1的低分子量化合物可用于抗癌治疗，需要得到更多的关注和发展[2，3]。

参考文献：
1.  Bamborough, P., et al., Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem, 2008. 51(24): p. 7898-914.
2.  Natarajan, K., et al., The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms. Biochem Pharmacol, 2013. 85(4): p. 514-24.
3.  Tsuganezawa, K., et al., A novel Pim-1 kinase inhibitor targeting residues that bind the substrate peptide. J Mol Biol, 2012. 417(3): p. 240-52.