XL-388

XL-388是一种药物，可用作哺乳动物雷帕霉素靶蛋白（mTOR）mTORC1和mTORC2两种亚型机制性靶标的潜在选择性抑制剂。Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N. Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). J Med Chem. 2013 Mar 28;56(6):2218-34.  它目前处于各类癌症治疗的研究中，Zhu YR, Zhou XZ, Zhu LQ, Yao C, Fang JF, Zhou F, Deng XW, Zhang YQ. The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models. Oncotarget. 2016 Aug 2;7(31):49527-49538.  Xiong Z, Zang Y, Zhong S, Zou L, Wu Y, Liu S, Fang Z, Shen Z, Ding Q, Chen S. The preclinical assessment of XL388, a mTOR kinase inhibitor, as a promising anti-renal cell carcinoma agent. Oncotarget. 2017 May 2;8(18):30151-30161.  Zhong S, Xue J, Cao JJ, Sun B, Sun QF, Bian LG, Hu LY, Pan SJ. The therapeutic value of XL388 in human glioma cells. Aging (Albany NY). 2020 Nov 6;12(22):22550-22563.  并且mTOR抑制剂还被证明可用于神经性疼痛的治疗。Choi S, Kim K, Cha M, Kim M, Lee BH. mTOR signaling intervention by Torin1 and XL388 in the insular cortex alleviates neuropathic pain. Neurosci Lett. 2020 Jan 23;718:134742.  Cha M, Choi S, Kim K, Lee BH. Manganese-enhanced MRI depicts a reduction in brain responses to nociception upon mTOR inhibition in chronic pain rats. Mol Brain. 2020 Nov 23;13(1):158.  

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Category:酶抑制剂
Category:氨基吡啶
Category:酰胺
Category:氟苯衍生物
Category:苯基砜