作者: Chung-Pu Wu , Megumi Murakami , Sung-Han Hsiao , An-Wei Chou , Yan-Qing Li
DOI: 10.1021/ACS.MOLPHARMACEUT.7B00277
关键词: RPTOR 、 Kinase activity 、 Cancer cell 、 PI3K/AKT/mTOR pathway 、 Biology 、 Cell biology 、 Protein kinase B 、 Abcg2 、 ATP-binding cassette transporter 、 Cancer
摘要: Deregulated activation of phosphoinositide 3-kinase (PI3K)/Akt/mammalian target rapamycin (mTOR) pathway is frequently found in human cancers, which plays a key role promoting cancer proliferation and resistance to anticancer therapies. Therefore, developing inhibitors targeting components the PI3K/Akt/mTOR signaling has great clinical significance. PF-4989216 novel, orally available small-molecule drug that was developed selectively inhibit subsequent cell proliferation. exhibited potent selective inhibition against PI3K kinase activity preclinical small-cell lung (SCLC) models, especially effective SCLCs harboring PIK3CA mutation. Unfortunately, addition innate mechanisms, extrusion by efflux pumps may also contribute development acquired cells. The overexpression ATP-binding cassette (ABC)...