Figure 1
From: PIK3CA mutations in breast cancer: reconciling findings from preclinical and clinical data
Schema of phosphoinositide 3-kinase blocking agents currently under clinical development. Dual phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors (for example, BEZ235, XL765, GDC-0980, GSK1059615), pan-PI3K inhibitors (BKM120, GDC-0941, BAY 80–6946, SF1126, PX-866, XL147, CH5132799, GSK1059615), isoform-selective PI3K inhibitors (p110α selective: BYL719, MLN1117; p110β selective: TGX-221, GSK2636771; p110γ selective: AS-252424; p110δ selective: CAL-101), AKT inhibitors (MK-2206, XL418, GDC-0068, AR-67, GSK690693, VQD-002), mTORC1/2 inhibitors (OSI-027, AZD-8055, PP-242, INK-128), and PDK1 inhibitors (AR-12, UCN-01). PIP2, phosphatidylinositol-4,5-bisphosphate; PIP3, phosphatidylinositol-4,5-trisphosphate; RTK, receptor tyrosine kinase.