Review Volume 7, Issue 12 pp 1032—1049

Figure 4. Actions of therapeutics targeting PTEN deficiency in lymphoid malignancies.

PTEN deficiency is associated with increased sensitivity to PI3K, AKT, and mTOR inhibitors. In addition, because PI3K is involved in BCR signaling activation, BCR pathway inhibitors may also be effective in PTEN-deficient lymphoid malignancies. SRC family kinase inhibitors include dasatinib (which can also inhibit BTK), saracatinib, bosutinib, SU6656, CGP76030, and KX-01. BTK inhibitors include ibrutinib and AVL-292. Sotrastaurin is a PKCβ inhibitor; A20, a MALT1 paracaspase inhibitor; and MLN120B, an IKKβ inhibitor. SYK inhibitors include fostamatinib and PRT062607. Idelalisib is a PI3Kδ-specific inhibitor. MK-2206 is an AKT inhibitor. mTOR inhibitors include everolimus and temsirolimus.