The search is on for effective specific inhibitors for PI3Kα mutants. PI3Kα, a critical lipid
kinase, has two subunits, catalytic and inhibitory. PIK3CA, the gene that encodes the p110α …

Phosphatidylinositol 3-kinases (PI3Ks) are important therapeutic targets for the treatment of
cancer, thrombosis, and inflammatory and immune diseases. The four highly homologous …

Impressive responses have been observed in patients treated with checkpoint inhibitory anti–
programmed cell death-1 (PD-1) or anti–cytotoxic T-lymphocyte-associated antigen-4 (CTLA …

A high incidence of cancer has given rise to the development of more anti-tumor drugs. From
2015 to 2020, fifty-six new small-molecule anticancer drugs, divided into ten categories …

A (series) range of potential dimorpholinoquinazoline-based inhibitors of the PI3K/Akt/mTOR
cascade was synthesized. Several compounds exhibited cytotoxicity towards a panel of …

Abstract The PI3K/AKT/mTOR signaling pathway is well known to be involved in cell growth,
proliferation, metabolism and other cellular physiological processes. Abnormal activation of …

The growing smooth talk in the field of natural compounds is due to the ancient and current
interest in herbal medicine and their potentially positive effects on health. Dozens of …

Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic
domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform …

The phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases central to regulating a
wide range of important intracellular processes. Despite the vast knowledge around class I …

A series of amino-substituted triazines were developed and examined for PI3Kβ inhibition
and anti-platelet function. Structural adaptations of a morpholine ring of the prototype pan …