The PI3K signaling cascade is the key moderator of cell proliferation, survival, motility,
and apoptosis. Class I PI3K proteins are well characterized and linked to thrombosis (PI3Kβ), rheumatoid
arthritis (PI3Kδ), and cancer (PI3Kα). In this review, we explore the latest progress in the design
and development of selective Class I PI3K inhibitors from the perspective of drug design and structure activity relationships.
Keywords: Class I PI3Ks, p100α, Anticancer, Drug design, Mutation, LY294002, GDC-0941, NVP-BEZ235, PI3Kγ, KRAS,
BRAF, EGFR, MEK, PI3K/AKT, GSK2118436, Selectivity, and mTOR.
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