Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors

Title:Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors

Volume: 16 Issue: 13

Author(s): Dima A. Sabbah, Jian Hu and Haizhen A. Zhong

Affiliation:

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.

Abstract: 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.

Cite this article as:

Sabbah A. Dima, Hu Jian and Zhong A. Haizhen, Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors , Current Topics in Medicinal Chemistry 2016; 16 (13) . https://dx.doi.org/10.2174/1568026615666150915115823