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

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 16 , Issue 13 , 2016

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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.

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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Article Details

VOLUME: 16
ISSUE: 13
Year: 2016
Page: [1413 - 1426]
Pages: 14
DOI: 10.2174/1568026615666150915115823
Price: $58

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