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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

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

Volume 16 , Issue 13 , 2016

Page: [1413 - 1426] Pages: 14

DOI: 10.2174/1568026615666150915115823

Price: $65


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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