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

[ Vol. 16 , Issue. 13 ]

Author(s):

Dima A. Sabbah, Jian Hu and Haizhen A. Zhong   Pages 1413 - 1426 ( 14 )

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.

Affiliation:

DSC 362, Department of Chemistry, The University of Nebraska at Omaha, 6001 Dodge Street, Omaha, Nebraska 68182 U.S.A

Graphical Abstract:



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