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.
Current Topics in Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/1568026615666150915115823 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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