Advances in the development of class I phosphoinositide 3-kinase (PI3K) inhibitors

Dima A. Sabbah; Jian Hu; Haizhen A. Zhong

doi:10.2174/1568026615666150915115823

Advances in the development of class I phosphoinositide 3-kinase (PI3K) inhibitors

Dima A. Sabbah, Jian Hu, Haizhen A. Zhong

Research output: Contribution to journal › Review article › peer-review

26 Scopus citations

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.

Original language	English (US)
Pages (from-to)	1413-1426
Number of pages	14
Journal	Current Topics in Medicinal Chemistry
Volume	16
Issue number	13
DOIs	https://doi.org/10.2174/1568026615666150915115823
State	Published - May 1 2016

Keywords

Anticancer
BRAF
Class I PI3Ks
Drug design
EGFR
GDC-0941
GSK2118436
KRAS
LY294002
MEK
Mutation
NVP-BEZ235
P100α
PI3K/AKT
PI3Kγ
Selectivity
mTOR

ASJC Scopus subject areas

Drug Discovery

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10.2174/1568026615666150915115823

Cite this

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title = "Advances in the development of class I phosphoinositide 3-kinase (PI3K) inhibitors",

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 = "Anticancer, BRAF, Class I PI3Ks, Drug design, EGFR, GDC-0941, GSK2118436, KRAS, LY294002, MEK, Mutation, NVP-BEZ235, P100α, PI3K/AKT, PI3Kγ, Selectivity, mTOR",

author = "Sabbah, {Dima A.} and Jian Hu and Zhong, {Haizhen A.}",

note = "Funding Information: HAZ would like to thank the financial support from the Faculty Development Fellowship from the University of Nebraska at Omaha (2014-2015) Publisher Copyright: {\textcopyright} 2016 Bentham Science Publishers.",

year = "2016",

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doi = "10.2174/1568026615666150915115823",

language = "English (US)",

volume = "16",

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AU - Sabbah, Dima A.

AU - Hu, Jian

AU - Zhong, Haizhen A.

N1 - Funding Information: HAZ would like to thank the financial support from the Faculty Development Fellowship from the University of Nebraska at Omaha (2014-2015) Publisher Copyright: © 2016 Bentham Science Publishers.

PY - 2016/5/1

Y1 - 2016/5/1

N2 - 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.

AB - 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.

KW - Anticancer

KW - BRAF

KW - Class I PI3Ks

KW - Drug design

KW - EGFR

KW - GDC-0941

KW - GSK2118436

KW - KRAS

KW - LY294002

KW - MEK

KW - Mutation

KW - NVP-BEZ235

KW - P100α

KW - PI3K/AKT

KW - PI3Kγ

KW - Selectivity

KW - mTOR

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Advances in the development of class I phosphoinositide 3-kinase (PI3K) inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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