Class II but not second class - prospects for the development of class II PI3K inhibitors

Simon John Mountford; Zhaohua Zheng; Krithika Sundaram; Ian Jennings; Justin Raymond Hamilton; Philip Thompson

doi:10.1021/ml500354e

Class II but not second class - prospects for the development of class II PI3K inhibitors

Simon John Mountford, Zhaohua Zheng, Krithika Sundaram, Ian Jennings, Justin Raymond Hamilton, Philip Thompson

Research output: Contribution to journal › Editorial › Research › peer-review

10 Citations (Scopus)

Abstract

The Class II PI3 kinases are emerging from the shadows of their Class I cousins. The data emerging from PIK3C2 genetic modification studies and from siRNA knockdown suggest important roles in physiology and pathology. With some well-studied Class I isoform inhibitors showing strong Class II activity and a wealth of crystallographic information available, the structural similarity of these isoforms to Class I provides both the opportunity and the challenge in design of selective pharmacological inhibitors.

Original language	English
Pages (from-to)	3 - 6
Number of pages	4
Journal	ACS Medicinal Chemistry Letters
Volume	6
Issue number	1
DOIs	https://doi.org/10.1021/ml500354e
Publication status	Published - 2015

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10.1021/ml500354e

Cite this

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title = "Class II but not second class - prospects for the development of class II PI3K inhibitors",

abstract = "The Class II PI3 kinases are emerging from the shadows of their Class I cousins. The data emerging from PIK3C2 genetic modification studies and from siRNA knockdown suggest important roles in physiology and pathology. With some well-studied Class I isoform inhibitors showing strong Class II activity and a wealth of crystallographic information available, the structural similarity of these isoforms to Class I provides both the opportunity and the challenge in design of selective pharmacological inhibitors.",

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AU - Mountford, Simon John

AU - Zheng, Zhaohua

AU - Sundaram, Krithika

AU - Jennings, Ian

AU - Hamilton, Justin Raymond

AU - Thompson, Philip

PY - 2015

Y1 - 2015

N2 - The Class II PI3 kinases are emerging from the shadows of their Class I cousins. The data emerging from PIK3C2 genetic modification studies and from siRNA knockdown suggest important roles in physiology and pathology. With some well-studied Class I isoform inhibitors showing strong Class II activity and a wealth of crystallographic information available, the structural similarity of these isoforms to Class I provides both the opportunity and the challenge in design of selective pharmacological inhibitors.

AB - The Class II PI3 kinases are emerging from the shadows of their Class I cousins. The data emerging from PIK3C2 genetic modification studies and from siRNA knockdown suggest important roles in physiology and pathology. With some well-studied Class I isoform inhibitors showing strong Class II activity and a wealth of crystallographic information available, the structural similarity of these isoforms to Class I provides both the opportunity and the challenge in design of selective pharmacological inhibitors.

UR - http://pubs.acs.org/doi/pdf/10.1021/ml500354e

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DO - 10.1021/ml500354e

M3 - Editorial

SN - 1948-5875

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SP - 3

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JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 1

ER -

Class II but not second class - prospects for the development of class II PI3K inhibitors

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Examining novel cell signalling in the regulation of platelet structure and function

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Class II but not second class - prospects for the development of class II PI3K inhibitors

Abstract

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Examining novel cell signalling in the regulation of platelet structure and function

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