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

Research output: Contribution to journalEditorialResearchpeer-review

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 languageEnglish
Pages (from-to)3 - 6
Number of pages4
JournalA C S Medicinal Chemistry Letters
Volume6
Issue number1
DOIs
Publication statusPublished - 2015

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.",
author = "Mountford, {Simon John} and Zhaohua Zheng and Krithika Sundaram and Ian Jennings and Hamilton, {Justin Raymond} and Philip Thompson",
year = "2015",
doi = "10.1021/ml500354e",
language = "English",
volume = "6",
pages = "3 -- 6",
journal = "A C S Medicinal Chemistry Letters",
issn = "1948-5875",
publisher = "ACS Publications",
number = "1",

}

Class II but not second class - prospects for the development of class II PI3K inhibitors. / Mountford, Simon John; Zheng, Zhaohua; Sundaram, Krithika; Jennings, Ian; Hamilton, Justin Raymond; Thompson, Philip.

In: A C S Medicinal Chemistry Letters, Vol. 6, No. 1, 2015, p. 3 - 6.

Research output: Contribution to journalEditorialResearchpeer-review

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T1 - Class II but not second class - prospects for the development of class II PI3K inhibitors

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

U2 - 10.1021/ml500354e

DO - 10.1021/ml500354e

M3 - Editorial

VL - 6

SP - 3

EP - 6

JO - A C S Medicinal Chemistry Letters

JF - A C S Medicinal Chemistry Letters

SN - 1948-5875

IS - 1

ER -