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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.

SUBMITTER: Mountford SJ

PROVIDER: S-EPMC4291705 | biostudies-literature | 2015 Jan

REPOSITORIES: biostudies-literature

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Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.

Mountford Simon J SJ Zheng Zhaohua Z Sundaram Krithika K Jennings Ian G IG Hamilton Justin R JR Thompson Philip E PE

ACS medicinal chemistry letters 20140924 1

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 i ...[more]

PMID: 25589915

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