Class IA PI3Ks (phosphoinositide 3-kinases) regulate a wide range of cellular responses through the production of PI(3,4,5)P3 (phosphatidylinositol 3,4,5-trisphosphate) in cellular membranes. They are activated by receptor tyrosine kinases, by Ras and Rho family GTPases, and in some cases by Gβγ subunits from trimeric G-proteins. Crystallographic studies on the related class IB PI3Kγ, and biochemical and structural studies on the class IA PI3Ks, have led to new insights into how these critical enzymes are regulated in normal cells and how mutations can lead to their constitutive activation in transformed cells. The present paper will discuss recent studies on the regulation of class I (p85/p110) PI3Ks, with a focus on the role of SH2 domains (Src homology 2 domains) in the p85 regulatory subunit in modulating PI3K activity.
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April 2007
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Conference Article|
March 20 2007
Regulation of class IA PI3Ks
H. Wu;
H. Wu
1Department of Molecular Pharmacology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, U.S.A.
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Y. Yan;
Y. Yan
1Department of Molecular Pharmacology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, U.S.A.
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J.M. Backer
J.M. Backer
1
1Department of Molecular Pharmacology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, U.S.A.
1To whom correspondence should be addressed (email Backer@aecom.yu.edu).
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Publisher: Portland Press Ltd
Received:
October 23 2006
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2007 The Biochemical Society
2007
Biochem Soc Trans (2007) 35 (2): 242–244.
Article history
Received:
October 23 2006
Citation
H. Wu, Y. Yan, J.M. Backer; Regulation of class IA PI3Ks. Biochem Soc Trans 1 April 2007; 35 (2): 242–244. doi: https://doi.org/10.1042/BST0350242
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