Class II Phosphoinositide 3-Kinases as Novel Drug Targets
- 21 October 2016
- journal article
- review article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 60 (1) , 47-65
Abstract
The phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases central to regulating a wide range of important intracellular processes. Despite the vast knowledge around class I PI3Ks, the class II PI3Ks have been neglected, seemingly only due to the chronology of their discovery. Here we focus on the cellular functions of the three class II PI3K isoforms, PI3KC2α, PI3KC2β, and PI3KC2γ, in different cell systems and underline the emerging importance of these enzymes in different physiological and pathological contexts. We provide an overview on the current development of class II PI3 kinase inhibitors and outline the potential use for such inhibitors. The field is in its infancy as compared to their class I counterparts. Nevertheless, recent advances in understanding the roles of class II PI3 kinases in different pathological contexts is leading to an increased interest in the development of specific inhibitors that can provide potential novel pharmacological tools.Keywords
This publication has 151 references indexed in Scilit:
- Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysisBiochemical Journal, 2012
- Intersectin 1 is required for neuroblastoma tumorigenesisOncogene, 2012
- Somatic deletions of genes regulating MSH2 protein stability cause DNA mismatch repair deficiency and drug resistance in human leukemia cellsNature Medicine, 2011
- Integrative Genomic Profiling of Human Prostate CancerCancer Cell, 2010
- Targeting the PI3K signaling pathway in cancerCurrent Opinion in Genetics & Development, 2010
- The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitorsNature Chemical Biology, 2010
- A survey of glioblastoma genomic amplifications and deletionsJournal of Neuro-Oncology, 2009
- PI3K pathway alterations in cancer: variations on a themeOncogene, 2008
- Genetic profiling of chromosome 1 in breast cancer: mapping of regions of gains and losses and identification of candidate genes on 1qBritish Journal of Cancer, 2006
- A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin SignalingCell, 2006