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Class II Phosphoinositide 3-Kinases as Novel Drug Targets

Falasca, Marco ; Hamilton, Justin R ; Selvadurai, Maria ; Sundaram, Krithika ; Adamska, Aleksandra LU and Thompson, Philip E (2017) In Journal of Medicinal Chemistry 60(1). p.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.... (More)

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.

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author
; ; ; ; and
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Animals, Disease, Enzyme Inhibitors/pharmacology, Humans, Phosphoinositide-3 Kinase Inhibitors
in
Journal of Medicinal Chemistry
volume
60
issue
1
pages
19 pages
publisher
The American Chemical Society (ACS)
external identifiers
  • scopus:85018523970
  • pmid:27644332
ISSN
1520-4804
DOI
10.1021/acs.jmedchem.6b00963
language
English
LU publication?
no
id
ddfefecf-0f2b-4541-8162-bc43025c2485
date added to LUP
2023-05-22 10:08:55
date last changed
2024-04-05 18:03:19
@article{ddfefecf-0f2b-4541-8162-bc43025c2485,
  abstract     = {{<p>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.</p>}},
  author       = {{Falasca, Marco and Hamilton, Justin R and Selvadurai, Maria and Sundaram, Krithika and Adamska, Aleksandra and Thompson, Philip E}},
  issn         = {{1520-4804}},
  keywords     = {{Animals; Disease; Enzyme Inhibitors/pharmacology; Humans; Phosphoinositide-3 Kinase Inhibitors}},
  language     = {{eng}},
  month        = {{01}},
  number       = {{1}},
  pages        = {{47--65}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{Journal of Medicinal Chemistry}},
  title        = {{Class II Phosphoinositide 3-Kinases as Novel Drug Targets}},
  url          = {{http://dx.doi.org/10.1021/acs.jmedchem.6b00963}},
  doi          = {{10.1021/acs.jmedchem.6b00963}},
  volume       = {{60}},
  year         = {{2017}},
}