Class II Phosphoinositide 3-Kinases as Novel Drug Targets
(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
- Falasca, Marco ; Hamilton, Justin R ; Selvadurai, Maria ; Sundaram, Krithika ; Adamska, Aleksandra LU and Thompson, Philip E
- publishing date
- 2017-01-12
- 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}}, }