PI3K in cancer: divergent roles of isoforms, modes of activation, and therapeutic targeting

By Lauren M Thorpe, Haluk Yuzugullu, Jean J. Zhao. Nature Reviews. Cancer, 2014

1,246 citations recorded by the source corpus.

Phosphatidylinositol 3-kinases (PI3Ks) are crucial coordinators of intracellular signalling in response to extracellular stimuli. Hyperactivation of PI3K signalling cascades is one of the most common events in human cancers. In this Review, we discuss recent advances in our knowledge of the roles of specific PI3K isoforms in normal and oncogenic signalling, the different ways in which PI3K can be upregulated, and the current state and future potential of targeting this pathway in the clinic.

Subfields: Genetics, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/50cf2e78125aab1633f065079edc6575666f2078

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In Genetics

1. Ping Wee
2. Carlos L. Arteaga
3. Zhixiang Wang
4. R. Abraham
5. D. Fruman

In Molecular Biology

1. Ping Wee
2. Zhixiang Wang
3. D. Fruman
4. Carlos L. Arteaga
5. B. Hopkins
6. Ingrid A. Mayer
7. R. Abraham
8. Honyin Chiu

Citations in the corpus

• LncRNA-mediated regulation of cell signaling in cancer (2017, background): “LncRNAs as AKT regulators Overwhelming evidence supports the role of AKT in cancer (Thorpe et al 2015).”
• The PI3K/AKT Pathway as a Target for Cancer Treatment. (2016, background): “PIK3CB and PIK3CD, unlike PIK3CA, are amplified or overexpressed but not mutated in human neoplasias (6).”
• Proliferation, survival and metabolism: the role of PI3K/AKT/mTOR signalling in pluripotency and cell fate determination (2016, background): “1), which stimulates the conversion of membrane-bound phosphatidylinositol-(4,5)bisphosphate [PtdIns(4,5)P2; PIP2] to phosphatidylinositol-(3,4,5)trisphosphate [PtdIns(3,4,5)P3; PIP3] (Vanhaesebroeck et al., 2010; Thorpe et al., 2015).”
• Epidermal Growth Factor Receptor Cell Proliferation Signaling Pathways (2017, background): “There are three classes of PI3K, Class I, II, and III, which defer in structure, regulation, and function [226].”
• The PI3K pathway in human disease (2017, positive): “Pharmacological inhibition of the PI3K pathway in cancer cell lines in culture is frequently followed, within hours to days, by the induction of adaptive (non-genetic) resistance mechanisms (Thorpe et al., 2015) (Figure 6).”