Targeting PI3K in cancer: mechanisms and advances in clinical trials
By Jing Yang, Ji Nie, Xuelei Ma, Yuquan Wei, Yong Peng, Xiawei Wei. Molecular Cancer, 2019
1,281 citations recorded by the source corpus.
Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling is one of the most important intracellular pathways, which can be considered as a master regulator for cancer. Enormous efforts have been dedicated to the development of drugs targeting PI3K signaling, many of which are currently employed in clinical trials evaluation, and it is becoming increasingly clear that PI3K inhibitors are effective in inhibiting tumor progression. PI3K inhibitors are subdivided into dual PI3K/mTOR inhibitors, pan-PI3K inhibitors and isoform-specific inhibitors. In this review, we performed a critical review to summarize the role of the PI3K pathway in tumor development, recent PI3K inhibitors development based on clinical trials, and the mechanisms of resistance to PI3K inhibition.
Subfields: Genetics, Molecular Biology, Pathology and Forensic Medicine
View Paper: https://www.semanticscholar.org/paper/a6d524ce524ae91108f4bd81b6b6fbae6c663252
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In Genetics
In Molecular Biology
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- Kenneth Atz
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- Rajiv K. Tonk
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- Vivek Panwar
- Manini Bhatt
- Shinjinee Sengupta
Citations in the corpus
- Multifaceted role of mTOR (mammalian target of rapamycin) signaling pathway in human health and disease (2023, background): “295 Mutations increase the catalytic activity of mTORC1/2 and thereby reduce the effectiveness of such compounds towards rapalogs, dual inhibitors as well as TOR-KI.”
- PI3K/AKT/mTOR signaling transduction pathway and targeted therapies in cancer (2023, background): “Indeed, PIK3CA is usually either mutated or amplified in several human cancers [55], including colorectal cancer (CRC) [56], breast [57], lung [58], gastric [59], prostate [60], and cervical cancer [61, 62].”
- Leveraging molecular structure and bioactivity with chemical language models for de novo drug design (2023, methodology): “The protein target PI3K γ 26 was selected on the basis of the data available in the DTC 35 database.”