Potent phosphatidylinositol 3-kinase inhibitors and their biology
Mukesh Chandra Joshi, Krishan Kumar, Vikrant Kumar1
1Department of Chemistry, Motilal Nehru College, University of Delhi, Delhi-110021, India. mukeshjoshi21@gmail.com.
Abstract:
The Phosphoinositide 3-kinase (PI3k) is an important regulator of intracellular signalling pathways, like cell proliferation, migration, survival, and angiogenesis upon activation by growth factor or receptors. The PI3k's pathway is frequently up-regulated in human cancers, thus inhibition of PI3k's is a promising approach for cancer therapy. Many potent PI3k's inhibitors have been reported so far and few of them are in clinical trial like GDC-0941, BGT-226, AZD-6482 and others are natural products etc.
Insights
Phosphoinositide 3-kinase (PI3k) regulates cell functions and is often overactive in cancers. Inhibiting this pathway offers a promising cancer therapy strategy, with several PI3k inhibitors in development.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Phosphoinositide 3-kinase (PI3k) is a key regulator of intracellular signaling pathways.
- These pathways control critical cellular processes including proliferation, migration, survival, and angiogenesis.
- The PI3k pathway is frequently dysregulated in human cancers, making it a significant therapeutic target.
Purpose of the Study:
- To review the role of PI3k in cellular functions and cancer.
- To highlight the therapeutic potential of PI3k inhibitors in cancer treatment.
- To summarize existing and developing PI3k inhibitors.
Main Methods:
- Literature review of PI3k signaling pathways.
- Analysis of PI3k pathway's role in oncogenesis.
- Survey of reported PI3k inhibitors and their clinical status.
Main Results:
- PI3k pathway activation is crucial for cell growth and survival.
- Upregulation of PI3k signaling is a common event in various human cancers.
- Numerous potent PI3k inhibitors have been identified, with some progressing to clinical trials.
Conclusions:
- Inhibition of the PI3k pathway represents a promising strategy for cancer therapy.
- Ongoing research and development of PI3k inhibitors show potential for clinical application.
- A range of synthetic and natural product-based PI3k inhibitors are under investigation.
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