Abstract
The PI3K/AKT/mTOR pathway is an intracellular signaling pathway, being important in apoptosis hence cancer such as breast cancer and non-small-cell lung cancer. It signaling axis controls cell proliferation and survival and has achieved major importance as a target for cancer therapy. The serine/threonine kinase Akt (also known as protein kinase B or PKB), since its initial discovery as a protooncogene, has become a major focus of attention because of its critical regulatory role in diverse cellular processes, including cancer progression and insulin metabolism. The Akt cascade is activated by receptor tyrosine kinases, integrins, B and T cell receptors, cytokine receptors, G protein coupled receptors and other stimuli that induce the production of phosphatidylinositol 3,4,5 triphosphates (PtdIns(3,4,5)P3) by phosphoinositide 3-kinase (PI3K). Therefore, PI3K plays an important role in in numerous cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking. In this review, we introduced the structure of the PI3K, and then focused on its biological activities. In addition, we reviewed the advances in the researches of PI3K as well as related inhibitors over the last couple of decades. Finally, we also discussed the prospect and developmental trend of phosphatidylinositol 3-kinase as antitumor agents.
Keywords: Antitumor agents, cancer therapy, G protein, phosphoinositide 3-kinase, PI3K/AKT/mTOR pathway, serine/threonine kinase Akt.
Anti-Cancer Agents in Medicinal Chemistry
Title:Advances in the Researches on the Biological Activities and Inhibitors of Phosphatidylinositol 3-kinase
Volume: 14 Issue: 5
Author(s): Jian-Feng Tang, Qing Wen, Jian Sun, Wei-Ming Zhang and Hai-Liang Zhu
Affiliation:
Keywords: Antitumor agents, cancer therapy, G protein, phosphoinositide 3-kinase, PI3K/AKT/mTOR pathway, serine/threonine kinase Akt.
Abstract: The PI3K/AKT/mTOR pathway is an intracellular signaling pathway, being important in apoptosis hence cancer such as breast cancer and non-small-cell lung cancer. It signaling axis controls cell proliferation and survival and has achieved major importance as a target for cancer therapy. The serine/threonine kinase Akt (also known as protein kinase B or PKB), since its initial discovery as a protooncogene, has become a major focus of attention because of its critical regulatory role in diverse cellular processes, including cancer progression and insulin metabolism. The Akt cascade is activated by receptor tyrosine kinases, integrins, B and T cell receptors, cytokine receptors, G protein coupled receptors and other stimuli that induce the production of phosphatidylinositol 3,4,5 triphosphates (PtdIns(3,4,5)P3) by phosphoinositide 3-kinase (PI3K). Therefore, PI3K plays an important role in in numerous cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking. In this review, we introduced the structure of the PI3K, and then focused on its biological activities. In addition, we reviewed the advances in the researches of PI3K as well as related inhibitors over the last couple of decades. Finally, we also discussed the prospect and developmental trend of phosphatidylinositol 3-kinase as antitumor agents.
Export Options
About this article
Cite this article as:
Tang Jian-Feng, Wen Qing, Sun Jian, Zhang Wei-Ming and Zhu Hai-Liang, Advances in the Researches on the Biological Activities and Inhibitors of Phosphatidylinositol 3-kinase, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (5) . https://dx.doi.org/10.2174/18715206113136660367
DOI https://dx.doi.org/10.2174/18715206113136660367 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
The Therapeutical Potential of a Novel Pterocarpanquinone LQB-118 to Target Inhibitor of Apoptosis Proteins in Acute Myeloid Leukemia Cells
Anti-Cancer Agents in Medicinal Chemistry Nicotine Replacement Therapy During Pregnancy and Lactation Induce Structural and Functional Changes in the Lungs of the Progeny
Current Women`s Health Reviews Subject Index to Volume 3
Current Medicinal Chemistry - Anti-Cancer Agents Advances in the Treatment of Ovarian Cancer Using PARP Inhibitors and the Underlying Mechanism of Resistance
Current Drug Targets The Molecular Bases of the Self-Renewal and Differentiation of Leukemic Stem Cells
Current Cancer Therapy Reviews Recent Advances in Heterocyclic Tubulin Inhibitors Targeting the Colchicine Binding Site
Anti-Cancer Agents in Medicinal Chemistry Deciphering the Systems Biology of mTOR Inhibition by Integrative Transcriptome Analysis
Current Pharmaceutical Design Antibody Development and Immunoassays for Polycyclic Aromatic Hydrocarbons (PAHs)
Current Organic Chemistry Intracellular Bioinorganic Chemistry and Cross Talk Among Different -Omics
Current Topics in Medicinal Chemistry NF-κB Down–regulation and PARP Cleavage by novel 3-α-butyryloxy-β-boswellic Acid Results in Cancer Cell Specific Apoptosis and in vivo Tumor Regression
Anti-Cancer Agents in Medicinal Chemistry DTCM-Glutarimide Hinders Growth of Childhood Leukemia Cells but Fails to Improve the Efficacy of Commonly Used Chemotherapeutic Agents
Current Bioactive Compounds Effects of Dietary Broccoli on Human in Vivo Caffeine Metabolism: A Pilot Study on a Group of Jordanian Volunteers
Current Drug Metabolism Methods for Biomarker Verification and Assay Development
Current Proteomics Design, Synthesis, and Evaluation of (2-(Pyridinyl)methylene)-1-tetralone Chalcones for Anticancer and Antimicrobial Activity
Medicinal Chemistry Review: The JAK/STAT Protein Activation – Role in Cancer Development and Targeted Therapy
Current Signal Transduction Therapy Anti-Cancer Effect of Melatonin via Downregulation of Delta-like Ligand 4 in Estrogen-Responsive Breast Cancer Cells
Recent Patents on Anti-Cancer Drug Discovery Isothiouronium Salts Reduce NRAS Expression, Induce Apoptosis and Decrease Invasion of Melanoma Cells
Anti-Cancer Agents in Medicinal Chemistry Methacholin Provocation Test in COPD and Healthy Smokers
Current Respiratory Medicine Reviews Technological Advances in Preclinical Drug Evaluation: The Role of -Omics Methods
Current Medicinal Chemistry Phytochemicals for Breast Cancer Therapy: Current Status and Future Implications
Current Cancer Drug Targets