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
-
Structural Key Genes: Differentiating Lung Squamous Cell Carcinomas from Adenocarcinomas
Current Bioinformatics VDAC1 Mediated Anticancer Activity of Gallic Acid in Human Lung Adenocarcinoma A549 Cells
Anti-Cancer Agents in Medicinal Chemistry Pathobiology and Prevention of Cancer Chemotherapy-Induced Bone Growth Arrest, Bone Loss, and Osteonecrosis
Current Molecular Medicine Modulation of Cell Death in Age-Related Diseases
Current Pharmaceutical Design New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs
Current Neuropharmacology Small Molecule Inhibitors Targeting Key Proteins in the DNA Damage Response for Cancer Therapy
Current Medicinal Chemistry Role of Graphene Nano-Composites in Cancer Therapy: Theranostic Applications, Metabolic Fate and Toxicity Issues
Current Drug Metabolism FAK and Nanog Cross Talk with p53 in Cancer Stem Cells
Anti-Cancer Agents in Medicinal Chemistry A Review on Chemical Profile of Coumarins and their Therapeutic Role in the Treatment of Cancer
Current Drug Delivery Long Non-Coding RNA: An Emerging Paradigm of Pancreatic Cancer
Current Molecular Medicine Deubiquitinating Enzyme Inhibitors and their Potential in Cancer Therapy
Current Cancer Drug Targets Synthesis and Biological Evaluations of Cytotoxic and Antiangiogenic Triterpenoids-Jacaranone Conjugates
Medicinal Chemistry Antineoplastic Activity of Monocrotaline Against Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Dose and Sequence Dependent Synergism from the Combination of Oxaliplatin with Emetine and Patulin Against Colorectal Cancer
Anti-Cancer Agents in Medicinal Chemistry Cytotoxic T Cell Reponses Against Immunoglobulin in Malignant and Normal B Cells: Implications for Tumor Immunity and Autoimmunity
Current Pharmaceutical Design Cytokines as Novel Therapeutic Agents for Neuroinflammatory Disorders: A Role for Interferon-β in the Treatment of Multiple Sclerosis
Current Medicinal Chemistry - Central Nervous System Agents Chemomodulating Effects of Flavonoids in Human Leukemia Cells
Anti-Cancer Agents in Medicinal Chemistry Applications of Recombinant Adenovirus-p53 Gene Therapy for Cancers in the Clinic in China
Current Gene Therapy Anticancer Agents Derived from Natural Products
Mini-Reviews in Medicinal Chemistry Discovery of Anticancer Agents from 2-Pyrazoline-Based Compounds
Current Medicinal Chemistry