Abstract
Phosphoinositide 3-kinases (PI3K) represent a family of intracellular signaling proteins, which control a variety of important cellular functions such as proliferation, apoptosis and migration. Recent findings suggest an involvement of PI3K in the pathogenesis of numerous diseases including cancer, heart failure and autoimmune / inflammatory disorders. This review summarizes the current knowledge of the emerging therapeutic value of PI3K as targets for the intervention of several pathological disorders and in particular focusing on oncogenesis. A brief introduction on the molecular and biochemical features of these signaling proteins will be followed by a depiction of signaling interactions of PI3K in a cellular context. PI3K dependent signaling involved in the control of cell growth, proliferation, survival and cytoskeletal remodeling and the link to cellular dysfunctions will be discussed. Further we will summarize the phenotypic consequences by genetic targeting PI3K signaling in mice. In its final part this review outlines challenges and activities considering PI3K as targets for therapeutic intervention and progress in the development of first generation small molecule inhibitors.
Keywords: pI 3-kinase, target, inhibitor, signal transduction, cancer, inflammation
Current Pharmaceutical Design
Title: Phosphoinositide 3-Kinases as Targets for Therapeutic Intervention
Volume: 10 Issue: 16
Author(s): Reinhard Wetzker and Christian Rommel
Affiliation:
Keywords: pI 3-kinase, target, inhibitor, signal transduction, cancer, inflammation
Abstract: Phosphoinositide 3-kinases (PI3K) represent a family of intracellular signaling proteins, which control a variety of important cellular functions such as proliferation, apoptosis and migration. Recent findings suggest an involvement of PI3K in the pathogenesis of numerous diseases including cancer, heart failure and autoimmune / inflammatory disorders. This review summarizes the current knowledge of the emerging therapeutic value of PI3K as targets for the intervention of several pathological disorders and in particular focusing on oncogenesis. A brief introduction on the molecular and biochemical features of these signaling proteins will be followed by a depiction of signaling interactions of PI3K in a cellular context. PI3K dependent signaling involved in the control of cell growth, proliferation, survival and cytoskeletal remodeling and the link to cellular dysfunctions will be discussed. Further we will summarize the phenotypic consequences by genetic targeting PI3K signaling in mice. In its final part this review outlines challenges and activities considering PI3K as targets for therapeutic intervention and progress in the development of first generation small molecule inhibitors.
Export Options
About this article
Cite this article as:
Wetzker Reinhard and Rommel Christian, Phosphoinositide 3-Kinases as Targets for Therapeutic Intervention, Current Pharmaceutical Design 2004; 10 (16) . https://dx.doi.org/10.2174/1381612043384402
DOI https://dx.doi.org/10.2174/1381612043384402 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Ivabradine for Treatment of Coronary Artery Disease: From Last Chance Resort to Mainstem of a Reasoned Therapy
Cardiovascular & Hematological Agents in Medicinal Chemistry Interfering with Hedgehog Pathway: New Avenues for Targeted Therapy in Rhabdomyosarcoma
Current Drug Targets <i>Nigella sativa</i> – A Functional Spice From A Pharaoh’s Tomb to Modern Healthcare
The Natural Products Journal Changes in the Expression of the Alzheimers Disease-Associated Presenilin Gene in Drosophila Heart Leads to Cardiac Dysfunction
Current Alzheimer Research G Protein-Coupled Receptor Fusion Proteins in Drug Discovery
Current Pharmaceutical Design Role of Nanomedicine in Hepatic Targeting- Deciphering Strategies with Molecular Insights and Preclinical Prospects
Drug Delivery Letters Thiazolidinediones and Cardiovascular Risk — A Question of Balance
Current Cardiology Reviews Hormonal, Metabolic and Hemodynamic Adaptations to Glycosuria in Type 2 Diabetes Patients Treated with Sodium-Glucose Co-Transporter Inhibitors
Current Diabetes Reviews Bipolar Affective Disorder in Young People: A Review
Adolescent Psychiatry Ligand-Based Peptide Design and Combinatorial Peptide Libraries to Target G Protein-Coupled Receptors
Current Pharmaceutical Design Biomarkers Associated with Atrial Fibrosis and Remodeling
Current Medicinal Chemistry Morbidity and Mortality Associated with Pharmacotherapy. Evolution and Current Concept of Drug-Related Problems
Current Pharmaceutical Design Safety Limits of Antidepressant Use Plus Combinations: Focus on Cardiovascular Function
Current Drug Metabolism In-Vivo Gene Delivery by Sonoporation: Recent Progress and Prospects
Current Gene Therapy Drug Treatment of Metabolic Syndrome
Current Clinical Pharmacology Novel Therapeutic Targets for Diabetic Nephropathy
Endocrine, Metabolic & Immune Disorders - Drug Targets Calcium Ions in Inherited Cardiomyopathies
Medicinal Chemistry COPD Evaluation: Beyond the Airway Obstruction, a Follow Up
Current Respiratory Medicine Reviews Triiodothyronine (T3) Effects on Cardiovascular System in Patients with Heart Failure
Recent Patents on Cardiovascular Drug Discovery Novel Anticoagulants vs Warfarin for Stroke Prevention in Atrial Fibrillation
Cardiovascular & Hematological Disorders-Drug Targets