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
-
Inhibition of Matrix Metalloproteinases (MMPs) as a Potential Strategy to Ameliorate Hypertension-Induced Cardiovascular Alterations
Current Drug Targets Rheumatoid Arthritis and Cardiovascular Risk: Between Lights and Shadows
Current Rheumatology Reviews Monoclonal Antobodies: Application in Radiopharmacy
Current Radiopharmaceuticals Long-Term Use of Short- and Long-Acting Nitrates in Stable Angina Pectoris
Current Clinical Pharmacology Pathophysiology of Arterial Hypertension: Insights from Pediatric Studies
Current Pediatric Reviews Beta-2 Agonists in Asthma: Medicine or Murderer?
Current Respiratory Medicine Reviews Patented Small Molecules Used for Reprogramming
Recent Patents on Regenerative Medicine Role of Wnt Signaling in Tissue Fibrosis, Lessons from Skeletal Muscle and Kidney
Current Molecular Medicine Neurotransmission Alterations in Central Cardiovascular Control in Experimental Hypertension
Current Hypertension Reviews Genomics and the Prospects of Existing and Emerging Therapeutics for Cardiovascular Diseases
Current Pharmaceutical Design Blood Pressure Lowering and Outcomes in type 2 Diabetes: Implications of the Blood Pressure-Lowering Arm of the Advance Trial
Current Hypertension Reviews Tyrosine Kinase Inhibitors – A Review on Pharmacology, Metabolism and Side Effects
Current Drug Metabolism Herbal and Traditional Chinese Medicine for the Treatment of Cardiovascular Complications in Diabetes Mellitus
Current Diabetes Reviews Theoretical and Evidence-Based Benefit of Afterload Reduction in the Postoperative Pediatric Heart
Current Vascular Pharmacology The Control of Arterial Hypertension: Epidemiological and Economic Challenge
Current Hypertension Reviews Pneumonia in the Elderly
Current Respiratory Medicine Reviews Neuregulin1 as Novel Therapy for Heart Failure
Current Pharmaceutical Design Impact of Clinical Audit on Adherence to the Guidelines Directed Medical Therapy in Patients Admitted with Heart Failure
Current Drug Safety Effects of Oxymatrine from Ku Shen on Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Patent Selections :
Recent Patents on Cardiovascular Drug Discovery