Abstract
Cellular signalling processes are governed by a delicate balance of phosphatase and kinase activity. Over the past few years there has been considerable effort directed toward the development of kinase based therapeutic agents, whilst phosphatase based therapeutics have lagged. Herein we address key issues relating to selected therapeutic targets: malignancy, diabetes, immunosuppression, cystic fibrosis, asthma and cardiovascular disease. As part of ongoing studies we examine the recent developments in understanding the key interactions between the okadaic acid class of compounds and the serine / threonine protein phosphatases 1, 2A and 2B. Crystal structure and molecular modelling guided inhibitor development is also a key focus of this article.
Keywords: protein phosphatase inhibition, structure based design, okadaic acid, serine/threonine protein phosphatases
Current Pharmaceutical Design
Title: Protein Phosphatase Inhibition: Structure Based Design. Towards New Therapeutic Agents
Volume: 10 Issue: 10
Author(s): Jennette A. Sakoff and Adam McCluskey
Affiliation:
Keywords: protein phosphatase inhibition, structure based design, okadaic acid, serine/threonine protein phosphatases
Abstract: Cellular signalling processes are governed by a delicate balance of phosphatase and kinase activity. Over the past few years there has been considerable effort directed toward the development of kinase based therapeutic agents, whilst phosphatase based therapeutics have lagged. Herein we address key issues relating to selected therapeutic targets: malignancy, diabetes, immunosuppression, cystic fibrosis, asthma and cardiovascular disease. As part of ongoing studies we examine the recent developments in understanding the key interactions between the okadaic acid class of compounds and the serine / threonine protein phosphatases 1, 2A and 2B. Crystal structure and molecular modelling guided inhibitor development is also a key focus of this article.
Export Options
About this article
Cite this article as:
Sakoff A. Jennette and McCluskey Adam, Protein Phosphatase Inhibition: Structure Based Design. Towards New Therapeutic Agents, Current Pharmaceutical Design 2004; 10 (10) . https://dx.doi.org/10.2174/1381612043452686
DOI https://dx.doi.org/10.2174/1381612043452686 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
-
New Therapies to Modulate Post-Infarction Inflammatory Alterations in the Myocardium: State of the Art and Forthcoming Applications
Current Radiopharmaceuticals Oxidative-Nitrosative Stress In Hypertension
Current Vascular Pharmacology Therapeutic Strategies of Plant-derived Compounds for Diabetes Via Regulation of Monocyte Chemoattractant Protein-1
Current Medicinal Chemistry Outcomes of Patients with Chronic Heart Failure and Iron Deficiency Treated with Intravenous Iron: A Meta-analysis
Cardiovascular & Hematological Disorders-Drug Targets Cancer Proteomics: New Horizons and Insights into Therapeutic Applications
Current Proteomics The Role of Negative Costimulators During Parasitic Infections
Endocrine, Metabolic & Immune Disorders - Drug Targets Free Fatty Acids: Circulating Contributors of Metabolic Syndrome
Cardiovascular & Hematological Agents in Medicinal Chemistry The Right Ventricle: Biologic Insights and Response to Disease
Current Cardiology Reviews Biomarker Assays for Personalised Stroke Risk Assessment in Atrial Fibrillation
Cardiovascular & Hematological Disorders-Drug Targets Meet Our Editorial Board Member:
Current Diabetes Reviews Cardiovascular Aspect of Beta-Thalassaemia
Cardiovascular & Hematological Agents in Medicinal Chemistry Curcumin, Hesperidin, and Rutin Selectively Interfere with Apoptosis Signaling and Attenuate Streptozotocin-Induced Oxidative Stress- Mediated Hyperglycemia
Current Neurovascular Research Phytochemicals and Cancer Stem Cells: A Pancreatic Cancer Overview
Current Chemical Biology Short-term RR-Interval Power Spectral Analysis as a New Tool to Stratify the Risk of Sudden Death in Various Cardiovascular Conditions
Vascular Disease Prevention (Discontinued) Aetiology, Diagnosis and Treatment of Hydrops Foetalis
Current Pediatric Reviews A Review of Patents Relating to Therapeutic Angiogenesis Using Endothelial Progenitors and Other Vasculogenesis-Related Cell Types
Recent Patents on Regenerative Medicine Artificial Intelligence for Epigenetics: Towards Personalized Medicine
Current Medicinal Chemistry New Insights in Drug-Induced Mitochondrial Toxicity
Current Pharmaceutical Design Function and Expression Pattern of Nonsyndromic Deafness Genes
Current Molecular Medicine Stem Cell Therapy for the Treatment of Myocardial Infarction
Current Pharmaceutical Design