Abstract
The serine / threonine phosphatases are inhibited by a variety of natural toxins, including the microcystins and nodularins. Progress in understanding the details of the biosynthetic origin and the binding of these compounds is discussed, as is the progress made in synthesizing the members of these families. Additionally, the work by several groups to either synthesize simplified analogues that are still potent, or introduce selectivity for PP1 over PP2A are discussed. Finally, the properties of a series of five new truncated analogues are examined.
Keywords: Microcystins, PP1, PP2A, threonine phosphatases
Current Medicinal Chemistry
Title: The Microcystins and Nodularins: Cyclic Polypeptide Inhibitors of PP1 and PP2A
Volume: 9 Issue: 22
Author(s): B. M. Gulledge, J. B. Aggen, H.- B. Huang, A. C. Nairn and A. R. Chamberlin
Affiliation:
Keywords: Microcystins, PP1, PP2A, threonine phosphatases
Abstract: The serine / threonine phosphatases are inhibited by a variety of natural toxins, including the microcystins and nodularins. Progress in understanding the details of the biosynthetic origin and the binding of these compounds is discussed, as is the progress made in synthesizing the members of these families. Additionally, the work by several groups to either synthesize simplified analogues that are still potent, or introduce selectivity for PP1 over PP2A are discussed. Finally, the properties of a series of five new truncated analogues are examined.
Export Options
About this article
Cite this article as:
Gulledge M. B., Aggen B. J., Huang B. H.-, Nairn C. A. and Chamberlin R. A., The Microcystins and Nodularins: Cyclic Polypeptide Inhibitors of PP1 and PP2A, Current Medicinal Chemistry 2002; 9 (22) . https://dx.doi.org/10.2174/0929867023368845
DOI https://dx.doi.org/10.2174/0929867023368845 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
Neglected Diseases - New Compounds and Treatments
Current Medicinal Chemistry Strategies for Small Molecule Library Design
Current Pharmaceutical Design Recent Advances in the Design and Synthesis of Small Molecule Carbonic Anhydrase IX Inhibitors
Current Topics in Medicinal Chemistry Aptamers Against COVID-19: An Untested Opportunity
Mini-Reviews in Medicinal Chemistry Tau Therapeutic Strategies for the Treatment of Alzheimers Disease
Current Topics in Medicinal Chemistry Deciphering Role of Cytokines for Therapeutic Strategies Against Rheumatoid Arthritis
Current Drug Targets Application of Pharmacophore Models for the Design and Synthesis of New Anticonvulsant Drugs
Mini-Reviews in Medicinal Chemistry Serum Procalcitonin Levels in Febrile Patients with Systemic Autoimmune Diseases
Current Rheumatology Reviews Progress Towards Liver and Lung-Directed Gene Therapy with Helper- Dependent Adenoviral Vectors
Current Gene Therapy Receptor Tryosine Kinase Inhibitors as Potent Weapons in War Against Cancers
Current Pharmaceutical Design Syntheses and Effect of Bombesin-Fragment6-14 and its Four Analogues on Food Intake in Rats
Current Pharmaceutical Biotechnology Effective Use of Drugs to Counter Chemical Terrorism
Current Drug Therapy Indole-based, Antiproliferative Agents Targeting Tubulin Polymerization
Current Topics in Medicinal Chemistry Downregulation of Membrane-bound Angiotensin Converting Enzyme 2 (ACE2) Receptor has a Pivotal Role in COVID-19 Immunopathology
Current Drug Targets Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
Current Medicinal Chemistry Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors
Current Medicinal Chemistry Molecular Targets for Modulating Lung Inflammation and Injury
Current Drug Targets Prediction of Small Molecules Metabolic Pathways Based on Functional Group Composition
Protein & Peptide Letters Estrogen Activates Classical and Alternative Mechanisms to Orchestrate Neuroprotection
Current Neurovascular Research A High Throughput, 384-Well, Semi-Automated, Hepatocyte Intrinsic Clearance Assay for Screening New Molecular Entities in Drug Discovery
Combinatorial Chemistry & High Throughput Screening