Abstract
The RING (Really Interesting New Gene) family is the largest type of E3 ubiquitin ligases. RING finger domains bind two zinc ions in a unique “cross-brace” arrangement through a defined motif of cysteine and histidine residues. This arrangement endows the RING domain with a globular conformation, characterized by a central α-helix and variable-length loops separated by several small β-strands. RING E3 ubiquitin ligases, play an essential role in the regulation of many biologic processes and defects in some of them are involved in cancer development. Furthermore, some RING E3 ligases are frequently overexpressed in human cancers. Today, RING ligases represent potentially molecular targets for disease intervention and could act as prognostic biomarkers. Targeting specific RING E3 ligases could lead to the development of a novel class of anticancer drugs. However RING fingers exhibit remarkable variations in their sequence and their topology characteristics. Structure determination of new RING finger domain is in the core of the design of new pharmaceuticals and what is presented in this article is a thorough review of achievements on the NMR or Xray structure determinations. Protein preparation protocols along with analysis of the structural features of known RING finger are also presented.
Keywords: Ubiquitin, E3 ubiquitin ligase, RING finger, zinc-coordination, anticancer drugs
Current Pharmaceutical Design
Title: RING Finger E3 Ubiquitin Ligases: Structure and Drug Discovery
Volume: 15 Issue: 31
Author(s): Christos T. Chasapis and Georgios A. Spyroulias
Affiliation:
Keywords: Ubiquitin, E3 ubiquitin ligase, RING finger, zinc-coordination, anticancer drugs
Abstract: The RING (Really Interesting New Gene) family is the largest type of E3 ubiquitin ligases. RING finger domains bind two zinc ions in a unique “cross-brace” arrangement through a defined motif of cysteine and histidine residues. This arrangement endows the RING domain with a globular conformation, characterized by a central α-helix and variable-length loops separated by several small β-strands. RING E3 ubiquitin ligases, play an essential role in the regulation of many biologic processes and defects in some of them are involved in cancer development. Furthermore, some RING E3 ligases are frequently overexpressed in human cancers. Today, RING ligases represent potentially molecular targets for disease intervention and could act as prognostic biomarkers. Targeting specific RING E3 ligases could lead to the development of a novel class of anticancer drugs. However RING fingers exhibit remarkable variations in their sequence and their topology characteristics. Structure determination of new RING finger domain is in the core of the design of new pharmaceuticals and what is presented in this article is a thorough review of achievements on the NMR or Xray structure determinations. Protein preparation protocols along with analysis of the structural features of known RING finger are also presented.
Export Options
About this article
Cite this article as:
Chasapis T. Christos and Spyroulias A. Georgios, RING Finger E3 Ubiquitin Ligases: Structure and Drug Discovery, Current Pharmaceutical Design 2009; 15 (31) . https://dx.doi.org/10.2174/138161209789271825
DOI https://dx.doi.org/10.2174/138161209789271825 |
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
-
Protein Phosphatase 1 and Its Complexes in Carcinogenesis
Current Cancer Drug Targets The Effect of Claudin-5 Overexpression on the Interactions of Claudin-1 and -2 and Barrier Function in Retinal Cells
Current Molecular Medicine Development and Application of Bioprobes for Mammalian Cell Cycle Analyses
Current Medicinal Chemistry Synthesis, Biological Evaluation and Molecular Dynamics Simulation Studies of Novel Diphenyl Ethers
Medicinal Chemistry Cathepsin D as a Promising Target for the Discovery of Novel Anticancer Agents
Current Cancer Drug Targets Cyclin-Dependent Kinase as a Novel Therapeutic Target: An Endless Story
Current Chemical Biology New Framework for the Discovery of PRC2 Inhibitors: Epigenetic Drugs
Current Drug Targets Novel Therapeutic Approaches to Regulate Human Dihydrofolate Reductase Activity and Expression
Current Enzyme Inhibition IP6 & Inositol in Cancer Prevention and Therapy
Current Cancer Therapy Reviews Drug Repurposing for Retinoblastoma: Recent Advances
Current Topics in Medicinal Chemistry Preclinical Studies of PROTACs in Hematological Malignancies
Cardiovascular & Hematological Disorders-Drug Targets Polymorphisms in Methotrexate Pathways: What Is Clinically Relevant, What Is Not, and What Is Promising
Current Drug Metabolism Subject Index To Volume 6
Current Molecular Medicine Telomere Maintenance Mechanisms in Cancer: Clinical Implications
Current Pharmaceutical Design DNA Methylation and Breast Cancer
Current Genomics Stem Cells: In Sickness and in Health
Current Stem Cell Research & Therapy Implications of Fibroblast Growth Factors (FGFs) in Cancer: From Prognostic to Therapeutic Applications
Current Drug Targets Exploiting APC Function as a Novel Cancer Therapy
Current Drug Targets 7-aa Peptide Mimic from HVR1 of HCV Protects Hepatic Injury in Rats by Reduced Expression of Key Pro-Inflammatory Factors
Inflammation & Allergy - Drug Targets (Discontinued) MicroRNAs in the Pathobiology of Multiple Myeloma
Current Cancer Drug Targets