Abstract
This review includes an analysis of available X-ray and NMR structures of both members of the immunophilin family; cyclophilins and the FK-506 binding proteins (FKBPs). Available structures are compared and contrasted to highlight different structural features seen both within and between species. Each immunophilin family has been structurally characterised with a variety of small molecule ligands, principally immunosuppressive drugs and their analogues and an overview of these complexes is also presented. Currently the Protein Data Base contains over 60 entries for cyclophilins and over 40 entries for FKBPs. A number of FKBP related structures are also available including structures of MIP (Macrophage Infectivity Potentiator protein) from Legionella pneumophila and Trypanosoma cruzi and Trigger Factor from Mycoplasma genitalium. For all structures discussed in the review a summary of the available biological data is also presented.
Keywords: comparison of x-ray, nmr structures of cyclophilins and fkbps, variation among species, families of cyclophilin ligands and their structures, families of fkbp ligands and their structures, immunophilin protein complexes
Current Topics in Medicinal Chemistry
Title: Structures of Immunophilins and their Ligand Complexes
Volume: 3 Issue: 12
Author(s): Jacqueline Dornan, Paul Taylor and Malcolm D. Walkinshaw
Affiliation:
Keywords: comparison of x-ray, nmr structures of cyclophilins and fkbps, variation among species, families of cyclophilin ligands and their structures, families of fkbp ligands and their structures, immunophilin protein complexes
Abstract: This review includes an analysis of available X-ray and NMR structures of both members of the immunophilin family; cyclophilins and the FK-506 binding proteins (FKBPs). Available structures are compared and contrasted to highlight different structural features seen both within and between species. Each immunophilin family has been structurally characterised with a variety of small molecule ligands, principally immunosuppressive drugs and their analogues and an overview of these complexes is also presented. Currently the Protein Data Base contains over 60 entries for cyclophilins and over 40 entries for FKBPs. A number of FKBP related structures are also available including structures of MIP (Macrophage Infectivity Potentiator protein) from Legionella pneumophila and Trypanosoma cruzi and Trigger Factor from Mycoplasma genitalium. For all structures discussed in the review a summary of the available biological data is also presented.
Export Options
About this article
Cite this article as:
Dornan Jacqueline, Taylor Paul and Walkinshaw D. Malcolm, Structures of Immunophilins and their Ligand Complexes, Current Topics in Medicinal Chemistry 2003; 3 (12) . https://dx.doi.org/10.2174/1568026033451899
DOI https://dx.doi.org/10.2174/1568026033451899 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...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
-
Do Folate, Vitamins B<sub>6</sub> and B<sub>12</sub> Play a Role in the Pathogenesis of Migraine? The Role of Pharmacoepigenomics
CNS & Neurological Disorders - Drug Targets Conventional and Alternative Treatment Options for Allergic Rhinitis
Current Respiratory Medicine Reviews Globalization of Clinical Trials – Where are We Heading?
Current Clinical Pharmacology Screening Haemostasis – Looking for Global Assays: The Overall Haemostasis Potential (OHP) Method – A Possible Tool for Laboratory Investigation of Global Haemostasis in Both Hypo- and Hypercoagulable Conditions
Current Vascular Pharmacology Current Approach to the Diagnosis and Treatment of Femoral-Popliteal Arterial Disease. A Systematic Review
Current Cardiology Reviews Prognostic Parameters for Symptomatic Intracranial Hemorrhage after Intravenous Thrombolysis in Acute Ischemic Stroke in an Asian Population
Current Neurovascular Research An Insight into Biomarkers for Canine Parvovirus Diagnosis: A Minireview
Current Biomarkers (Discontinued) Identification of New Drug Targets and Biomarkers Related to Obesity and Eating Disorders: an Approach Based on Reward Deficit and Addiction
Current Pharmaceutical Design Assessment and Imaging of the Cerebrovascular Glycocalyx
Current Neurovascular Research Diltiazem Analogues: The Last Ten Years on Structure Activity Relationships
Current Medicinal Chemistry COVID-19 in People with Diabetes: Perspectives from Saudi Arabia
Current Diabetes Reviews Autologous Cell Therapy for Vascular Regeneration: The Role of Proangiogenic Cells
Current Medicinal Chemistry Evolution of Antipsychotic Intervention in the Schizophrenic Psychosis
Current Drug Targets Coronary Atherosclerosis The Implications of Being a Woman
Current Hypertension Reviews Searching for Disease-Modifying Drugs in AD: Can We Combine Neuropsychological Tools with Biological Markers?
CNS & Neurological Disorders - Drug Targets Peptide-Derived Protease-Activated Receptor-1 (PAR-1) Antagonists
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Compendious Review on Bioactive Constituents and Pharmacotherapeutic Profile of Heliotropium indicum Linn
The Natural Products Journal Cilostazol: A New Drug in the Treatment Intermittent Claudication
Recent Patents on Cardiovascular Drug Discovery Potassium Channels: Novel Emerging Biomarkers and Targets for Therapy in Cancer
Recent Patents on Anti-Cancer Drug Discovery Improvement of Microscopic MR Imaging of Amyloid Plaques with Targeting and Non-Targeting Contrast Agents
Current Medical Imaging