Abstract
We would like to review the recent study of the inhibitors for peptidyl-prolyl cis/trans isomerase (PPIase), such as cyclophilin (Cyp), FK506- binding protein (FKBP) and Pin1. The inhibitors of Cyp and FKBP, CsA and FK506 respectively are well known potent immunosuppressive drugs. However, they cause a variety of side- effects. Therefore efforts are under way to identify PPIase inhibitors with less side- effects. In this review, efforts of discovering small molecule inhibitors are emphasized. While Cyp and FKBP inhibitors have been explored fairly thoroughly, the number of efforts to screen inhibitors of Pin1 is still limited so far. We think that the inhibitor of Pin1 has high potential as a drug.
Keywords: Peptidyl-prolyl cis/trans isomerases, cyclophilin, FK-506 binding protein, Pin1, small molecule inhibitors
Current Enzyme Inhibition
Title: Small Molecule Inhibitors of Peptidylprolyl cis/trans Isomerase
Volume: 6 Issue: 1
Author(s): Tadashi Mori and Takafumi Uchida
Affiliation:
Keywords: Peptidyl-prolyl cis/trans isomerases, cyclophilin, FK-506 binding protein, Pin1, small molecule inhibitors
Abstract: We would like to review the recent study of the inhibitors for peptidyl-prolyl cis/trans isomerase (PPIase), such as cyclophilin (Cyp), FK506- binding protein (FKBP) and Pin1. The inhibitors of Cyp and FKBP, CsA and FK506 respectively are well known potent immunosuppressive drugs. However, they cause a variety of side- effects. Therefore efforts are under way to identify PPIase inhibitors with less side- effects. In this review, efforts of discovering small molecule inhibitors are emphasized. While Cyp and FKBP inhibitors have been explored fairly thoroughly, the number of efforts to screen inhibitors of Pin1 is still limited so far. We think that the inhibitor of Pin1 has high potential as a drug.
Export Options
About this article
Cite this article as:
Mori Tadashi and Uchida Takafumi, Small Molecule Inhibitors of Peptidylprolyl cis/trans Isomerase, Current Enzyme Inhibition 2010; 6 (1) . https://dx.doi.org/10.2174/157340810790712005
DOI https://dx.doi.org/10.2174/157340810790712005 |
Print ISSN 1573-4080 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6662 |
- 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
Related Articles
-
Inflammation: Beneficial or Detrimental After Spinal Cord Injury?
Recent Patents on CNS Drug Discovery (Discontinued) Fluorescent Carbon Dots and Nanodiamonds for Biological Imaging: Preparation, Application, Pharmacokinetics and Toxicity
Current Drug Metabolism Interactions Between Nanosized Materials and the Brain
Current Medicinal Chemistry Cell-Selective Mitochondrial Targeting: Progress in Mitochondrial Medicine
Current Drug Delivery Non-Genotoxic p53-Activators and their Significance as Antitumor Therapy of Future
Current Medicinal Chemistry Molecular Chaperone Activity and Biological Regulatory Actions of the TPR-Domain Immunophilins FKBP51 and FKBP52
Current Protein & Peptide Science Tumor Promoters - Microcystin-LR, Nodularin and TNF-α and Human Cancer Development
Anti-Cancer Agents in Medicinal Chemistry Prion Diseases: Time for a Therapy ?
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Novel Chemotherapeutic Agents - The Contribution of Scorpionates
Current Medicinal Chemistry Neuroglobin and Estrogen Receptors: A New Pathway of Cell Survival and Cell Death Balance
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Manipulation of Glycolysis in Malignant Tumors: Fantasy or Therapy?
Current Medicinal Chemistry Metal Ions and Metal Complexes in Alzheimer’s Disease
Current Pharmaceutical Design Insights on the Structure of Amyloid Fibrils from Site-Directed Mutagenesis
Protein & Peptide Letters Isoindole Derivatives: Propitious Anticancer Structural Motifs
Current Topics in Medicinal Chemistry Ganglioside GM3 and Its Role in Cancer
Current Medicinal Chemistry The Role of Neuronal Insulin/Insulin-Like Growth Factor-1 Signaling for the Pathogenesis of Alzheimer’s Disease: Possible Therapeutic Implications
CNS & Neurological Disorders - Drug Targets Pulmonary Circulation and Pulmonary Function in Neonatal Lung Hypoplasia:Treatment with Corticosteroids
Current Pediatric Reviews The Influence of Cox-2 and Bioactive Lipids on Hematological Cancers
Current Angiogenesis (Discontinued) Neuronal and Extraneuronal Nicotinic Acetylcholine Receptors
Current Neuropharmacology Synthesis, Structure-Activity Relationships and Biological Activity of New Isatin Derivatives as Tyrosinase Inhibitors
Current Topics in Medicinal Chemistry