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
-
Small Peptide and Protein-based Molecular Probes for Imaging Neurological Diseases
Current Protein & Peptide Science Transferrin and the Transferrin Receptor: Of Magic Bullets and Other Concerns
Inflammation & Allergy - Drug Targets (Discontinued) The MYCN Oncogene as a Specific and Selective Drug Target for Peripheral and Central Nervous System Tumors
Current Cancer Drug Targets Betulinic Acid as a Potent and Complex Antitumor Phytochemical: A Minireview
Anti-Cancer Agents in Medicinal Chemistry Pharmacological Approaches of Neurofibrillary Degeneration
Current Alzheimer Research Nutritional Approaches to Modulate Oxidative Stress in Alzheimers Disease
Current Alzheimer Research Novel Colchicine Derivatives and their Anti-cancer Activity
Current Topics in Medicinal Chemistry Protein Kinases as Tumor Biomarkers and Therapeutic Targets
Current Pharmaceutical Design Immunomodulatory Properties of Antibiotics
Current Molecular Pharmacology Radiosensitizing Potential of Epigenetic Anticancer Drugs
Anti-Cancer Agents in Medicinal Chemistry Implication of Green Tea as a Possible Therapeutic Approach for Parkinson Disease
CNS & Neurological Disorders - Drug Targets Schizophrenia: Redox Regulation and Volume Neurotransmission
Current Neuropharmacology The Clinical Impact of Quantitative Cell-free DNA, KRAS, and BRAF Mutations on Response to Anti-EGFR Treatment in Patients with Metastatic Colorectal Cancer
Current Pharmaceutical Design Immunotoxins Constructed with Ribosome-Inactivating Proteins and their Enhancers: A Lethal Cocktail with Tumor Specific Efficacy
Current Pharmaceutical Design The Tachykinergic System as Avenues for Drug Intervention
Recent Patents on CNS Drug Discovery (Discontinued) Cancer Cell Reprogramming: Stem Cell Differentiation Stage Factors and An Agent Based Model to Optimize Cancer Treatment
Current Pharmaceutical Biotechnology Molecular Targeted Approaches to Cancer Therapy and Prevention Using Chalcones
Current Cancer Drug Targets Non-Homologous DNA End Joining in Anticancer Therapy
Current Cancer Drug Targets Exploiting Protein Phosphatase Inhibitors Based on Cantharidin Analogues for Cancer Drug Discovery
Mini-Reviews in Medicinal Chemistry Diagnostic and Therapeutic Uses of Nanomaterials in the Brain
Current Medicinal Chemistry