Abstract
FK506 binding protein 51 (FKBP51) is an immunophilin physiologically expressed in lymphocytes. Very recently, aberrant expression of this protein was found in melanoma; FKBP51 expression correlates with melanoma aggressiveness and is maximal in metastatic lesions. FKBP51 promotes NF-κB activation and is involved in the resistance to genotoxic agents, including anthracyclines and ionizing radiation. FKBP51 is a cochaperone with peptidyl-prolyl isomerase activity that regulates several biological processes through protein-protein interaction. There is increasing evidence that FKBP51 hyperexpression is associated with cancer and this protein has a relevant role in sustaining cell growth, malignancy, and resistance to therapy. There is also evidence that FKBP ligands are potent anticancer agents, in addition to their immunosuppressant activity. In particular, rapamycin and its analogs have shown antitumor activity across a variety of human cancers in clinical trials. Although, classically, rapamycin actions are ascribed to inhibition of mTOR, recent studies indicate FKBP51 is also an important molecular determinant of the drugs anticancer activity. The aim of this article is to review the functions of FKBP51, especially in view of the recent findings that this protein is a potential oncogene when deregulated and a candidate target for signaling therapies against cancer.
Keywords: FKBP51, cancer, apoptosis, NF-κB, rapamycin, FK506 binding protein, immunophilin, physiologically expressed, lymphocytes, melanoma aggressiveness
Current Medicinal Chemistry
Title: The Emerging Role of Large Immunophilin FK506 Binding Protein 51 in Cancer
Volume: 18 Issue: 35
Author(s): S. Romano, A. Sorrentino, A. L. Di Pace, G. Nappo, C. Mercogliano and M. F. Romano
Affiliation:
Keywords: FKBP51, cancer, apoptosis, NF-κB, rapamycin, FK506 binding protein, immunophilin, physiologically expressed, lymphocytes, melanoma aggressiveness
Abstract: FK506 binding protein 51 (FKBP51) is an immunophilin physiologically expressed in lymphocytes. Very recently, aberrant expression of this protein was found in melanoma; FKBP51 expression correlates with melanoma aggressiveness and is maximal in metastatic lesions. FKBP51 promotes NF-κB activation and is involved in the resistance to genotoxic agents, including anthracyclines and ionizing radiation. FKBP51 is a cochaperone with peptidyl-prolyl isomerase activity that regulates several biological processes through protein-protein interaction. There is increasing evidence that FKBP51 hyperexpression is associated with cancer and this protein has a relevant role in sustaining cell growth, malignancy, and resistance to therapy. There is also evidence that FKBP ligands are potent anticancer agents, in addition to their immunosuppressant activity. In particular, rapamycin and its analogs have shown antitumor activity across a variety of human cancers in clinical trials. Although, classically, rapamycin actions are ascribed to inhibition of mTOR, recent studies indicate FKBP51 is also an important molecular determinant of the drugs anticancer activity. The aim of this article is to review the functions of FKBP51, especially in view of the recent findings that this protein is a potential oncogene when deregulated and a candidate target for signaling therapies against cancer.
Export Options
About this article
Cite this article as:
Romano S., Sorrentino A., L. Di Pace A., Nappo G., Mercogliano C. and F. Romano M., The Emerging Role of Large Immunophilin FK506 Binding Protein 51 in Cancer, Current Medicinal Chemistry 2011; 18 (35) . https://dx.doi.org/10.2174/092986711798194333
DOI https://dx.doi.org/10.2174/092986711798194333 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
Repurposing Drugs for Cancer Prevention
Current Topics in Medicinal Chemistry Potential Disease Targets for Drugs that Disrupt Protein - Protein Interactions of Grb2 and Crk Family Adaptors
Current Pharmaceutical Design Development of Taxol and Other Endophyte Produced Anti-Cancer Agents
Recent Patents on Anti-Cancer Drug Discovery Discovery and Development of Topoisomerase Inhibitors as Anticancer Agents
Mini-Reviews in Medicinal Chemistry AMPK as a Potential Anticancer Target - Friend or Foe?
Current Pharmaceutical Design Inhibition of Angiogenesis as a Treatment Strategy for Neuroblastoma
Current Cancer Therapy Reviews Intravesical Drug Delivery into the Bladder to Treat Cancers
Current Drug Delivery Role of the Akt Pathway in Prostate Cancer
Current Cancer Drug Targets Co-delivery of Plasmid DNA and Antisense Oligodeoxyribonucleotide into Human Carcinoma Cells by Cationic Liposomes
Current Pharmaceutical Biotechnology Induction of GST and Related Events by Dietary Phytochemicals: Sources, Chemistry, and Possible Contribution to Chemoprevention
Current Topics in Medicinal Chemistry Molecular and Cellular Activities of Vitamin E Analogues
Mini-Reviews in Medicinal Chemistry Anti-Angiogenic Therapy: Strategies to Develop Potent VEGFR-2 Tyrosine Kinase Inhibitors and Future Prospect
Current Medicinal Chemistry S100A1: Structure, Function, and Therapeutic Potential
Current Chemical Biology Regulating TRAIL Receptor-Induced Cell Death at the Membrane: A Deadly Discussion
Recent Patents on Anti-Cancer Drug Discovery Evaluation of the Influence of the Conjugation Site of the Chelator Agent HYNIC to GLP1 Antagonist Radiotracer for Insulinoma Diagnosis
Current Radiopharmaceuticals Polyunsaturated Fatty Acids in Pregnancy and Metabolic Syndrome: A Review
Current Pharmaceutical Biotechnology Pregnancy and Postpartum Influences on Rheumatoid Arthritis Activity:Natures Model to Investigate Systemic Biological Mechanisms in the Disease
Current Rheumatology Reviews Role of microRNAs on Blood Brain Barrier Dysfunction in Vascular Cognitive Impairment
Current Drug Delivery Involvement of Cysteine Proteases in Cancer
Current Medicinal Chemistry Isolation and Characterization of a Lectin from Japanese Mottled Beans
Protein & Peptide Letters