Abstract
Phosphatase and tensin homologue deleted on chromosome 10 (PTEN) is one of the most frequently disrupted tumor suppressors in cancer. The lipid phosphatase activity of PTEN antagonizes the phosphatidylinositol 3-kinase (PI3K)/AKT/mTOR pathway to repress tumor cell growth and survival. In the nucleus, PTEN promotes chromosome stability and DNA repair. Consequently, loss of PTEN function increases genomic instability. PTEN deficiency is caused by inherited germline mutations, somatic mutations, epigenetic and transcriptional silencing, post-translational modifications, and protein-protein interactions. Given the high frequency of PTEN deficiency across cancer subtypes, therapeutic approaches that exploit PTEN loss-of-function could provide effective treatment strategies. Herein, we discuss therapeutic strategies aimed at cancers with loss of PTEN function, and the challenges involved in treating patients afflicted with such cancers. We review preclinical and clinical findings, and highlight novel strategies under development to target PTENdeficient cancers.
Keywords: Cancer, phosphatase, targeted therapy, tumor, tumor suppressor, PI3K, mTOR, synthetic lethal.
Current Drug Targets
Title:Therapeutic Targeting of Cancers with Loss of PTEN Function
Volume: 15 Issue: 1
Author(s): Lloye M. Dillon and Todd W. Miller
Affiliation:
Keywords: Cancer, phosphatase, targeted therapy, tumor, tumor suppressor, PI3K, mTOR, synthetic lethal.
Abstract: Phosphatase and tensin homologue deleted on chromosome 10 (PTEN) is one of the most frequently disrupted tumor suppressors in cancer. The lipid phosphatase activity of PTEN antagonizes the phosphatidylinositol 3-kinase (PI3K)/AKT/mTOR pathway to repress tumor cell growth and survival. In the nucleus, PTEN promotes chromosome stability and DNA repair. Consequently, loss of PTEN function increases genomic instability. PTEN deficiency is caused by inherited germline mutations, somatic mutations, epigenetic and transcriptional silencing, post-translational modifications, and protein-protein interactions. Given the high frequency of PTEN deficiency across cancer subtypes, therapeutic approaches that exploit PTEN loss-of-function could provide effective treatment strategies. Herein, we discuss therapeutic strategies aimed at cancers with loss of PTEN function, and the challenges involved in treating patients afflicted with such cancers. We review preclinical and clinical findings, and highlight novel strategies under development to target PTENdeficient cancers.
Export Options
About this article
Cite this article as:
Dillon M. Lloye and Miller W. Todd, Therapeutic Targeting of Cancers with Loss of PTEN Function, Current Drug Targets 2014; 15 (1) . https://dx.doi.org/10.2174/1389450114666140106100909
DOI https://dx.doi.org/10.2174/1389450114666140106100909 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...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
Related Articles
-
Inhibition of Proliferation of ECV304 Cells by a Disintegrin from Chinese Green Tree Viper
Protein & Peptide Letters Trans-Platinum Complexes as Anticancer Drugs: Recent Developments and Future Prospects
Current Medicinal Chemistry The Effect of PDE5 Inhibitors on the Male Reproductive Tract
Current Pharmaceutical Design PET Tracers Based on Zirconium-89
Current Radiopharmaceuticals Fighting Fire with Fire: A Patent for the Combined Application of Oncolytic Herpes Viruses and Antiangiogenic Agents in the Battle Against Human Cancers
Recent Patents on Anti-Cancer Drug Discovery Impaired Autophagy Mediates Resistance to Low-Dose Metronomic Cyclophosphamide Chemotherapy
Clinical Cancer Drugs Delta Np63 alpha – Responsive microRNA Modulate the Expression of Metabolic Enzymes
Current Pharmaceutical Biotechnology Assortment of Human Amniotic Membrane and Curcumin: a Potential Therapeutic Strategy for Burn Wound Healing
Current Drug Therapy Animal Models of Carcinogenesis in Inflamed Colorectum: Potential Use in Chemoprevention Study
Current Drug Targets In Vitro Regulatory Effect of Epididymal Serpin CRES on Protease Activity of Proprotein Convertase PC4/PCSK4
Current Molecular Medicine A Review of the Effects of Gold, Silver, Selenium, and Zinc Nanoparticles on Diabetes Mellitus in Murine Models
Mini-Reviews in Medicinal Chemistry Advances in Nanomedicine Towards Clinical Application in Oncology and Immunology
Current Pharmaceutical Biotechnology Radiobromine-Labelled Tracers for Positron Emission Tomography: Possibilities and Pitfalls
Current Radiopharmaceuticals Anticancer and Cytotoxic Activities of [Cu(C6H16N2O2)2][Ni(CN)4] and [Cu(C6H16N2O2)Pd(CN)4] Cyanidometallate Compounds on HT29, HeLa, C6 and Vero Cell Lines
Anti-Cancer Agents in Medicinal Chemistry A Sialic Acid-Specific Lectin from the Mushroom Paecilomyces Japonica that Exhibits Hemagglutination Activity and Cytotoxicity
Protein & Peptide Letters The Rational Design of Anticancer Platinum Complexes: The Importance of the Structure-Activity Relationship
Current Medicinal Chemistry Genetics of Bladder Malignant Tumors in Childhood
Current Genomics An Insight into Drug Repositioning for the Development of Novel Anti-Cancer Drugs
Current Topics in Medicinal Chemistry COX Selectivity and Animal Models for Colon Cancer
Current Pharmaceutical Design Patent Selections
Recent Patents on Regenerative Medicine