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
-
Anti-Tumor Efficacy of Pyrvinium Pamoate Nanoliposomes in an Experimental Model of Melanoma
Anti-Cancer Agents in Medicinal Chemistry Monitoring of Treatment-Induced Apoptosis in Oncology with PET and SPECT
Current Pharmaceutical Design Cancer Cell Cannibalism: A Primeval Option to Survive.
Current Molecular Medicine Identification of KEY lncRNAs and mRNAs Associated with Oral Squamous Cell Carcinoma Progression
Current Bioinformatics Secondary Hypertension: The Ways of Management
Current Vascular Pharmacology The Scatter Factor Signaling Pathways as Therapeutic Associated Target in Cancer Treatment
Current Medicinal Chemistry Peroxynitrite-Mediated Structural Changes in Histone H2A: Biochemical and Biophysical Analysis
Protein & Peptide Letters Tumor Stroma as a Target in Cancer
Current Cancer Drug Targets Peptides Targeting Angiogenesis Related Growth Factor Receptors
Current Pharmaceutical Design Garlic (<i>Allium sativum</i> L.): Its Chemistry, Nutritional Composition, Toxicity, and Anticancer Properties
Current Topics in Medicinal Chemistry Polymorphisms of Human N-Acetyltransferases and Cancer Risk
Current Drug Metabolism Is it Necessary to Calculate Young’s Modulus in AFM Nanoindentation Experiments Regarding Biological Samples?
Micro and Nanosystems Novel Marine-Derived Anti-Cancer Agents
Current Pharmaceutical Design Bioremediation of Toxic Heavy Metals: A Patent Review
Recent Patents on Biotechnology Too Much of a Good Thing: Suicide Prevention Promotes Chemoresistance in Ovarian Carcinoma
Current Cancer Drug Targets (Review Article) Screening for Disease-Markers and Investigating Drug Effects by Proteome Profiling: Can it Meet Expectations?
Combinatorial Chemistry & High Throughput Screening From TGF-β to Cancer Therapy
Current Drug Targets Clinical Trials of Targeted Alpha Therapy for Cancer
Reviews on Recent Clinical Trials Enzyme / Abzyme Prodrug Activation Systems: Potential Use in Clinical Oncology
Current Pharmaceutical Design Resistance to Anti-VEGF Agents
Current Pharmaceutical Design